Search Result
Results for "
M1 acetylcholine receptors
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- 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 .
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-
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- HY-17360
-
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BA679 BR
|
mAChR
|
Inflammation/Immunology
|
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Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
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-
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- HY-70020B
-
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AF102B hydrochloride
|
mAChR
|
Neurological Disease
Cancer
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Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
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-
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- HY-13204A
-
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KL 373
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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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-
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- HY-32067
-
|
Quinuclidin-3-yl acetate
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
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-
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- HY-B1277
-
|
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mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
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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-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
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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-17037
-
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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-B0298
-
Clemastine
Maximum Cited Publications
11 Publications Verification
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 .
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- 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 .
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- HY-15618
-
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M1 receptor modulator
|
mAChR
Calcium Channel
|
Neurological Disease
|
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MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC50 = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD) .
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- HY-N8376
-
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(±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone
|
Amyloid-β
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
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- HY-122190
-
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mAChR
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Neurological Disease
|
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TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM .
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- HY-176710
-
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Protein Arginine Deiminase
Opioid Receptor
mAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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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 .
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- HY-19752A
-
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CID-25010775
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mAChR
|
Neurological Disease
|
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VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia .
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- HY-122743
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Iperoxo
2 Publications Verification
|
mAChR
|
Neurological Disease
|
|
Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors when labeled with tritium .
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- HY-76772
-
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SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
Cancer
|
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Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
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-
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- HY-70020
-
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AF102B
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mAChR
|
Neurological Disease
Cancer
|
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Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline can cross the blood-brain barrier (BBB) .
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- HY-32067A
-
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Quinuclidin-3-yl acetate hydrochloride
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mAChR
|
Neurological Disease
|
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Aceclidine (Quinuclidin-3-yl acetate) hydrochloride is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine hydrochloride is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine hydrochloride has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
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- HY-159829
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NBI-1117568; HTL-0016878
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mAChR
|
Neurological Disease
|
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Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
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- HY-B0460
-
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BA-679 BR monohydrate
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mAChR
|
Inflammation/Immunology
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Tiotropium bromide monohydrate (BA-679 BR monohydrate) is a long-acting anticholinergic bronchodilator. Tiotropium bromide monohydrate blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide monohydrate is applicable to research related to chronic obstructive pulmonary disease and asthma .
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- HY-17360S1
-
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BA679 BR-d6
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Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
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Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
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- HY-14562
-
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mAChR
Amyloid-β
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Neurological Disease
Inflammation/Immunology
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TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC50=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis) .
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- HY-N12302
-
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N1-Dihydrocaffeoyl, N10-caffeoyl spermidine
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mAChR
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Others
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Scotanamine D (N1-Dihydrocaffeoyl, N10-caffeoyl spermidine) is a spermidine alkaloid. It can be isolated from S. tangutica. Scotanamine D potently and selectively inhibits the activity of the M1 muscarinic acetylcholine receptor, with an IC50 of 32 nM. It can be used in studies related to Parkinson's disease .
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- HY-N7247
-
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mAChR
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Metabolic Disease
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Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
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- HY-176200
-
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AF98943
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mAChR
|
Neurological Disease
|
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VU6008055 (AF98943) is a brain-penetrant, orally active and selective muscarinic acetylcholine receptor subtype 4 (mAChR4) activator with human EC50 values of 73.4 nM. VU6008055 potentiates mAChR4 receptor activity in the presence of acetylcholine, and exhibits no activity at mAChR1, mAChR3, or mAChR5. VU6008055 can be used for the research of schizophrenia, parkinson’s disease, alzheimer’s disease .
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- HY-116586
-
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Sigma Receptor
mAChR
ERK
Amyloid-β
Tau Protein
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Neurological Disease
|
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AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease .
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- HY-N4157
-
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mAChR
5-HT Receptor
Bacterial
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Neurological Disease
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Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
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- HY-121806
-
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mAChR
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Neurological Disease
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VU0486846 is an orally active and selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) .
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- HY-123852
-
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mAChR
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Neurological Disease
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PF-06764427 is a selective M1 muscarinic acetylcholine receptor positive allosteric modulator. PF-06764427 exhibits robust M1 agonist activity. PF-06764427 can be used in the research of Alzheimer's disease and schizophrenia .
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- HY-B1277A
-
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mAChR
Cholinesterase (ChE)
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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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- HY-119918
-
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mAChR
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Neurological Disease
|
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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 .
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- HY-118356
-
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Neurokinin Receptor
mAChR
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Neurological Disease
|
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WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
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-
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- HY-65036
-
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4-Bromo-2-pyridone
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Biochemical Assay Reagents
Drug Intermediate
|
Neurological Disease
|
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4-Bromo-2-hydroxypyridine is an intermediate. 4-Bromo-2-hydroxypyridine can be used to synthesize M1 muscarinic acetylcholine receptor (M1 mAChR) positive allosteric modulators. 4-Bromo-2-hydroxypyridine can be used in the research of Alzheimer's disease and schizophrenia .
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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 .
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-
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- HY-13204B
-
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KL 373 lactate
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mAChR
|
Neurological Disease
|
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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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-
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- HY-12158
-
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mAChR
|
Neurological Disease
|
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VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .
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-
-
- HY-17360S
-
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BA679 BR-d3
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Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
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-
-
- HY-175532
-
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mAChR
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Neurological Disease
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M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
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- HY-146102
-
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mAChR
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Others
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M1 ligand 1 (compound 3b-b) is a muscarinic acetylcholine receptor M1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer .
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- HY-148961
-
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mAChR
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Neurological Disease
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HTL-9936 is a selective M1 muscarinic acetylcholine receptor (M1-mAChR) agonist. HTL-9936 is promising for research of neurodegenerative disorders (e.g., Alzheimer’s) .
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- HY-170032
-
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mAChR
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Neurological Disease
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Oxotremorine is an agonist for mAChR, that activates M1 and M3 acetylcholine receptors. Oxotremorine exhibits nicotine-like effects in drug discrimination experiments in macaques .
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- HY-19752
-
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CID-25010775 free base
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mAChR
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Neurological Disease
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VU0357017 (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 can be used for the research of Alzheimer’s disease and schizophrenia .
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-
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- HY-122510
-
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Atropine oxidation
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Parasite
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Neurological Disease
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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.
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- HY-128783
-
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mAChR
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Neurological Disease
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VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .
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- HY-122510A
-
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Atropine oxidation hydrochloride
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mAChR
|
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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 .
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- HY-B1277AS
-
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Isotope-Labeled Compounds
mAChR
Cholinesterase (ChE)
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Neurological Disease
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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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Isotope-Labeled Compounds
mAChR
Cholinesterase (ChE)
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Neurological Disease
|
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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-123778
-
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mAChR
|
Neurological Disease
|
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VU6007678 is a CNS-penetrant muscarinic acetylcholine receptor (mAChR) modulator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke .
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-
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- HY-N7247R
-
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Reference Standards
mAChR
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Metabolic Disease
|
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Thiochrome (Standard) is the analytical standard of Thiochrome. This product is intended for research and analytical applications. Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
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- HY-B1277R
-
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Reference Standards
mAChR
Cholinesterase (ChE)
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Neurological Disease
|
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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. .
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- HY-182587
-
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|
mAChR
|
Neurological Disease
|
|
VU0415248 is a selective muscarinic acetylcholine receptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1 muscarinic acetylcholine receptors, with an IC50 of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome .
|
-
- HY-13204AR
-
|
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-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-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-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-119333
-
|
|
mAChR
|
Neurological Disease
|
|
NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia .
|
-
- HY-70020BR
-
|
AF102B hydrochloride (Standard)
|
mAChR
Reference Standards
|
Neurological Disease
Cancer
|
|
Cevimeline (hydrochloride) (Standard) is the analytical standard of Cevimeline (hydrochloride). This product is intended for research and analytical applications. Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
|
-
- HY-19651A
-
|
TAK-147
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .
|
-
- HY-19651B
-
|
TAK-147 fumarate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .
|
-
- 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-17360R
-
|
BA679 BR (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Tiotropium (Bromide) (Standard) is the analytical standard of Tiotropium (Bromide). This product is intended for research and analytical applications.
Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
|
-
- 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-19651
-
|
TAK-147 free base
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .
|
-
- 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-120184
-
|
AZ13713945
|
mAChR
|
Neurological Disease
|
|
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
|
-
- 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-N4157R
-
|
|
Reference Standards
mAChR
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
|
-
- HY-123661
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
MIPS1455 is a light-activated M1 muscarinic acetylcholine receptor ligand with irreversible binding activity to the allosteric site of the receptor. MIPS1455 is a drug target under investigation for the suppression of cognitive deficits and may become a valuable molecular tool for further investigation of allosteric interactions of the receptor .
|
-
- 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-183144
-
|
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states .
|
-
- HY-76772R
-
|
SNI-2011 (Standard); AF102B hydrochloride hemihydrate (Standard)
|
mAChR
Reference Standards
|
Neurological Disease
Cancer
|
|
Cevimeline (hydrochloride hemihydrate) (Standard) is the analytical standard of Cevimeline (hydrochloride hemihydrate). This product is intended for research and analytical applications. Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
|
-
- HY-101196
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
PG 9 maleate is a compound with analgesic and anti-memory loss activity. PG 9 maleate exerts analgesic effects by enhancing central cholinergic transmission. PG 9 maleate protects against memory loss caused by scopolamine or dicyclomine within a specific dose range. The affinity profile of PG 9 maleate indicates significant selectivity among the M4/M1 receptor subtypes, which may be the mechanism for its analgesic and anti-memory loss effects. PG 9 maleate can increase the release of acetylcholine, thereby improving its biological activity .
|
-
- HY-180143
-
|
|
mAChR
Drug Derivative
|
Neurological Disease
|
|
VU6052254, a derivative of VU0467319 (HY-173396), is a selective, potent, orally active and brain-penetrant muscarinic M1 acetylcholine receptor (mAChR1) positive allosteric modulator with an EC50 of 59 nM. VU6052254 has no activity on the M2-5 receptor (EC50 > 30 μM). VU6052254 can improve memory recognition ability and reverse the cognitive impairment induced by Scopolamine (HY-N0296) with minimum effective dose both of 1 mg/kg. VU6052254 can be used for the research of neurological disease, such as Alzheimer's disease .
|
-
- HY-131196
-
|
|
mAChR
|
Neurological Disease
|
|
M3 mAChR agonist 1 is an M3-preferring M3/M5 mAChR dual positive allosteric modulators (PAM). M3 mAChR agonist 1 shows excellent subtype selectivity over other subtypes of mAChRs including M1, M2, and M4 mAChRs. M3 mAChR agonist 1 increases the contraction of isolated rat bladder strips by modulating the M3 muscarinic acetylcholine receptor, leading to enhanced signaling pathways. M3 mAChR agonist 1 can be used for the research of endocrinology .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-65036
-
|
4-Bromo-2-pyridone
|
Biochemical Assay Reagents
|
|
4-Bromo-2-hydroxypyridine is an intermediate. 4-Bromo-2-hydroxypyridine can be used to synthesize M1 muscarinic acetylcholine receptor (M1 mAChR) positive allosteric modulators. 4-Bromo-2-hydroxypyridine can be used in the research of Alzheimer's disease and schizophrenia .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N8376
-
|
(±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone
|
Flavanonols
Flavonoids
Plants
Rhus glabra L.
Source Classification
Anacardiaceae
|
Amyloid-β
mAChR
Cholinesterase (ChE)
|
|
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
|
-
-
- HY-N12302
-
-
-
- HY-N4157
-
|
|
Uncaria rhynchophylla (Miq.) Miq. ex Havil.
Structural Classification
Iridoids
Terpenoids
Rubiaceae
Plants
Source Classification
|
mAChR
5-HT Receptor
Bacterial
|
|
Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
|
-
-
- HY-N4157R
-
|
|
Uncaria rhynchophylla (Miq.) Miq. ex Havil.
Structural Classification
Iridoids
Terpenoids
Rubiaceae
Plants
Source Classification
|
Reference Standards
mAChR
5-HT Receptor
Bacterial
|
|
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17360S1
-
|
|
|
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
|
-
-
- HY-17360S
-
|
|
|
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
|
-
-
- HY-B1277AS
-
|
|
|
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
-
|
|
|
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-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-17037S1
-
|
|
|
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-17037AS
-
|
|
|
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-B0298AS
-
1 Publications Verification
|
|
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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