2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mAChR

mAChR

Muscarinic acetylcholine receptor

mAChR

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mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia.

mAChR Isoform Specific Products:

mAChR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-131196
    M3 mAChR agonist 1
    		Agonist
    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.
    M3 mAChR agonist 1
  • HY-120004
    PF-06827443
    PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion.
    PF-06827443
  • HY-128783
    VU0090157
    		Modulator
    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.
    VU0090157
  • HY-B0394R
    Atropine sulfate monohydrate (Standard)
    		Antagonist
    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.
    Atropine sulfate monohydrate (Standard)
  • HY-B1188R
    Propantheline bromide (Standard)
    		Antagonist
    Propantheline (bromide) (Standard) is the analytical standard of Propantheline (bromide). This product is intended for research and analytical applications. Propantheline bromide is an orally active mAChR antagonist. Propantheline bromide can be used in the research of smooth muscle dysfunction, excessive sweating, cramps or spasms of the stomach, intestines or bladder, and involuntary urination.
    Propantheline bromide (Standard)
  • HY-123566
    PSD-506
    		Antagonist
    PSD-506 (RO 3202904) is a muscarinic M2/M3 antagonist. PSD-506 has the potential to be used in studies of bladder overactivity and urinary incontinence.
    PSD-506
  • HY-120081B
    Metixene hydrochloride
    		Antagonist
    Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride can be used for the research of parkinsonian.
    Metixene hydrochloride
  • HY-122548
    Butropium bromide
    		Antagonist
    Butropium bromide is a competitive mAChR antagonist. Butropium bromide blocks acetylcholine-mediated glandular secretion and muscle contraction signals, suppressing salivary gland secretion and respiratory smooth muscle spasms. Butropium bromide is promising for research of excessive salivation.
    Butropium bromide
  • HY-118406A
    Ethybenztropine hydrochloride
    		Inhibitor
    Ethybenztropine hydrochloride (Ponalid hydrochloride) is an anticholinergic drug with antiparkinsonian activity. Ethybenztropine hydrochloride may also have dopamine reuptake inhibitory effects. Ethybenztropine hydrochloride is used to improve motor symptoms in patients with Parkinson's disease. Ethybenztropine hydrochloride exerts its inhibitory effects by regulating the balance of neurotransmitters.
    Ethybenztropine hydrochloride
  • HY-P5175
    Muscarinic toxin 7
    		Antagonist
    Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor.
    Muscarinic toxin 7
  • HY-N17849
    Frititorine A
    Frititorine A is a steroidal alkaloid that exists in the bulbs of Fritillaria tortifolia. Frititorine A exerts a relaxing effect on acetylcholine-induced tracheal contraction. Frititorine A can be used in asthma-related research.
    Frititorine A
  • HY-181559S
    VU6025733
    		Activator
    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.
    VU6025733
  • HY-B0662A
    Imidafenacin hydrochloride
    		Inhibitor
    Imidafenacin (KRP-197; ONO-8025) hydrochloride is an orally active inhibitor of muscarinic (mAChR) M1 and M3 receptors. Imidafenacin hydrochloride potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin hydrochloride can be used in research related to overactive bladder.
    Imidafenacin hydrochloride
  • HY-123852
    PF-06764427
    		Modulator
    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.
    PF-06764427
  • HY-A0083B
    Methacholine bromide
    		Agonist
    Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
    Methacholine bromide
  • HY-14539S3
    Clozapine-d3
    		Modulator
    Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine-d<sub>3</sub>
  • HY-172418
    Betovumeline
    		Agonist
    Betovumeline is the agonist for muscarinic receptor and can be used for researchs of neurological disorders.
    Betovumeline
  • HY-116569
    VU0455691
    		Antagonist
    VU0455691 is a potent, selective orthosteric M1 mAChR antagonist (pIC50=6.64; IC50=0.23 µM for hM1).
    VU0455691
  • HY-109013S
    Sofpironium-13C,d3 bromide
    		Inhibitor
    Sofpironium-13C,d3 bromide (BBI 4000-13C,d3) is the deuterium and 13C-labeled Sofpironium bromide (HY-109013). 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.
    Sofpironium-<sup>13</sup>C,d<sub>3</sub> bromide
  • HY-105793
    Mazaticol
    		Inhibitor
    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.
    Mazaticol
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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