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-162491
    JR-6
    		Agonist
    JR-6 is a Gi/o pathway biased and muscarinic M2 selective partial agonist.
    JR-6
  • HY-182587
    VU0415248
    		Inhibitor
    VU0415248 is a selective muscarinic acetylcholine receptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1 muscarinic acetylcholine receptors, with an IC50 of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome.
    VU0415248
  • 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..
    Trihexyphenidyl-d<sub>5</sub>
  • HY-183203
    VU0476406
    		Activator
    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.
    VU0476406
  • HY-B0321R
    Tropicamide (Standard)
    		Antagonist
    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.
    Tropicamide (Standard)
  • HY-76570S2
    (Rac)-5-Hydroxymethyl tolterodine-d5
    		Antagonist
    (Rac)-5-hydroxymethyl Tolterodine-d5 ((Rac)-Desfesoterodine-d5; (Rac)-PNU-200577-d5) is deuterium-labeled (Rac)-5-Hydroxymethyl Tolterodine (HY-76570).
    (Rac)-5-Hydroxymethyl tolterodine-d<sub>5</sub>
  • HY-G0021S1
    N-Desmethylclozapine-d8 hydrochloride
    		Agonist 99.74%
    N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist.
    N-Desmethylclozapine-d<sub>8</sub> hydrochloride
  • HY-131507
    Emepronium bromide
    		Ligand
    Emepronium bromide is an antispasmodic agent for the bladder and a muscarinic receptor ligand, with an IC50 of 236 nM. Emepronium bromide is applicable to research related to bladder diseases.
    Emepronium bromide
  • HY-120322
    MK-0969
    		Antagonist
    MK-0969 is a M3 antagonist. MK-0969 can be used for research about chronic obstructive pulmonary disease and urinary incontinence.
    MK-0969
  • HY-109006
    Ilmetropium iodide
    		Inhibitor
    Ilmetropium iodide is an anticholinergic agent. Ilmetropium iodide selectively blocks M-cholinergic receptors of bronchial muscle, reduces or prevents bronchoconstrictor response associated with both cholinergic stimulation, as well as the impact of the factors that provoke bronchospasm. Strength and selectivity of ilmetropium iodide action substantially exceeds Atropine sulfate (HY-B1205A) and Ipratropium bromide (HY-B0241).
    Ilmetropium iodide
  • HY-19685A
    Sintropium bromide
    		Antagonist
    Sintropium bromide is a mAChR antagonist with anticholinergic effects. Sintropium bromide can be used for pain and spasm research.
    Sintropium bromide
  • HY-137311
    (S)-Albuterol hydrochloride
    		Activator
    (S)-Albuterol hydrochloride is a muscarinic receptor and phospholipase C activator. (S)-Albuterol hydrochloride increases intracellular free calcium in airway smooth muscle.
    (S)-Albuterol hydrochloride
  • HY-116586A
    (Rac)-AF710B
    		Agonist
    (Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.
    (Rac)-AF710B
  • HY-119363
    VU6009453
    		Agonist
    VU6009453 (compound 15q) is a brain-penetrant M4 mAChR positive allosteric modulator (PAM) with an EC50 of 383 nM. VU6009453 can be used for research on neurological diseases.
    VU6009453
  • HY-B0520AR
    Benztropine mesylate (Standard)
    		Inhibitor
    Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
    Benztropine mesylate (Standard)
  • HY-17037S
    Pirenzepine-d8
    Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
    Pirenzepine-d<sub>8</sub>
  • HY-107656
    PTAC oxalate
    		Modulator
    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 (Ki 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.
    PTAC oxalate
  • HY-122086
    Prifinium bromide
    		Inhibitor 99.41%
    Prifinium bromide is an anticholinergic drug with anticholinergic and antispasmodic activities, and it exhibits oral activity. Prifinium bromide competitively antagonizes cholinergic receptors and relieves symptoms of spasm or hypermotility in the digestive and urinary tracts, with its anticholinergic activity representing the core mechanism underlying the inhibition of bladder smooth muscle contraction. Prifinium bromide can be used in research related to spasms and diverticular disease.
    Prifinium bromide
  • 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.
    Dicyclomine-d<sub>4</sub>
  • HY-175532
    M4 mAChR Modulator-2
    		Activator
    M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
    M4 mAChR Modulator-2
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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