Search Result
Results for "
Muscarinic receptor antagonist
" in MedChemExpress (MCE) Product Catalog:
41
Isotope-Labeled Compounds
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
-
- HY-17366
-
|
|
Drug Metabolite
mAChR
Dopamine Receptor
|
Neurological Disease
|
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Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
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-
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- HY-17366A
-
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mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
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Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride cannot cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
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-
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- HY-14539
-
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HF 1854; ZINC000019796155
|
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
Ligands for E3 Ligase
|
Neurological Disease
Cancer
|
|
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
|
-
-
- HY-A0033
-
|
UK-88525
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
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Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
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- HY-N0471
-
|
Hyoscyamine
|
mAChR
|
Neurological Disease
|
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L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
|
-
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- HY-13204A
-
|
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
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- HY-A0012
-
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UK-88525 hydrobromide
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
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- HY-N0340
-
|
Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
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-
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- HY-B0461
-
|
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mAChR
|
Neurological Disease
|
|
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
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- HY-A0034
-
|
YM905 free base
|
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
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- HY-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
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- HY-A0002
-
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YM905
|
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
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- HY-B1339
-
|
Dicycloverine hydrochloride
|
mAChR
|
Neurological Disease
|
|
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
|
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- HY-101381
-
|
AF-DX 116
|
mAChR
|
Neurological Disease
Metabolic Disease
|
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Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively .
|
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- HY-B1487
-
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Tricyclamol hydrochloride; (±)-Procyclidine hydrochloride
|
iGluR
mAChR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
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- HY-B0344
-
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(-)-Scopolamine methyl bromide; Hyoscine methyl bromide
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mAChR
|
Neurological Disease
|
|
Methscopolamine bromide ((-)-Scopolamine methyl bromide; Hyoscine methyl bromide) is a peripherally acting muscarinic receptor (mAChR) antagonist that cannot cross the blood-brain barrier. Methscopolamine bromide blocks the muscarinic negative feedback regulation of acetylcholine release from striatal cholinergic terminals, thereby increasing acetylcholine release in the striatum of freely moving rats. Methscopolamine bromide does not induce motor excitation in freely moving rats, nor does it alter the duration of ethanol-induced loss of righting reflex in mice. Methscopolamine bromide fails to antagonize the arecoline-mediated reduction in the duration of ethanol-induced loss of righting reflex in mice .
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-
- HY-107646
-
|
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mAChR
|
Neurological Disease
|
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PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively . Antidyskinetic effect.
|
-
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- HY-107647
-
|
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mAChR
Histamine Receptor
|
Inflammation/Immunology
|
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(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48) .
|
-
-
- HY-B1621A
-
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DL-Cyclopentolate hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice .
|
-
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- HY-12980
-
|
GSK961081; TD-5959
|
Adrenergic Receptor
mAChR
|
Inflammation/Immunology
Endocrinology
|
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Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
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-
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- HY-B0547A
-
|
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mAChR
|
Neurological Disease
|
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Homatropine Bromide is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent .
|
-
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- HY-22437
-
|
(±)-UK-88525
|
mAChR
|
Neurological Disease
Cancer
|
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(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist .
|
-
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- HY-B1388
-
|
Homatropine methobromide
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mAChR
|
Infection
Neurological Disease
|
|
Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
|
-
-
- HY-I0230
-
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YM905 hydrochloride
|
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
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- HY-105545
-
|
(+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide
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mAChR
|
Neurological Disease
|
|
Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinity muscarinic receptor antagonist. Dexetimide can be used in studies of parkinson's disease .
|
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- HY-107649
-
|
UK-76654 fumarate
|
mAChR
|
Metabolic Disease
|
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Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome .
|
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- HY-B0394S
-
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Tropine tropate-d5; DL-Hyoscyamine-d5
|
mAChR
Autophagy
|
Neurological Disease
|
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Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect .
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- HY-B0461R
-
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mAChR
Reference Standards
|
Neurological Disease
|
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Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
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- HY-14825A
-
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SVT-40776 D-tartrate
|
mAChR
|
Inflammation/Immunology
|
|
Tarafenacin (SVT-40776) D-tartrate is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin D-tartrate does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin D-tartrate can be used in the research of overactive bladder .
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- HY-B1789A
-
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mAChR
|
Neurological Disease
|
|
Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects .
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- HY-14539A
-
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HF 1854 hydrochloride
|
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
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- HY-14539R
-
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HF 1854 (Standard)
|
Reference Standards
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
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- HY-B1547A
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-
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- HY-B0547
-
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mAChR
|
Neurological Disease
|
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Homatropine is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent .
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-
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- HY-B0461S
-
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Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
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Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
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- HY-123337
-
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UK-76654
|
mAChR
|
Metabolic Disease
|
|
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome .
|
-
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- HY-B1277A
-
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mAChR
Cholinesterase (ChE)
|
Cardiovascular Disease
Neurological Disease
|
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Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
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-
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- HY-177309
-
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mAChR
|
Neurological Disease
|
|
Muscarinic M3 receptor antagonist-1 (Example 4) is a muscarinic acetylcholine receptor M3 antagonist. Muscarinic M3 receptor antagonist-1 can be used to study inflammatory and obstructive airway diseases .
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-
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- HY-177310
-
-
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- HY-12426A
-
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mAChR
|
Neurological Disease
|
|
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
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-
-
- HY-107645
-
|
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mAChR
|
Neurological Disease
|
|
DAU 5884 hydrochloride is a potent muscarinic M3 receptor antagonist. DAU 5884 hydrochloride inhibits methacholine-dependent effects on cell proliferation and muscle contractility .
|
-
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- HY-13204B
-
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KL 373 lactate
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders .
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-
-
- HY-U00139
-
-
-
- HY-101743
-
-
-
- HY-P5175
-
|
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mAChR
|
Neurological Disease
|
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
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-
-
- HY-12426
-
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|
mAChR
|
Neurological Disease
|
|
mAChR-IN-1 is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM .
|
-
-
- HY-B1621
-
|
DL-Cyclopentolate
|
mAChR
|
Neurological Disease
|
|
Cyclopentolate (DL-Cyclopentolate) is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate is an anti-muscarinic agent commonly used in the ophthalmologic practice .
|
-
-
- HY-U00302
-
|
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mAChR
|
Inflammation/Immunology
|
|
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .
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- HY-P1376
-
|
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mAChR
Adrenergic Receptor
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Endocrinology
|
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G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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-
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- HY-13204R
-
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KL 373 hydrochloride (Standard)
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Reference Standards
mAChR
|
Neurological Disease
|
|
Biperiden (hydrochloride) (Standard) is the analytical standard of Biperiden (hydrochloride). This product is intended for research and analytical applications. Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-B1339A
-
|
Dicycloverine
|
mAChR
|
Neurological Disease
|
|
Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
|
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- HY-B1487A
-
|
Tricyclamol; (±)-Procyclidine
|
mAChR
iGluR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
|
-
- HY-N0471C
-
|
Daturine sulfate hydrate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate hydrate, a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate hydrate is a levo-isomer to Atropine (HY-B1205) .
|
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- HY-148533
-
|
|
mAChR
Adrenergic Receptor
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Neurological Disease
|
|
β2AR agonist /M-receptor antagonist-1 is a potent dual muscarinic antagonist/beta 2 agonist (MABA). β2AR agonist /M-receptor antagonist-1 potently relaxes either Carbachol?(HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol?(HY-B1208), or Histamine(HY-B1204)-induced contraction (β2) .
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- HY-13204AR
-
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KL 373 (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-A0012R
-
|
UK-88525 hydrobromide (Standard)
|
Reference Standards
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
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-
- HY-120792
-
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mAChR
|
Others
|
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DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
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- HY-109196
-
-
- HY-134971
-
|
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mAChR
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Neurological Disease
|
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AE9C90CB, muscarinic receptor antagonist, has greater affinity for M3 muscarinic receptors with pKi of 9.90 and was 20-fold more selective for M3 than for M2 muscarinic receptors .
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- HY-134081
-
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mAChR
|
Others
|
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Desiodomethyl 4-DAMP is a muscarinic receptor antagonist .
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- HY-19652A
-
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Esoxybutynin hydrochloride
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mAChR
|
Neurological Disease
|
|
(S)-Oxybutynin (Esoxybutynin) hydrochloride is a potent muscarinic receptor antagonist .
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- HY-120418
-
|
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mAChR
|
Others
|
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L-687306 is a high affinity muscarinic M1 receptor partial agonist with activity as a partial agonist of M1 receptors in rat ganglia and as a high affinity competitive antagonist at guinea pig cardiac M2 and ileal M3 muscarinic receptors, useful for studying the receptor reserve of muscarinic receptors.
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- HY-167699
-
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mAChR
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Others
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Cyclodrine is a cholinergic receptor antagonist that exhibits biological activity by influencing both muscarinic and nicotinic receptors.
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- HY-W708197
-
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mAChR
|
Neurological Disease
|
|
Tolterodine dimer is the impurity of Tolterodine (HY-A0024). Tolterodine is a potent muscarinic receptor antagonist.
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-
- HY-115413
-
-
- HY-14825
-
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SVT-40776
|
mAChR
|
Inflammation/Immunology
|
|
Tarafenacin (SVT-40776) is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin can be used in the research of overactive bladder .
|
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- HY-22437S1
-
-
- HY-156128
-
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mAChR
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Neurological Disease
|
|
Imidafenacin Metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist Imidafenacin (HY-B0662) .
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- HY-17037S
-
-
- HY-171449
-
-
- HY-W700319
-
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|
mAChR
|
Neurological Disease
|
|
(Rac)-5-Carboxy tolterodine is an inactive metabolite of the muscarinic acetylcholine receptor antagonist Tolterodine (HY-A0024).
|
-
- HY-22437S
-
-
- HY-43421
-
|
Solifenacin N1-oxide
|
mAChR
|
Neurological Disease
|
|
Solifenacin N-oxide (Solifenacin N1-oxide) is an inactive metabolite of the muscarinic receptor antagonist Solifenacin (HY-A0034) .
|
-
- HY-135329
-
|
|
mAChR
|
Neurological Disease
|
|
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively .
|
-
- HY-B1621AR
-
|
DL-Cyclopentolate hydrochloride (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Cyclopentolate (hydrochloride) (Standard) is the analytical standard of Cyclopentolate (hydrochloride). This product is intended for research and analytical applications. Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice .
|
-
- HY-129826
-
|
|
mAChR
|
Others
|
|
J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation .
|
-
- HY-160440A
-
|
|
mAChR
|
Neurological Disease
|
|
VU6021625 is a selective antagonist muscarinic acetylcholine receptors (mAChRs), with the IC50 value of 0.44 nM, 57 nM for human M4 and rat M4, respectively .
|
-
- HY-108030
-
-
- HY-I0230S
-
|
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Solifenacin-d7 (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-14539B
-
|
HF 1854 dihydrochloride
|
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
|
-
- HY-120329
-
|
|
mAChR
|
Others
|
|
Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
|
-
- HY-15502
-
-
- HY-P1376A
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
|
-
- HY-13204AS
-
|
KL 373-d5
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-119953
-
|
|
mAChR
|
Neurological Disease
|
|
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
|
-
- HY-172559
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Solifenacin N-glucuronide is a metabolite formed by direct glucuronidation of the muscarinic receptor antagonist Solifenacin (HY-A0034). The levels of Solifenacin N-glucuronide are associated with diseases such as hepatic impairment .
|
-
- HY-171843
-
|
|
mAChR
|
Endocrinology
|
|
TD-6301 is a bladder-selective M2/4 muscarinic receptor antagonist. TD-6301 binds to and blocks M2/4 muscarinic receptors with high selectivity, especially human M2 receptors with strong affinity (Ki = 0.36 nM). TD-6301 inhibits volume-induced bladder contractions (ID50 = 0.075 mg/kg). TD-6301 can be used in the research of overactive bladder .
|
-
- HY-B1339AS
-
|
Dicycloverine-d4
|
mAChR
|
Neurological Disease
|
|
Dicyclomine-d4 is the deuterium labeled Dicyclomine . Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
|
-
- HY-B1339R
-
|
Dicycloverine hydrochloride (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Dicyclomine (hydrochloride) (Standard) is the analytical standard of Dicyclomine (hydrochloride). This product is intended for research and analytical applications. Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
|
-
- HY-A0033S1
-
|
UK-88525-d4
|
mAChR
|
Cancer
|
|
Darifenacin-d4 is the deuterium labeled Darifenacin . Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) .
|
-
- HY-B0547AR
-
|
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Homatropine (Bromide) (Standard) is the analytical standard of Homatropine (Bromide). This product is intended for research and analytical applications. Homatropine Bromide is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent .
|
-
- HY-A0002S
-
|
YM905-d5
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-B1339S
-
|
Dicycloverine-d4 hydrochloride
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
|
-
- HY-166417S
-
|
|
Isotope-Labeled Compounds
mAChR
|
Others
|
|
Tiotropium-d3 iodide is the deuterium labeled Tiotropium iodide. Tiotropium-d3 iodide is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand. Tiotropium-d3 iodide serves as a stable isotope tracer for quantitative analysis .
|
-
- HY-183932
-
|
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
NPC-14695 is a competitive and selective M3 muscarinic receptor antagonist, with a Kd value of 15 nM for guinea pig M3, 60 nM for guinea pig M2, and 25 nM for rabbit M1. NPC-14695 exhibits higher activity towards M3 receptors in bronchial smooth muscle than towards those regulating salivary secretion. NPC-14695 inhibits Carbachol (HY-B1208)-induced contraction of isolated rabbit iris smooth muscle .
|
-
- HY-B0953A
-
-
- HY-126862
-
|
|
mAChR
|
Others
|
|
AQ-RA 721 is a muscarinic receptor antagonist with differential affinity for the m4 and M2 sites, which can be used to characterize muscarinic receptor subtypes. Other muscarinic receptor antagonists have differential affinity for the M1 (rat cerebral cortex), M2 (rat heart), M3 (rat submandibular gland), m4 (receptor expressed in Chinese hamster ovary cells transfected with CHO), and guinea pig uterine smooth muscle at the muscarinic binding site .
|
-
- HY-186083
-
|
|
mAChR
|
Cardiovascular Disease
|
|
Propylbenzilylcholine mustard (PrBCM) is an irreversible, covalently binding selective antagonist targeting rat cardiac muscarinic receptors, with a preference for muscarinic receptor subtypes that show low affinity for agonists. Propylbenzilylcholine mustard inactivates such receptors in a dose- and time-dependent manner in vitro, and its receptor selectivity remains stable across different ionic strengths and in GTP-containing buffer systems. Propylbenzilylcholine mustard can be applied to basic pharmacological studies on the structure and function of muscarinic receptors, especially focusing on the heterogeneity of cardiac muscarinic receptors and related cardiovascular pharmacological research .
|
-
- HY-180358
-
|
|
mAChR
Cholinesterase (ChE)
|
Inflammation/Immunology
|
|
Gallamine is an allosteric, selective muscarinic M2 acetylcholine receptor antagonist (EC50: 130 nM for [ 3H]NMS dissociation from porcine muscarinic M2 receptors). Gallamine is also an acetylcholinesterase inhibitor (IC50s : 1070 μM, 1480 μM, 235 μM for EeAChE, hAChE, hBChE, respectively (in the absence of MeCN)). Gallamine increases free norepinephrine levels. Gallamine can be used as a muscle relaxant .
|
-
- HY-116294
-
|
|
mAChR
|
Cardiovascular Disease
|
|
Methoctramine is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine can inhibit Muscarine (HY-121404)-induced bradycardia in vivo. Methoctramine can be used in the study of cardiovascular diseases .
|
-
- HY-W746075A
-
|
|
mAChR
|
Neurological Disease
|
|
(±)-Darifenacin N-Oxide is the impurity of Darifenacin (HY-A0033). Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9 .
|
-
- HY-N0471A
-
|
Daturine sulfate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-17465
-
|
Glycopyrronium bromide; Glycopyrrolate bromide
|
mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
|
-
- HY-107647R
-
|
|
Reference Standards
mAChR
Histamine Receptor
|
Inflammation/Immunology
|
|
(S)-(+)-Dimethindene maleate (Standard) is the analytical standard of (S)-(+)-Dimethindene (maleate) (HY-107647). This product is intended for research and analytical applications. (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48) .
|
-
- HY-A0034R
-
|
YM905 free base (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin (Standard) is the analytical standard of Solifenacin. This product is intended for research and analytical applications. Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-B1277
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Trihexyphenidyl hydrochloride is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
|
-
- HY-W011040
-
-
- HY-A0002R
-
|
YM905 (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin (Succinate) (Standard) is the analytical standard of Solifenacin (Succinate). This product is intended for research and analytical applications. Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
- HY-119918
-
|
|
mAChR
|
Neurological Disease
|
|
Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder .
|
-
- HY-122510
-
|
Atropine oxidation
|
Parasite
|
Neurological Disease
|
|
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.
|
-
- HY-122510A
-
|
Atropine oxidation hydrochloride
|
mAChR
|
|
|
Atropine Oxide (Atropine oxidation) hydrochloride, a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings .
|
-
- HY-N0214A
-
-
- HY-B0954A
-
|
|
mAChR
|
Endocrinology
|
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
|
-
- HY-N0214
-
-
- HY-B1487R
-
|
Tricyclamol hydrochloride (Standard); (±)-Procyclidine hydrochloride (Standard)
|
Reference Standards
iGluR
mAChR
|
Neurological Disease
|
|
Procyclidine (hydrochloride) (Standard) is the analytical standard of Procyclidine (hydrochloride). This product is intended for research and analytical applications. Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
|
-
- HY-113057R
-
|
|
Reference Standards
Endogenous Metabolite
|
Cancer
|
|
Trihexyphenidyl (hydrochloride) (Standard) is the analytical standard of Trihexyphenidyl (hydrochloride). This product is intended for research and analytical applications. Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
|
-
- HY-116294A
-
|
|
mAChR
|
Cardiovascular Disease
|
|
Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine (HY-121404)-induced bradycardia in vivo. Methoctramine tetrahydrochloride can be used in the study of cardiovascular diseases .
|
-
- HY-W748582
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
mAChR
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide-d8 is the deuterium labeled Clozapine N-oxide (HY-17366). Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
|
-
- HY-17366R
-
|
|
Reference Standards
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide (Standard) is the analytical standard of Clozapine N-oxide. This product is intended for research and analytical applications. Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide cannot cross the blood-brain barrier[1][2][3][4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].
|
-
- HY-17366AR
-
|
|
Reference Standards
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide (dihydrochloride) (Standard) is the analytical standard of Clozapine N-oxide (dihydrochloride). This product is intended for research and analytical applications. Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier[1][2][3][4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].
|
-
- HY-14539S3
-
|
HF 1854-d3
|
Isotope-Labeled Compounds
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
mAChR
|
Neurological Disease
Cancer
|
|
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
|
-
- HY-157956
-
|
|
mAChR
|
Neurological Disease
|
|
LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine .
|
-
- HY-B1487S1
-
|
Tricyclamol-d5; (±)-Procyclidine-d5
|
Isotope-Labeled Compounds
iGluR
mAChR
|
Neurological Disease
|
|
Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
|
-
- HY-167633
-
|
|
mGluR
Histamine Receptor
|
Neurological Disease
|
|
Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine hydrochloride is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki= 84 nM, M1 receptor) and low (Ki= 1.65 μM, M2 receptor) affinity sites [1]. Oxomemazine hydrochloride an antihistamine and anticholinergic agent used for the study of cough treatment .
|
-
- HY-A0030
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-176710A
-
|
|
Drug Isomer
|
Others
|
|
(R)-PAD-PF2 is an isomer of PAD-PF2 (HY-176710). PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM).
|
-
- HY-135329S
-
|
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
(1R,3S-)Solifenacin-d5 hydrochloride is the deuterium labeled Solifenacin hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively .
|
-
- HY-70053
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
- HY-B1277AS
-
|
|
Isotope-Labeled Compounds
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Trihexyphenidyl-d5 is deuterium labeled Trihexyphenidyl (HY-B1277A). Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
|
-
- HY-B1277S
-
|
|
Isotope-Labeled Compounds
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Trihexyphenidyl-d5 hydrochloride is deuterium labeled Trihexyphenidyl hydrochloride (HY-B1277). Trihexyphenidyl hydrochloride is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
|
-
- HY-N0471S
-
|
Daturine-d3
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-B0321S
-
|
Ro 1-7683-d3
|
mAChR
|
Neurological Disease
|
|
Tropicamide-d3 is the deuterium labeled Tropicamide . Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
|
-
- HY-12980R
-
|
GSK961081 (Standard); TD-5959 (Standard)
|
Adrenergic Receptor
mAChR
Reference Standards
|
Inflammation/Immunology
Endocrinology
|
|
Batefenterol (Standard) is the analytical standard of Batefenterol. This product is intended for research and analytical applications. Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
|
-
- HY-B0321
-
|
Ro 1-7683
|
mAChR
|
Neurological Disease
|
|
Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. When used as an eye drop, Tropicamide causes short-term mydriasis (pupil dilation) and cycloplegia. Tropicamide can be used in the research of neurological diseases, such as epilepsy .
|
-
- HY-107649R
-
|
UK-76654 fumarate (Standard)
|
Reference Standards
mAChR
|
Metabolic Disease
|
|
Zamifenacin fumarate (Standard) is the analytical standard of Zamifenacin (fumarate) (HY-107649). This product is intended for research and analytical applications. Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome .
|
-
- HY-14828
-
|
SMP-986
|
mAChR
|
Metabolic Disease
|
|
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB) .
|
-
- HY-163702
-
|
|
Adrenergic Receptor
mAChR
|
Inflammation/Immunology
|
|
CHF-6550 is an antagonist for muscarinic M3 receptor and an agonist for β2 adrenoceptor (MABA), with pKi of 9.3 and 10.6, respectively. CHF-6550 exhibits good hepatocyte clearance in rat models and good pharmacokinetic characteristics in guinea pigs .
|
-
- HY-122203A
-
PCS1055
2 Publications Verification
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-B1332
-
|
Sch 1000 bromide hydrate
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
- HY-B0241
-
|
Sch 1000
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
- HY-148524
-
|
|
mAChR
Adrenergic Receptor
|
Cardiovascular Disease
|
|
β2AR/M-receptor agonist-1 (example 131) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-1 shows potency to β2 adrenoceptor with an EC50 value of 9.2 nM. β2AR/M-receptor agonist-1 also has potency to muscarinic receptor with a Ki value of 30.2 nM. β2AR/M-receptor agonist-1 shows MABA potency with an EC50 value of 4.0 nM .
|
-
- HY-B0321R
-
|
Ro 1-7683 (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Tropicamide (Standard) is the analytical standard of Tropicamide. This product is intended for research and analytical applications. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
|
-
- HY-101368A
-
|
|
Bradykinin Receptor
mAChR
|
Neurological Disease
|
|
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM) .
|
-
- HY-B1277R
-
|
|
Reference Standards
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Trihexyphenidyl hydrochloride (Standard) is the analytical standard of Trihexyphenidyl hydrochloride (HY-B1277). This product is intended for research and analytical applications. Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
|
-
- HY-100979
-
|
HDMPPA
|
mAChR
|
Others
|
|
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
|
-
- HY-70053A
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .
|
-
- HY-127151
-
|
Levophencynonate hydrochloride
|
Endogenous Metabolite
|
Neurological Disease
|
|
Levophencynonate is a muscarinic receptor antagonist with anticholinergic activity. The biological activity of levophencynonate makes it a key target for the determination of its concentration in human plasma in medical research. Levophencynonate was analyzed by high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) and showed good specificity and linearity .
|
-
- HY-N0471R
-
|
Hyoscyamine (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (Standard) is the analytical standard of L-Hyoscyamine. This product is intended for research and analytical applications. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-W654210
-
|
Glycopyrronium-d3 bromide
|
Isotope-Labeled Compounds
mAChR
|
Cancer
|
|
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
|
-
- HY-135543
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Levophencynonate is a muscarinic receptor antagonist with anticholinergic activity. The biological activity of levophencynonate makes it a key target for the determination of its concentration in human plasma in medical research. Levophencynonate was analyzed by high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) and showed good specificity and linearity .
|
-
- HY-136587
-
|
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs .
|
-
- HY-B0267C
-
|
Aroxybutynin
|
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
|
-
- HY-149504
-
|
|
Drug Metabolite
mAChR
|
Neurological Disease
|
|
3-Hydroxy darifenacin is a metabolite of Darifenacin (HY-A0033). 3-Hydroxy darifenacin is an antagonist of M1-5 muscarinic receptors with Kis values of 17.78, 79.43, 2.24, 36.31 and 6.17 nM, respectively in CHO cells .
|
-
- HY-17037
-
|
LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-17465R
-
|
Glycopyrronium bromide (Standard); Glycopyrrolate bromide (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
Cancer
|
|
Glycopyrrolate (Standard) is the analytical standard of Glycopyrrolate. This product is intended for research and analytical applications. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
|
-
- HY-B0241S
-
|
Sch 1000-d3
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
- HY-B0241S1
-
|
Sch 1000-d7 bromide
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
- HY-17585
-
|
|
mAChR
GPR109A
|
Others
Inflammation/Immunology
|
|
Mepenzolate bromide is an orally administered muscarinic receptor antagonist with Kis of 0.68 and 2.6 nM for hM2R and hM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome .Mepenzolate bromide is a GPR109A inhibitor .
|
-
- HY-107652
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-112076A
-
|
Methylatropine nitrate
|
mAChR
|
Neurological Disease
|
|
Atropine methyl bromide (Methylatropine nitrate), an antagonist of muscarinic acetylcholine receptors (mAChR), is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
|
-
- HY-159686
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Aclidinium is a long-acting muscarinic antagonist and long-acting β2-adrenoceptor (β2-AR) agonist with bronchodilator activity. Aclidinium can reduce hyperinflation of the lungs and increase lung function and exercise endurance time. Aclidinium is used in research on chronic obstructive pulmonary disease (COPD) .
|
-
- HY-17037A
-
|
LS 519 free base; Pirenzepin; Gastrozepin
|
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-157931
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
|
-
- HY-A0030S
-
|
|
mAChR
|
Metabolic Disease
|
|
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-70053S
-
|
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
Metabolic Disease
|
|
(Rac)-Fesoterodine-d14 fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKivalues of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
- HY-112076
-
|
Methylatropine bromide
|
mAChR
|
Neurological Disease
|
|
Atropine methyl bromide (Methylatropine bromide), an antagonist of muscarinic acetylcholine receptors (mAChR), is a quaternary ammonium salt of atropine and an active molecule used for pupil dilation during ophthalmic examinations. Due to its high polarity, it is used to relieve pyloric spasm in infants. It is less likely than atropine to cross the central nervous system .
|
-
- HY-N0471AR
-
|
Daturine sulfate (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (sulfate) (Standard) is the analytical standard of L-Hyoscyamine (sulfate). This product is intended for research and analytical applications. L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-N0214R
-
-
- HY-124223
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-A0030R
-
|
|
Reference Standards
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-170444
-
|
|
Histamine Receptor
mAChR
|
Neurological Disease
|
|
ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models .
|
-
- HY-W720879
-
|
|
Isotope-Labeled Compounds
mAChR
|
Metabolic Disease
|
|
Fesoterodine-d3 is the deuterium labeled Fesoterodine (HY-70053). Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
- HY-B1205
-
-
- HY-N0471S1
-
|
Hyoscyamine-d3
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine-d3-1 (Hyoscyamine-d3) is the deuterium labeled L-Hyoscyamine (HY-N0471). L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-17037R
-
|
LS 519 (Standard); Pirenzepin dihydrochloride (Standard); Gastrozepin dihydrochloride (Standard)
|
Reference Standards
mAChR
|
Metabolic Disease
Cancer
|
|
Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-A0082
-
|
Difenidol hydrochloride
|
mAChR
Sodium Channel
|
Neurological Disease
|
|
Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
|
-
- HY-107656
-
|
|
mAChR
|
Neurological Disease
|
|
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .
|
-
- HY-16489A
-
|
|
mAChR
Calcium Channel
|
Neurological Disease
|
|
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence .
|
-
- HY-17037AR
-
|
LS 519 free base (Standard); Pirenzepin (Standard); Gastrozepin (Standard)
|
mAChR
Reference Standards
|
Metabolic Disease
Cancer
|
|
Pirenzepine (Standard) is the analytical standard of Pirenzepine. This product is intended for research and analytical applications. Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-76569B
-
|
PNU-200577 formic
|
mAChR
|
Neurological Disease
|
|
5-Hydroxymethyl tolterodine (formate) (PNU-200577 (formic)) is an active metabolite of the muscarinic acetylcholine receptor antagonists Tolterodine (HY-A0024) and Fesoterodine (HY-70053). 5-Hydroxymethyl tolterodine (formate) is formed from tolterodine by the cytochrome P450 (CYP) isoform CYP2D6 and from fesoterodine by plasma esterases.
|
-
- HY-A0270
-
|
|
mAChR
Sodium Channel
|
Neurological Disease
|
|
Diphenidol is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea .
|
-
- HY-136587R
-
|
|
Reference Standards
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
|
Oxomemazine (Standard) is the analytical standard of Oxomemazine (HY-136587). This product is intended for research and analytical applications. Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs .
|
-
- HY-122203
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-B1332R
-
|
Sch 1000 bromide hydrate (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium (bromide hydrate) (Standard) is the analytical standard of Ipratropium (bromide hydrate). This product is intended for research and analytical applications. Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
- HY-76569
-
|
PNU-200577; 5-Hydroxymethyl Tolterodine
|
mAChR
|
Neurological Disease
Cancer
|
|
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-B0394
-
|
Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
|
mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1205B
-
|
Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide
|
mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1205A
-
|
Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
|
mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-P5846
-
|
MT3
|
mAChR
Adrenergic Receptor
|
Neurological Disease
|
|
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
|
-
- HY-B0298A
-
|
HS-592 fumarate; Meclastine fumarate
|
Histamine Receptor
Apoptosis
mAChR
Pyroptosis
Keap1-Nrf2
p62
Autophagy
mTOR
IKK
|
Neurological Disease
Metabolic Disease
|
|
Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
|
-
- HY-B0298
-
|
HS-592; Meclastine
|
Histamine Receptor
mAChR
Autophagy
Apoptosis
Keap1-Nrf2
p62
mTOR
Pyroptosis
IKK
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
|
-
- HY-B0267CS
-
|
Aroxybutynin-d10
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
|
-
- HY-B2065
-
|
(-)-Scopolamine hydrochloride; Hyoscine hydrochloride
|
mAChR
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
- HY-17037S1
-
|
LS 519-d8 dihydrochloride; Pirenzepin-d8 dihydrochloride; Gastrozepin-d8 dihydrochloride
|
Isotope-Labeled Compounds
mAChR
|
Cancer
|
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-B1205R
-
|
Tropine tropate (Standard); DL-Hyoscyamine (Standard)
|
Reference Standards
mAChR
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Standard) is the analytical standard of Atropine. This product is intended for research and analytical applications. Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
- HY-112076R
-
|
Methylatropine bromide (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Atropine methyl bromide (Standard) is the analytical standard of Atropine methyl bromide. This product is intended for research and analytical applications. Atropine methyl bromide (Methylatropine bromide), an antagonist of muscarinic acetylcholine receptors (mAChR), is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
|
-
- HY-B0298AS
-
|
HS-592-d5 fumarate; Meclastine-d5 fumarate
|
Isotope-Labeled Compounds
Histamine Receptor
Apoptosis
mAChR
Pyroptosis
Keap1-Nrf2
p62
Autophagy
mTOR
IKK
|
Neurological Disease
Metabolic Disease
|
|
Clemastine (HS-592; Meclastine)-d5 fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
|
-
- HY-151198
-
|
|
mAChR
Adrenergic Receptor
Calcium Channel
|
Inflammation/Immunology
Endocrinology
|
|
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD) .
|
-
- HY-W076756
-
|
|
mAChR
|
Inflammation/Immunology
|
|
4-Piperidyl N-(2-biphenyl)carbamate (compound MA) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist. 4-Piperidyl N-(2-biphenyl)carbamate exhibits higher affinity for M2 and M3 mAChR than β2AR (M2 pKi = 7.33; M3 pKi = 7.51; β2AR pKi = 4.94) .
|
-
- HY-A0082R
-
|
Difenidol hydrochloride (Standard)
|
Reference Standards
mAChR
Sodium Channel
|
Neurological Disease
|
|
Diphenidol (hydrochloride) (Standard) is the analytical standard of Diphenidol (hydrochloride). This product is intended for research and analytical applications. Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .
|
-
- HY-B0267B
-
|
Aroxybutynin hydrochloride
|
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-165527
-
|
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
S18327 is a multi-target antipsychotic agent. S18327 exerts its efficacy by acting on multiple neurotransmitter systems in the brain, and it has antagonistic effects on dopamine receptors (particularly the D2 receptor) and 5-hydroxytryptamine 2A receptors (5-HT2A receptor). S18327 can counteract excessive dopamine activity and hypo-function of glutamate. S18327 exhibits a multi-parameter pharmacological profile that is highly similar to that of Clozapine (HY-14539). S18327 can produce the same discriminative stimulus as Clozapine, improve cognitive filtering deficits associated with schizophrenia, and display anxiolytic properties. S18327 has relatively weak affinity for histaminergic receptors and muscarinic receptors, which avoids the side effects of Clozapine .
|
-
- HY-76569R
-
|
PNU-200577 (Standard); 5-Hydroxymethyl Tolterodine (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-W010892
-
|
Hyoscine hydrobromide trihydrate
|
mAChR
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine (Hyoscine) hydrobromide trihydrate is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide trihydrate competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide trihydrate can induce cognitive and memory deficits in animals. Scopolamine hydrobromide trihydrate can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
- HY-134004
-
|
Carbetapentane
|
Sigma Receptor
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
|
-
- HY-B0394R
-
|
Tropine tropate sulfate monohydrate (Standard); DL-Hyoscyamine sulfate monohydrate (Standard)
|
Reference Standards
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1205AR
-
|
Tropine tropate sulfate (Standard); DL-Hyoscyamine sulfate (Standard); Sulfatropinol (Standard)
|
Reference Standards
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-A0082S
-
|
Difenidol hydrochloride-d10
|
Isotope-Labeled Compounds
Sodium Channel
mAChR
|
Neurological Disease
|
|
Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
|
-
- HY-17037AS
-
|
LS 519 free base-d11; Pirenzepin-d11; Gastrozepin-d11
|
Isotope-Labeled Compounds
mAChR
|
Cancer
|
|
Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-76569S1
-
|
PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14
|
mAChR
Isotope-Labeled Compounds
|
Neurological Disease
|
|
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-B0298AR
-
|
HS-592 fumarate (Standard); Meclastine fumarate (Standard)
|
Reference Standards
Histamine Receptor
Apoptosis
mAChR
Pyroptosis
Keap1-Nrf2
p62
Autophagy
mTOR
IKK
|
Neurological Disease
Metabolic Disease
|
|
Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
|
-
- HY-148525
-
|
β2AR/M-receptor agonist-2
|
mAChR
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
β2AR/M-receptor agonist-2 (compound 15) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-2 shows potency to β2 adrenoceptor with an EC50 value of 3.7 nM. β2AR/M-receptor agonist-2 also has potency to human cloned M3 receptor with a Ki value of 0.73 nM. β2AR/M-receptor agonist-2 is a potent bronchodilator, it can be used for the research of chronic obstructive pulmonary disease (COPD) .
|
-
- HY-W010892S
-
|
Hyoscine-d3 hydrobromide
|
Isotope-Labeled Compounds
mAChR
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine-d3 hydrobromide is the deuterium labeled Scopolamine hydrobromide (HY-B2065). Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
- HY-114743
-
|
|
mAChR
Histamine Receptor
CRAC Channel
|
Others
|
|
GS 283 is a compound with calcium antagonist and weak histamine and muscarinic receptor blocking activity, with activity in modulating contraction of guinea pig and rat tracheal smooth muscle. GS 283 inhibits contractions induced by carbachol, histamine (guinea pig only), and high H + in guinea pig and rat tracheal smooth muscle, inhibits Ca 2+-induced contractions in guinea pig tracheal smooth muscle, and at high concentrations completely abolishes contractions induced by carbachol in Ca 2+-free medium.
|
-
- HY-182599
-
|
|
Calcium Channel
mAChR
|
Neurological Disease
|
|
RCC-36 hydrochloride is an L-type calcium channel inhibitor and competitive muscarinic receptor antagonist. RCC-36 hydrochloride inhibits L-type calcium currents in voltage- and concentration-dependent fashion with no effect on cardiac K + currents. RCC-36 hydrochloride suppresses maximum acetylcholine-induced contractile responses, inhibits detrusor muscle contractions induced by potassium chloride, calcium chloride, and electric field stimulation, including atropine-resistant contractions. RCC-36 hydrochloride can be used for the research of urinary frequency, urinary incontinence, and bladder overactivity .
|
-
- HY-14541A
-
|
LY170053 hydrochloride
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine hydrochloride is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine hydrochloride is an atypical antipsychotic .
|
-
- HY-76569S
-
|
PNU-200577-d5; 5-Hydroxymethyl Tolterodine-d5
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
Cancer
|
|
Desfesoterodine-d5 (PNU-200577-d5) is the deuterium labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-B1055
-
|
Carbetapentane citrate
|
Sigma Receptor
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Pentoxyverine (Carbetapentane) citrate is an orally active and blood-brain barrier permeability sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
|
-
- HY-134004R
-
|
Carbetapentane (Standard)
|
Reference Standards
Sigma Receptor
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
|
-
- HY-14541
-
|
LY170053
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-B0267BS
-
|
|
mAChR
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W010892R
-
|
Hyoscine hydrobromide trihydrate (Standard)
|
mAChR
Reference Standards
5-HT Receptor
|
Neurological Disease
|
|
Scopolamine hydrobromide trihydrate (Standard) is the analytical standard of Scopolamine hydrobromide trihydrate (HY-W010892). This product is intended for research and analytical applications. Scopolamine (Hyoscine) hydrobromide is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide can induce cognitive and memory deficits in animals. Scopolamine hydrobromide can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
- HY-B1101
-
|
Pimetixene
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-B1055R
-
|
Carbetapentane citrate (Standard)
|
Reference Standards
Sigma Receptor
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance [4].
|
-
- HY-B1101A
-
|
Pimetixene maleate
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-176710
-
|
|
Protein Arginine Deiminase
Opioid Receptor
mAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca 2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .
|
-
- HY-103109
-
|
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-10564
-
|
MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-B2169
-
|
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-14541R
-
|
LY170053 (Standard)
|
Reference Standards
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-14541S2
-
|
LY170053-d8
|
Isotope-Labeled Compounds
Apoptosis
Dopamine Receptor
Autophagy
mAChR
Mitophagy
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-10564R
-
|
MCI-9042 (Standard)
|
Reference Standards
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate (hydrochloride) (Standard) is the analytical standard of Sarpogrelate (hydrochloride). This product is intended for research and analytical applications. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-B2169R
-
|
|
5-HT Receptor
Reference Standards
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
|
-
- HY-B2169S2
-
|
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-10564S
-
|
MCI-9042-d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-14541S
-
|
LY170053-d3
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine-d3 (LY170053-d3) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-N0340R
-
|
Hyoscine butylbromide (Standard); (-)-Scopolamine butylbromide (Standard); Butylscopolamine bromide (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Scopolamine butylbromide (Standard) is the analytical standard of Scopolamine butylbromide (HY-N0340). This product is intended for research and analytical applications. Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
|
-
- HY-B1101AR
-
|
Pimetixene maleate (Standard)
|
Reference Standards
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Pimethixene maleate (Standard) is the analytical standard of Pimethixene maleate. This product is intended for research and analytical applications. Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-N1482
-
|
|
Environmental Pollutants
Parasite
|
Inflammation/Immunology
|
|
Methyl palmitate is a naturally occurring fatty acid ester. Methyl palmitate is a potent inhibitor of ΙκB phosphorylation. Methyl palmitate modulates macrophage activity and down-regulates pro-inflammatory mediators such as TNF-α and nitric oxide (NO). Methyl palmitate possesses anti-inflammatory and antifibrotic effects. Methyl palmitate can inhibit LPS (HY-D1056)-induced Kupffer cells and rat peritoneal macrophages. Methyl palmitate is able to inhibit the phagocytic function of RAW cells. Methyl palmitate is antagonistic to muscarinic receptors. Methyl palmitate exerts cardioprotective effects against ischemia/reperfusion injury in vivo. Methyl palmitate is highly toxic against adult T. cinnabarinus .
|
-
- HY-10564S1
-
|
MCI-9042-d4
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
| Cat. No. |
상품명 |
Target |
Research Area |
-
- HY-P5175
-
|
|
mAChR
|
Neurological Disease
|
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
|
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-P1376A
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
|
-
- HY-P5846
-
|
MT3
|
mAChR
Adrenergic Receptor
|
Neurological Disease
|
|
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
|
| Cat. No. |
상품명 |
Category |
Target |
Chemical Structure |
-
- HY-B1205
-
-
-
- HY-N0471
-
-
-
- HY-W010892
-
|
Hyoscine hydrobromide trihydrate
|
Alkaloids
Other Alkaloids
Datura metel L.
Solanaceae
Plants
Source Classification
|
mAChR
5-HT Receptor
|
|
Scopolamine (Hyoscine) hydrobromide trihydrate is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide trihydrate competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide trihydrate can induce cognitive and memory deficits in animals. Scopolamine hydrobromide trihydrate can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
-
- HY-N0340
-
|
Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
|
Alkaloids
Structural Classification
Other Alkaloids
Datura metel L.
Solanaceae
Plants
Source Classification
|
mAChR
|
|
Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
|
-
-
- HY-N1482
-
-
-
- HY-N0214
-
-
-
- HY-B2065
-
|
(-)-Scopolamine hydrochloride; Hyoscine hydrochloride
|
Alkaloids
Other Alkaloids
Atropa belladonna Linn.
Solanaceae
Plants
Source Classification
|
mAChR
5-HT Receptor
|
|
Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
-
- HY-N0471A
-
-
-
- HY-B1205R
-
|
Tropine tropate (Standard); DL-Hyoscyamine (Standard)
|
Atropa belladonna Linn.
Solanaceae
Plants
Endogenous metabolite
Source Classification
|
Reference Standards
mAChR
Endogenous Metabolite
|
|
Atropine (Standard) is the analytical standard of Atropine. This product is intended for research and analytical applications. Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
-
- HY-B1205AR
-
|
Tropine tropate sulfate (Standard); DL-Hyoscyamine sulfate (Standard); Sulfatropinol (Standard)
|
Alkaloids
Structural Classification
Other Alkaloids
Atropa belladonna Linn.
Solanaceae
Plants
Source Classification
|
Reference Standards
mAChR
|
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
-
- HY-N0214A
-
-
-
- HY-W010892R
-
|
Hyoscine hydrobromide trihydrate (Standard)
|
Alkaloids
Structural Classification
Other Alkaloids
Datura metel L.
Solanaceae
Plants
Source Classification
|
mAChR
Reference Standards
5-HT Receptor
|
|
Scopolamine hydrobromide trihydrate (Standard) is the analytical standard of Scopolamine hydrobromide trihydrate (HY-W010892). This product is intended for research and analytical applications. Scopolamine (Hyoscine) hydrobromide is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide can induce cognitive and memory deficits in animals. Scopolamine hydrobromide can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
-
- HY-N0471R
-
-
-
- HY-N0471AR
-
-
-
- HY-N0214R
-
-
-
- HY-B0394R
-
|
Tropine tropate sulfate monohydrate (Standard); DL-Hyoscyamine sulfate monohydrate (Standard)
|
Alkaloids
Structural Classification
Other Alkaloids
Atropa belladonna Linn.
Solanaceae
Plants
Source Classification
|
Reference Standards
mAChR
|
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
-
- HY-N0340R
-
|
Hyoscine butylbromide (Standard); (-)-Scopolamine butylbromide (Standard); Butylscopolamine bromide (Standard)
|
Alkaloids
Structural Classification
Other Alkaloids
Datura metel L.
Solanaceae
Plants
Source Classification
|
Reference Standards
mAChR
|
|
Scopolamine butylbromide (Standard) is the analytical standard of Scopolamine butylbromide (HY-N0340). This product is intended for research and analytical applications. Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
|
-
-
- HY-113057R
-
-
| Cat. No. |
상품명 |
Chemical Structure |
-
- HY-W654210
-
|
|
|
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
|
-
-
- HY-B0394S
-
|
|
|
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect .
|
-
-
- HY-B0461S
-
|
|
|
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
-
- HY-B0321S
-
|
|
|
Tropicamide-d3 is the deuterium labeled Tropicamide . Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
|
-
-
- HY-14541S
-
|
|
|
Olanzapine-d3 (LY170053-d3) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
-
- HY-A0030S
-
|
|
|
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
-
- HY-B0241S
-
|
|
|
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
-
- HY-W010892S
-
|
|
|
Scopolamine-d3 hydrobromide is the deuterium labeled Scopolamine hydrobromide (HY-B2065). Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .
|
-
-
- HY-B2169S2
-
|
|
|
Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
|
-
-
- HY-22437S1
-
|
|
|
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
|
-
-
- HY-17037S
-
|
|
|
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
|
-
-
- HY-22437S
-
|
|
|
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist .
|
-
-
- HY-I0230S
-
|
|
|
Solifenacin-d7 (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-13204AS
-
|
|
|
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
-
- HY-B1339AS
-
|
|
|
Dicyclomine-d4 is the deuterium labeled Dicyclomine . Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
|
-
-
- HY-A0033S1
-
|
|
|
Darifenacin-d4 is the deuterium labeled Darifenacin . Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) .
|
-
-
- HY-A0002S
-
|
|
|
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-B1339S
-
|
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Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-W748582
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Clozapine N-oxide-d8 is the deuterium labeled Clozapine N-oxide (HY-17366). Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
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- HY-14539S3
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Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
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- HY-B1487S1
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Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
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- HY-135329S
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(1R,3S-)Solifenacin-d5 hydrochloride is the deuterium labeled Solifenacin hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively .
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- HY-B1277AS
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Trihexyphenidyl-d5 is deuterium labeled Trihexyphenidyl (HY-B1277A). Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
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- HY-B1277S
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Trihexyphenidyl-d5 hydrochloride is deuterium labeled Trihexyphenidyl hydrochloride (HY-B1277). Trihexyphenidyl hydrochloride is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
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- HY-N0471S
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L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
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- HY-B0241S1
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Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
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- HY-70053S
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(Rac)-Fesoterodine-d14 fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKivalues of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
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- HY-W720879
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Fesoterodine-d3 is the deuterium labeled Fesoterodine (HY-70053). Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
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- HY-B0267CS
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(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
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- HY-17037S1
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Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
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- HY-B0298AS
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1 Publications Verification
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Clemastine (HS-592; Meclastine)-d5 fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
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- HY-A0082S
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Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
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- HY-17037AS
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Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
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- HY-76569S1
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(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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- HY-B0267BS
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Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-14541S2
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Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
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- HY-10564S
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Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
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- HY-10564S1
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Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
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- HY-166417S
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Tiotropium-d3 iodide is the deuterium labeled Tiotropium iodide. Tiotropium-d3 iodide is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand. Tiotropium-d3 iodide serves as a stable isotope tracer for quantitative analysis .
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- HY-N0471S1
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L-Hyoscyamine-d3-1 (Hyoscyamine-d3) is the deuterium labeled L-Hyoscyamine (HY-N0471). L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
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- HY-76569S
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Desfesoterodine-d5 (PNU-200577-d5) is the deuterium labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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| Cat. No. |
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Classification |
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- HY-120329
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Alkynes
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Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
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