Search Result

Results for "

muscarinic cholinergic receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	mAChR (35) 5-HT Receptor (5) Adrenergic Receptor (6) Apoptosis (4) Cholinesterase (ChE) (6) Cytochrome P450 (1) Dopamine Transporter (4) Histamine Receptor (4) Isotope-Labeled Compounds (5) nAChR (1) NO Synthase (1) Potassium Channel (5) Prolyl Endopeptidase (PREP) (1) Reference Standards (4) Serotonin Transporter (4) Sodium Channel (4) Trk Receptor (4)
By Research Areas:	Cardiovascular Disease (4) Endocrinology (4) Infection (1) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (37)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Antibodies

Targets Recommended: mAChR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0527A

Amitriptyline hydrochloride Maximum Cited Publications 8 Publications Verification	Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity .

HY-B0527

Amitriptyline Maximum Cited Publications 8 Publications Verification	Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis	Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity .

HY-B0461

Trospium chloride	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 .

HY-B1277

Trihexyphenidyl hydrochloride 3 Publications Verification	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-B1339

Dicyclomine hydrochloride 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 (K_i=5.1 nM) and M2 receptor subtype (K_i=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-B0344

Methscopolamine bromide 1 Publications Verification (-)-Scopolamine methyl bromide; Hyoscine methyl bromide	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 .

HY-159829

Direclidine NBI-1117568; HTL-0016878	mAChR	Neurological Disease
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 .

HY-B0461R

Trospium chloride (Standard)	mAChR Reference Standards	Neurological Disease
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 .

HY-173396

VU0467319 VU319	mAChR	Neurological Disease
VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC₅₀: 492 nM). VU0467319 is selective (EC₅₀ > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research .

HY-B0527AR

Amitriptyline hydrochloride (Standard) 4 Publications Verification	Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-B0461S

Trospium-d8 chloride	Isotope-Labeled Compounds mAChR	Neurological Disease
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-B0527AS

Amitriptyline-d6 hydrochloride	Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-12426A

mAChR-IN-1 hydrochloride	mAChR	Neurological Disease
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC₅₀ of 17 nM .

HY-119918

Cycrimine	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-B1277A

Trihexyphenidyl	mAChR Cholinesterase (ChE)	Cardiovascular Disease Neurological Disease
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-U00139

Cyclodrine hydrochloride	mAChR nAChR	Neurological Disease
Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.

HY-12426

mAChR-IN-1	mAChR	Neurological Disease
mAChR-IN-1 is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC₅₀ of 17 nM .

HY-120408

(±)-Scopolamine Atroscine	Adrenergic Receptor	Neurological Disease
(±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits α-adrenergic receptor activity. (±)-Scopolamine has K_i values of 33 μM and 7.25 nM for α₁-adrenerg receptor and muscarinic cholinergic receptor, respectively .

HY-B1339A

Dicyclomine 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 (K_i=5.1 nM) and M2 receptor subtype (K_i=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-100979

W-84 dibromide 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-167699

Cyclodrine	mAChR	Others
Cyclodrine is a cholinergic receptor antagonist that exhibits biological activity by influencing both muscarinic and nicotinic receptors.

HY-U00085

Itameline RU 47213	Cholinesterase (ChE)	Neurological Disease
Itameline (RU 47213) is a prodrug with oral and long-lasting *cholinergic* activity. Itameline is a novel tetrahydropyridine-oxime that is cleaved in vivo to form an active metabolite, RU 35963. RU 35963 is a muscarinic receptor agonist that is nonselective with respect to receptor subtypes. Itameline possesses the capacity to reduce memory deficits induced by an impairment of cholinergic transmission in the rat .

HY-117223

GEA 857	Potassium Channel	Neurological Disease
GEA 857 is a structural analog of the Serotonin (HY-B1473A) uptake blocker Alaproclate (HY-164011). GEA 857 enhances responses induced by muscarinic receptor agonists by inhibiting certain calcium-dependent potassium channels on membranes, a blockade that can enhance or prolong the muscarinic cholinergic effects. GEA 857 can be used in research on neurodegenerative diseases .

HY-B1339AS

Dicyclomine-d4 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

Dicyclomine hydrochloride (Standard) 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-B1339S

Dicyclomine-d4 hydrochloride 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-157956

LASSBio-873	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-P1376A

G-Protein antagonist peptide TFA 1 Publications Verification	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 G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .

HY-107650

Milameline hydrochloride CI 979 hydrochloride; RU 35926 hydrochloride	mAChR	Neurological Disease
Milameline (CI 979; RU35926) hydrochloride is a nonselective, partical and orally active **muscarinic receptor** agonist that improves cognition. Milameline hydrochloride has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydrochloride has a higher affinity for sites [ ³H]CMD (IC₅₀ = 20 nM), than [ ³H]QNB, (IC₅₀ = 3059 nM). Milameline hydrochloride produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydrochloride can be used for the study of Alzheimer’s Disease .

HY-135460

Milameline CI-979; RU35926	mAChR	Neurological Disease
Milameline (CI-979; RU35926) is a nonselective, partical and orally active **muscarinic receptor** agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [ ³H]CMD (IC₅₀ = 20 nM), than [ ³H]QNB, (IC₅₀ = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease .

HY-B1277AS

Trihexyphenidyl-d5	Isotope-Labeled Compounds mAChR Cholinesterase (ChE)	Cardiovascular Disease 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

Trihexyphenidyl-d5 hydrochloride	Isotope-Labeled Compounds mAChR Cholinesterase (ChE)	Cardiovascular Disease 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-105793

Mazaticol	mAChR	Neurological Disease
Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with high affinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .

HY-B1277R

Trihexyphenidyl hydrochloride (Standard)	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-15116

ONO 1603	Prolyl Endopeptidase (PREP)	Neurological Disease
ONO 1603, a novel prolyl endopeptidase inhibitor investigated as a potential antidementia drug, demonstrated neuroprotective and neurotrophic effects in cerebellar granule cells similar to tetrahydroaminoacridine (THA). At a concentration of 0.03 microM, ONO 1603 promoted neuronal survival, enhanced neurite outgrowth, increased m3-muscarinic acetylcholine receptor (mAChR) mRNA levels, and stimulated mAChR-mediated signaling pathways. These findings suggest that ONO 1603 shares pharmacological similarities with THA, indicating its potential as a therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and neuronal function .

HY-117284A

Eucatropine hydrochloride	mAChR	Neurological Disease
Eucatropine hydrochloride is a potent muscarinic acetylcholine receptor (mAChR) inhibitor with an IC₅₀ value of 0.583 μM. Eucatropine hydrochloride acts as an anticholinergic agent. Eucatropine hydrochloride produces behavioral effects via central cholinergic receptive sites in cats .

HY-107650A

Milameline hydroiodide CI 979 hydroiodide; RU 35926 hydroiodide	mAChR	Neurological Disease
Milameline (CI 979; RU35926) hydroiodide is a nonselective, partical and orally active **muscarinic receptor** agonist that improves cognition. Milameline hydroiodide has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydroiodide has a higher affinity for sites [ ³H]CMD (IC₅₀ = 20 nM), than [ ³H]QNB, (IC₅₀ = 3059 nM). Milameline hydroiodide produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydroiodide can be used for the study of Alzheimer’s Disease .

HY-30647

RS-86	mAChR	Neurological Disease
RS-86 is a potent, central acting, and selective **muscarinic acetylcholine receptor** agonist. RS-86 exhibits typical cholinergic excitatory effects, such as inducing smooth muscle contraction, ganglion depolarization, central hypothermia, etc. RS-86 can be used for research on Alzheimer's disease .

HY-159829A

Direclidine citrate NBI-1117568 citrate; HTL-0016878 citrate	mAChR	Neurological Disease
Direclidine (NBI-1117568, HTL-0016878) citrate is a selective orthosteric agonist targeting the **muscarinic acetylcholine M4 receptor*, exhibiting very low affinity for M1, M2, M3, and M5 receptors. Direclidine citrate binds to the orthosteric site of the M4 receptor* in a non-covalent, competitive manner. Direclidine citrate 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 citrate can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .

HY-122272A

Paroxetine acetate BRL29060 acetate	Cytochrome P450 5-HT Receptor NO Synthase	Neurological Disease
Paroxetine (BRL29060) acetate is a selective serotonin reuptake inhibitor with blood-brain barrier permeability. Paroxetine acetate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine acetate is widely used in the research of related diseases such as depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder and hot flashes .

Cat. No.	Product Name	Target	Research Area

HY-P1376A

G-Protein antagonist peptide TFA 1 Publications Verification	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 G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-120408

(±)-Scopolamine Atroscine	Alkaloids other families Other Alkaloids Plants Source Classification	Adrenergic Receptor
(±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits α-adrenergic receptor activity. (±)-Scopolamine has K_i values of 33 μM and 7.25 nM for α₁-adrenerg receptor and muscarinic cholinergic receptor, respectively .

Cat. No.	Product Name	Chemical Structure

HY-B0461S

Trospium-d8 chloride
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-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-B1339AS

Dicyclomine-d4

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-B1339S

Dicyclomine-d4 hydrochloride

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-B1277AS

Trihexyphenidyl-d5

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

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. .

Cat. No.	Compare	Product Name	Application	Reactivity	Image

HY-P81142

	Muscarinic Acetylcholine receptor M3 Antibody (YA3525) muscarinic Acetylcholine receptor M3; cholinergic receptor, muscarinic 3; CHRM 3; CHRM3; HM 3; HM3; HM3; EGBRS; M3 muscarinic receptor; muscarinic 3; m3 muscarinic acetylcholine receptor; ACM3_HUMAN; muscarinic receptor M3; muscarinic cholinergic m3 receptor; muscarinic m3 receptor; Acetylcholine receptor(M3).	WB	Human
	Muscarinic Acetylcholine receptor M3 Antibody (YA3525) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Muscarinic Acetylcholine receptor M3.

Compare Products


Products	In-stock - + Add to Cart
Cat. No.
Host
Reactivity
Application
Dilution Ratio
Molecular Weight
Conjugation
Clonality
Immunogen
Appearance
Isotype
Gene ID
SwissProt ID
Purity
Formulation
Free Sample	Yes No
Size	* This product has been "discontinued". Optimized version of product available: / In-stock - + Add to Cart Get quote

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks