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Results for "

Muscarinic M4 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	mAChR (85) 5-HT Receptor (10) Adrenergic Receptor (10) Apoptosis (8) Autophagy (4) Cholinesterase (ChE) (2) Dopamine Receptor (11) Dopamine Transporter (4) Drug Metabolite (5) Endogenous Metabolite (2) Environmental Pollutants (1) Histamine Receptor (11) IKK (4) Isotope-Labeled Compounds (8) Keap1-Nrf2 (4) Ligands for E3 Ligase (1) mGluR (1) mTOR (4) p62 (4) Parasite (1) Potassium Channel (4) Pyroptosis (4) Reference Standards (17) Serotonin Transporter (4) Sigma Receptor (1) Sodium Channel (8) Trk Receptor (4)
By Research Areas:	Cancer (10) Cardiovascular Disease (8) Endocrinology (4) Inflammation/Immunology (8) Metabolic Disease (12) Neurological Disease (78)

By Targets:

mAChR (85)

5-HT Receptor (10)

Adrenergic Receptor (10)

Apoptosis (8)

Autophagy (4)

Cholinesterase (ChE) (2)

Dopamine Receptor (11)

Dopamine Transporter (4)

Drug Metabolite (5)

Endogenous Metabolite (2)

Environmental Pollutants (1)

Histamine Receptor (11)

IKK (4)

Isotope-Labeled Compounds (8)

Keap1-Nrf2 (4)

Ligands for E3 Ligase (1)

mGluR (1)

mTOR (4)

p62 (4)

Parasite (1)

Potassium Channel (4)

Pyroptosis (4)

Reference Standards (17)

Serotonin Transporter (4)

Sigma Receptor (1)

Sodium Channel (8)

Trk Receptor (4)

By Research Areas:

Cancer (10)

Cardiovascular Disease (8)

Endocrinology (4)

Inflammation/Immunology (8)

Metabolic Disease (12)

Neurological Disease (78)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: mAChR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17366

Clozapine N-oxide Maximum Cited Publications 145 Publications Verification	Drug Metabolite mAChR Dopamine Receptor	Neurological Disease
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-B1205

Atropine 20+ Cited Publications Tropine tropate; DL-Hyoscyamine	Environmental Pollutants Endogenous Metabolite mAChR	Cardiovascular Disease Neurological Disease Cancer
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-17366A

Clozapine N-oxide dihydrochloride Maximum Cited Publications 145 Publications Verification	mAChR Dopamine Receptor Drug Metabolite	Neurological Disease
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 .

HY-14539

Clozapine 10+ Cited Publications 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 K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is 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-B0298A

Clemastine fumarate 10+ Cited Publications 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-105182

Xanomeline 5+ Cited Publications LY-246708	mAChR	Neurological Disease
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .

HY-B0527A

Amitriptyline hydrochloride 5+ Cited Publications	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 5+ Cited Publications	Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
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-132812

Emraclidine CVL-231	mAChR	Neurological Disease
Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases .

HY-105182A

Xanomeline tartrate 5+ Cited Publications LY 246708 tartrate	mAChR	Neurological Disease
Xanomeline (LY 246708) is the potent agonist of muscarinic *M1/M4* receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .

HY-A0030

Fesoterodine fumarate	mAChR	Neurological Disease Metabolic Disease Cancer
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i 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-B0394

Atropine sulfate monohydrate 20+ Cited Publications 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-B0298

Clemastine 10+ Cited Publications 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-B1205A

Atropine sulfate 20+ Cited Publications 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-107646

PD 102807	mAChR	Neurological Disease
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.

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-B0321

Tropicamide 5 Publications Verification 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-A0082

Diphenidol hydrochloride 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-107647

(S)-(+)-Dimethindene maleate 1 Publications Verification	mAChR Histamine Receptor	Inflammation/Immunology
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M₂-selective muscarinic receptor antagonist (pA₂ = 7.86/7.74; pK_i = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M₁ (pA₂ = 6.83/6.36; pK_i = 7.08), the M₃ (pA₂ = 6.92/6.96; pK_i = 6.70) and the M₄ receptors (pK_i = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H₁ receptor antagonist (pA₂ = 7.48) .

HY-70053

Fesoterodine	mAChR	Neurological Disease Metabolic Disease
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i 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-15885

LY2119620	mAChR	Neurological Disease
LY2119620 is a high-affinity muscarinic **M₂/M₄ receptor** agonist.

HY-112209

VU0467154 5 Publications Verification	mAChR	Neurological Disease
VU0467154 is a positive allosteric modulator of the *M4 muscarinic* acetylcholine receptor (mAChR), potentiating the response to ACh with pEC₅₀*s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor*, respectively.

HY-109013

Sofpironium bromide BBI 4000	mAChR	Neurological Disease
Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes .

HY-122203

PCS1055 dihydrochloride 2 Publications Verification	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 K_d** of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ ³H]-NMS binding to the M4 receptor with a K_i 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-N7247

Thiochrome	mAChR	Metabolic Disease
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 .

HY-B1205R

Atropine (Standard) 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-14539A

Clozapine hydrochloride 10+ Cited Publications 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 K_i of 75 nM. Clozapine hydrochloride inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is 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) .

HY-14539R

Clozapine (Standard) 10+ Cited Publications 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 K_i of 75 nM. Clozapine inhibits the **muscarinic M1 receptor** and serotonin 5HT2A receptor with K_is 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-17366R

Clozapine N-oxide (Standard)	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-70053A

Fesoterodine L-mandelate	mAChR	Neurological Disease Metabolic Disease Cancer
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i 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-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-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 K_d** of 5.72 nM. PCS1055 inhibits radioligand [ ³H]-NMS binding to the M4 receptor with a K_i 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-156331

VU6004909	mGluR	Neurological Disease
VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC₅₀s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .

HY-B0321S

Tropicamide-d3 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-105182S1

Xanomeline-d3 LY-246708-d₃	Isotope-Labeled Compounds mAChR	Neurological Disease
Xanomeline-d₃ (LY-246708-d₃) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .

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-101841

LY 2033298	mAChR	Neurological Disease
LY 2033298 is a selective positive allosteric modulator of the muscarinic M₄ receptor. LY 2033298 can be used in the study of psychiatric disorders .

HY-B1205AR

Atropine sulfate (Standard) 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-162663

VU0448088 ML253	mAChR	Neurological Disease
VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC₅₀ values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic .

HY-107656

PTAC oxalate	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 (K_i** 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-A0030S

Fesoterodine-d7 fumarate	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-174259

Muscarinic M4 modulator-1	mAChR	Neurological Disease
Muscarinic M4 modulator-1 is a **Muscarinic M4 receptor** positive allosteric modulator. Muscarinic M4 modulator-1 activates the muscarinic M4 receptor with allosteric potency EC₅₀ s of 14 and 3 Nm in CHO-K1 cells and HEK293 cells. Muscarinic M4 modulator-1 has an antipsychotic-like activity, promising for psychiatric and/or neurological disorders research .

HY-175532

M4 mAChR Modulator-2	mAChR	Neurological Disease
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 K_i 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

HY-N7247R

Thiochrome (Standard)	Reference Standards mAChR	Metabolic Disease
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 .

HY-105182AR

Xanomeline tartrate (Standard) LY 246708 tartrate (Standard)	Reference Standards mAChR	Neurological Disease
Xanomeline (tartrate) (Standard) is the analytical standard of Xanomeline (tartrate). This product is intended for research and analytical applications. Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .

HY-A0270

Diphenidol	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-107652

AF-DX 384	mAChR	Neurological Disease
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (K_is=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-12158

VU0238441	mAChR	Neurological Disease
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 .

HY-160440A

VU6021625	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-A0030R

Fesoterodine fumarate (Standard)	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) .

Cat. No.	Product Name	Target	Research Area

HY-P5846

Muscarinic toxin 3 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, α_1A, α_1B, α_1D,α_2A,α_2B and α_2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1205

Atropine 20+ Cited Publications Tropine tropate; DL-Hyoscyamine	Alkaloids Structural Classification Other Alkaloids Atropa belladonna Linn. Solanaceae Plants Endogenous metabolite Source Classification	Environmental Pollutants Endogenous Metabolite mAChR
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-B1205R

Atropine (Standard) 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

Atropine sulfate (Standard) 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-B0394R

Atropine sulfate monohydrate (Standard) 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 .

Cat. No.	Product Name	Chemical Structure

HY-B0321S

Tropicamide-d3
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-105182S1

Xanomeline-d3
Xanomeline-d₃ (LY-246708-d₃) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .

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-A0030S

Fesoterodine-d7 fumarate
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

rac-Fesoterodine-d14 fumarate
(Rac)-Fesoterodine-d₁₄ fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_ivalues 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-W720879

Fesoterodine-d3
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-A0082S

Diphenidol-d10 hydrochloride

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-W748582

Clozapine N-oxide-d8

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-14539S3

Clozapine-d3

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 K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is 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-B0298AS

Clemastine-d5 fumarate

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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