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

mAChR

Muscarinic acetylcholine receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-160888
    ASP8302
    Modulator 98.95%
    ASP8302 is a positive and allosteric muscarinic M3 receptor modulator. ASP8302 improves voiding efficiency and reduced residual urine volume in two voiding dysfunction models. ASP8302 can be used for research of underactive bladder.
    ASP8302
  • HY-107648
    McN-A-343
    Agonist 99.89%
    McN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 produces a significant inhibitory effect on Muscarine (HY-121404)-evoked catecholamine secretion from the isolated perfused rat adrenal gland. McN-A-343 is involved in the regulation of neuronal firing and activates enteroendocrine L cells to release glucagon-like peptide 1 (GLP-1) and modulates the secretion of α-melanocyte stimulating hormone (α-MSH) from the pituitary gland in the central nervous system. McN-A-343 reduces colonic inflammation and oxidative stress in Acetic acid (HY-Y0319)-induced ulcerative colitis (UC) mice. McN-A-343 can be used for the study of ulcerative colitis.
    McN-A-343
  • HY-107646
    PD 102807
    Antagonist 98.52%
    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.
    PD 102807
  • HY-13204
    Biperiden hydrochloride
    Inhibitor 99.90%
    Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders.
    Biperiden hydrochloride
  • HY-105296
    Blarcamesine
    Modulator 99.51%
    Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
    Blarcamesine
  • HY-B1789A
    Telenzepine dihydrochloride
    Antagonist 99.57%
    Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects.
    Telenzepine dihydrochloride
  • HY-U00050
    (E)-10-Hydroxynortriptyline
    99.65%
    (E)-10-Hydroxynortriptyline (E-10-OH-NT) is a blood-brain barrier-permeable norepinephrine uptake inhibitor. (E)-10-Hydroxynortriptyline effectively promotes central norepinephrine neuronal transmission, with little interindividual variation in in vivo potency. (E)-10-Hydroxynortriptyline has low affinity for muscarinic receptors, exhibits only extremely weak anticholinergic activity, and does not inhibit salivary secretion. (E)-10-Hydroxynortriptyline can be used in studies related to depression.
    (E)-10-Hydroxynortriptyline
  • HY-70053A
    Fesoterodine L-mandelate
    Antagonist 98.92%
    Fesoterodine L-mandelate 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 L-mandelate is used for the overactive bladder (OAB).
    Fesoterodine L-mandelate
  • HY-14539R
    Clozapine (Standard)
    Modulator
    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 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 (Standard)
  • HY-B0662
    Imidafenacin
    Inhibitor 99.26%
    Imidafenacin (KRP-197; ONO-8025) is an orally active inhibitor of muscarinic (mAChR) M1 and M3 receptors. Imidafenacin potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin can be used in research related to overactive bladder.
    Imidafenacin
  • HY-N0340
    Scopolamine butylbromide
    Antagonist 99.97%
    Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer.
    Scopolamine butylbromide
  • HY-12980
    Batefenterol
    Antagonist 99.72%
    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
    Batefenterol
  • HY-90010
    Tolterodine tartrate
    Antagonist 98.64%
    Tolterodine tartrate (Kabi-2234) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine tartrate competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine tartrate restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine tartrate ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine tartrate can be used for the research of urinary tract infections and overactive bladder.
    Tolterodine tartrate
  • HY-113616A
    VU0364572 TFA
    Agonist 98.79%
    VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant.
    VU0364572 TFA
  • HY-120081A
    Metixene hydrochloride hydrate
    Antagonist 99.92%
    Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride hydrate potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride hydrate can be used for the research of parkinsonian.
    Metixene hydrochloride hydrate
  • HY-B1339
    Dicyclomine hydrochloride
    Inhibitor 98.09%
    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.
    Dicyclomine hydrochloride
  • HY-70053
    Fesoterodine
    Antagonist 99.61%
    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).
    Fesoterodine
  • HY-118342
    PQCA
    Agonist 99.96%
    PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
    PQCA
  • HY-173396
    VU0467319
    Modulator 98.53%
    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.
    VU0467319
  • HY-109013
    Sofpironium bromide
    Inhibitor 98.26%
    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 bromide
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