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-163702
    CHF-6550
    		Antagonist
    CHF-6550 is an antagonist for muscarinic M3 receptor and an agonist for β2 adrenoceptor (MABA), with pKi of 9.3 and 10.6, respectively. CHF-6550 exhibits good hepatocyte clearance in rat models and good pharmacokinetic characteristics in guinea pigs.
    CHF-6550
  • HY-B0549
    Flavoxate
    		Antagonist
    Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections.
    Flavoxate
  • HY-127022
    Anisodine
    		Inhibitor
    Anisodine (Daturamine) is a neuroprotective compound that reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine inhibits calcium ion influx and reactive oxygen species (ROS)levels. Anisodine leads to decreased aspartate levels during hypoxia.
    Anisodine
  • HY-101197
    SM-21 maleate
    SM 21 maleate, 2-phenoxyalkanoic acid ester, binds to central muscarinic recrptor with affinity of 0.174 μM.
    SM-21 maleate
  • HY-A0012R
    Darifenacin hydrobromide (Standard)
    		Antagonist
    Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects.
    Darifenacin hydrobromide (Standard)
  • HY-W909173
    TAAR1 agonist 2
    		Agonist
    TAAR1 agonist 2 (compound 30) is a full agonist of trace amine-associated receptor 1 (TAAR1) (pEC50=7.5). TAAR1 agonist 2 also exhibits agonist activity at H1 receptors and activates several members of the muscarinic acetylcholine receptor family, such as the M2 receptor (pEC50=5). TAAR1 agonist 2 can be used in the study of neuropsychiatric diseases.
    TAAR1 agonist 2
  • HY-N4080
    Cyclobuxine D
    		Inhibitor
    Cyclobuxine D is a steroidal alkaloid extracted from Buxus microphylla. Cyclobuxine D has a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and Ba++−induced contraction of the longitudinal muscle isolated from the rabbit jejunum.
    Cyclobuxine D
  • HY-A0024S
    Tolterodine-d14 hydrochloride
    		99.0%
    Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride. Tolterodine hydrochloride is a potent muscarinic receptor antagonist.
    Tolterodine-d<sub>14</sub> hydrochloride
  • HY-120802A
    Navafenterol saccharinate
    		Antagonist
    Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
    Navafenterol saccharinate
  • HY-17037AS
    Pirenzepine-d11
    Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells.
    Pirenzepine-d<sub>11</sub>
  • HY-13204S1
    rel-Biperiden-d5
    		Inhibitor
    rel-Biperiden-d5 is deuterium labeled Biperiden (hydrochloride).
    rel-Biperiden-d<sub>5</sub>
  • HY-159829
    Direclidine
    		Agonist
    Direclidine is a muscarinic M4 receptor positive allosteric modulator.
    Direclidine
  • HY-14539A
    Clozapine hydrochloride
    		Modulator
    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 Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis 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).
    Clozapine hydrochloride
  • HY-B0480R
    Brompheniramine maleate (Standard)
    		Inhibitor
    Brompheniramine (maleate) (Standard) is the analytical standard of Brompheniramine (maleate). This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
    Brompheniramine maleate (Standard)
  • HY-167849
    Sofpironium tosylate
    		Inhibitor
    Sofpironium (BBI 4000) tosylate is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium tosylate reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium tosylate also has a high afnity for the M1, M2, M4 and M5 subtypes.
    Sofpironium tosylate
  • HY-120792
    DAU 5884
    		Antagonist
    DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
    DAU 5884
  • HY-B1277S
    Trihexyphenidyl-d5 hydrochloride
    		Inhibitor
    Trihexyphenidyl-d5 (hydrochloride) is deuterium labeled Trihexyphenidyl (hydrochloride).
    Trihexyphenidyl-d<sub>5</sub> hydrochloride
  • HY-B1339S
    Dicyclomine-d4 hydrochloride
    Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). 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-d<sub>4</sub> hydrochloride
  • HY-173031
    KTX-005
    		Agonist
    KTX-005 is the agonist for mAChR that regulates the signaling pathway of the neurotransmitter acetylcholine, and can be used for research of schizophrenia.
    KTX-005
  • HY-15502
    PF-3635659
    		Antagonist
    PF-3635659 is a potent antagonist of the muscarinic M3 receptor (mAChR3). PF-3635659 can be used for chronic obstructive pulmonary disease (COPD) research.
    PF-3635659
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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