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muscarinic acetylcholine receptor M4

" in MedChemExpress (MCE) Product Catalog:

By Targets:	mAChR (34) Apoptosis (4) Autophagy (4) Endogenous Metabolite (2) Environmental Pollutants (1) Histamine Receptor (4) IKK (4) Isotope-Labeled Compounds (1) Keap1-Nrf2 (4) mTOR (4) p62 (4) Parasite (1) Pyroptosis (4) Reference Standards (6)
By Research Areas:	Cancer (4) Cardiovascular Disease (8) Inflammation/Immunology (2) Metabolic Disease (5) Neurological Disease (32)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: mAChR nAChR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-B0394

Atropine sulfate monohydrate Maximum Cited Publications 25 Publications Verification 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 Maximum Cited Publications 25 Publications Verification 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-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-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-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-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-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-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-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-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-156128

Imidafenacin Metabolite M4	mAChR	Neurological Disease
Imidafenacin Metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist Imidafenacin (HY-B0662) .

HY-120184

VU0467485 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 EC₅₀*s 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-B1205B

Atropine hydrobromide Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide	mAChR	Cardiovascular Disease Neurological Disease Cancer
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC₅₀ values of 0.39 and 0.71 nM for Human mAChR M₄ and Chicken mAChR M₄, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia .

HY-119333

NNC 11-1607	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-122510

Atropine oxide Atropine oxidation	Parasite	Neurological Disease
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.

HY-122510A

Atropine oxide hydrochloride Atropine oxidation hydrochloride	mAChR
Atropine Oxide (Atropine oxidation) hydrochloride, a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings .

HY-B0394R

Atropine sulfate monohydrate (Standard) Tropine tropate sulfate monohydrate (Standard); DL-Hyoscyamine sulfate monohydrate (Standard)	Reference Standards mAChR	Cardiovascular Disease Neurological Disease
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC₅₀ values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .

HY-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-B0321R

Tropicamide (Standard) Ro 1-7683 (Standard)	Reference Standards mAChR	Neurological Disease
Tropicamide (Standard) is the analytical standard of Tropicamide. This product is intended for research and analytical applications. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .

HY-124223

AF-DX 384 methanesulfonate	mAChR	Neurological Disease
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (K_is=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .

HY-180421

VU6009048	mAChR	Neurological Disease
VU6009048 is a CNS-penetrant human M4 muscarinic acetylcholine receptor (mAChR4) positive allosteric modulator. VU6009048 can be used for the research of parkinson’s disease, huntington’s disease, schizophrenia .

HY-181559S

VU6025733 AG06827	mAChR	Neurological Disease
VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M₄ mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC₅₀ of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease .

HY-B0298AS

Clemastine-d5 fumarate 1 Publications Verification 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-B0298AR

Clemastine fumarate (Standard) 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-183203

VU0476406	mAChR	Neurological Disease
VU0476406 is a blood-brain barrier-permeable and selective muscarinic acetylcholine receptor subtype 4 (M4) activator with human EC₅₀ of 91.0 nM and human pEC₅₀ of 7.04. VU0476406 potentiates endogenous acetylcholine activity at M4 receptors. VU0476406 can be used for the research of Parkinson's disease .

HY-183144

Vedaclidine	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-123778

VU6007678	mAChR	Neurological Disease
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 .

HY-131196

M3 mAChR agonist 1	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	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-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 .

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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