mAChR2
The M2 muscarinic acetylcholine receptor (mAChR2) functions as a G protein-coupled receptor that regulates acetylcholine signaling in both neuronal and non-neuronal cells[1]. Mechanistically, M2 modulates presynaptic neurotransmitter release via coupling to protein kinase C (PKC) and PDK1, selectively influencing PKCβI and PKCε isoforms and downstream SNARE machinery[2]. In the neuromuscular junction, M2 participates in developmental synapse elimination by regulating activity-dependent acetylcholine release, coordinating with M1/M4 mAChRs and adenosine receptors[3][4]. Beyond the nervous system, M2 receptors control epithelial and immune cell functions, including endocytosis-mediated receptor trafficking and signaling regulation[1]. In cardiac myocytes, M2 activation triggers endothelial nitric oxide synthase (eNOS)-dependent nitration of p190A RhoGAP, enhancing RhoA activity and altering cytoskeletal dynamics[5]. In disease models, down-regulation of M2 adversely affects Alzheimer’s disease-relevant genes, including BACE1, and disrupts amyloid precursor protein processing[5][6]. Compared with related muscarinic isoforms, M2 uniquely suppresses BACE1 expression, whereas M1 activation increases it[6]. Pharmacologically, selective M2 inhibitors, such as methoctramine, can block agonist-induced signaling in smooth muscle and macrophages, providing tools for dissecting M2-specific pathways[7][8]. These characteristics render M2 a critical target for experimental modulation in studies of synaptic plasticity, neurodegeneration, cardiac physiology, and immune regulation[1][2][5].
References:
- [1]. Züchner T, et al. Beta-secretase BACE1 is differentially controlled through muscarinic acetylcholine receptor signaling. J Neurosci Res. 2004 Jul 15;77(2):250-7. [Content Brief]
- [2]. de la Torre E, et al. Muscarinic receptors participation in angiogenic response induced by macrophages from mammary adenocarcinoma-bearing mice. Breast Cancer Res. 2005;7(3):R345-52. [Content Brief]
- [3]. Tsymbalyuk OV, et al. 8-[(4-benzylpiperazin-1-yl)methyl]-3-(2-chlorophenyl)-7-hydroxy-chromen-4-one is an activator of contractile activity of intestinal smooth muscles with reversible M2 cholinomimetic properties. Stud Biol. 2023;17(4):15-36.
- [4]. Ockenga W, et al. Non-neuronal functions of the m2 muscarinic acetylcholine receptor. Genes (Basel). 2013 Apr 2;4(2):171-97. [Content Brief]
- [5]. Nadal L, et al. Presynaptic muscarinic acetylcholine autoreceptors (M1, M2 and M4 subtypes), adenosine receptors (A1 and A2A) and tropomyosin-related kinase B receptor (TrkB) modulate the developmental synapse elimination process at the neuromuscular junction. Mol Brain. 2016 Jun 23;9(1):67. [Content Brief]
- [6]. Cilleros-Mañé V, et al. M1 and M2 mAChRs activate PDK1 and regulate PKC βI and ε and the exocytotic apparatus at the NMJ. FASEB J. 2021 Jul;35(7):e21724. [Content Brief]
- [7]. Zuchner T, et al. Down-regulation of muscarinic acetylcholine receptor M2 adversely affects the expression of Alzheimer's disease-relevant genes and proteins. J Neurochem. 2005 Oct;95(1):20-32. [Content Brief]
- [8]. Levay MK, et al. The Muscarinic Acetylcholine M2 Receptor-Induced Nitration of p190A by eNOS Increases RhoA Activity in Cardiac Myocytes. Cells. 2023 Oct 11;12(20):2432. [Content Brief]
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mAChR2 Related Products (57)
Related Products (57)
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Dicyclomine
0 ImagesDicyclomine (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.
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A-72055
0 ImagesCat. No.: HY-108157CAS No.: 150358-76-2A-72055 is a partial agonist of muscarinic receptors. A-72055 has binding activity to both M1 and M2 receptors, with Ki values of 32 nM and 30 nM, respectively. A-72055 can enhance cognitive function and improve learning and memory deficits. A-72055 has better security. A-72055 can be used for research on neurological disorders such as cognitive impairment.
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MHP 133
0 ImagesCat. No.: HY-101653CAS No.: 147340-43-0MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
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M1/M2/M4 muscarinic agonist 1
0 ImagesCat. No.: HY-149704CAS No.: 2640109-42-6M1/M2/M4 muscarinic agonist 1 (Compound 42) is a muscarinic M4/M1/M2 agonist with EC50 values of 6.5, 26 and 210 nM for M4/M1/M2, respectively. M1/M2/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusion, etc.
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PSD-506
0 ImagesCat. No.: HY-123566CAS No.: 754177-77-0Synonyms: RO 3202904PSD-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.
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p-F-HHSiD
0 ImagesCat. No.: HY-137388CAS No.: 116679-83-5Synonyms: p-Fluorohexahydrosiladifenidolp-F-HHSiD (p-Fluorohexahydrosiladifenidol) is a potent and selective M3 mAChR antagonist. p-F-HHSiD has antagonistic effects on other subtypes of the M receptor and the alpha1-adrenoceptor. p-F-HHSiD can be used for the researches of cancer, metabolic, neurological and cardiovascular disease such as, colon cancer, Alzheimer’s disease and diabetes.
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TAAR1 agonist 2
0 ImagesCat. No.: HY-W909173CAS No.: 1804128-38-8TAAR1 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.
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Sofpironium tosylate
0 ImagesCat. No.: HY-167849CAS No.: 2409055-48-5Synonyms: BBI-4000 tosylateSofpironium (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.
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Ipratropium-d7 bromide
0 ImagesCat. No.: HY-B0241S1Synonyms: Sch 1000-d7 bromideIpratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
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AE9C90CB
0 ImagesCat. No.: HY-134971CAS No.: 893426-98-7AE9C90CB, muscarinic receptor antagonist, has greater affinity for M3 muscarinic receptors with pKi of 9.90 and was 20-fold more selective for M3 than for M2 muscarinic receptors.
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Revatropate
0 ImagesCat. No.: HY-126184CAS No.: 149926-91-0Synonyms: UK-112166Revatropate is an antimuscarinic compound. Revatropate has a much greater inhibitory effect on M1 and M3 receptors than on the M2 subtype. Revatropate is used in the study of urge urinary incontinence and functional bowel disorders.
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Atropine oxide hydrochloride
0 ImagesCat. No.: HY-122510ACAS No.: 4574-60-1Synonyms: Atropine oxidation hydrochlorideAtropine 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.
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Arecaidine-propargyl ester
0 ImagesCat. No.: HY-183853CAS No.: 35516-99-5Arecaidine-propargyl ester is a selective M2 muscarinic receptor agonist with blood-brain barrier permeability, with a pKi of 5.91 for hm1, 7.06 for hm2, 6.07 for hm3, 6.01 for hm4, and 6.03 for hm5. Arecaidine-propargyl ester stimulates central and peripheral muscarinic receptors. Arecaidine-propargyl ester increases intracellular ROS, induces DNA damage and Apoptosis, and upregulates the expression of MnSOD and SIRT1. Arecaidine-propargyl ester reduces sympathetic nerve outflow, induces dose-dependent hypotension, and triggers negative chronotropic effects at high peripheral doses. Arecaidine-propargyl ester can be used in research related to Alzheimer's disease and glioblastoma.
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(1R,3S-)Solifenacin-d5 hydrochloride
0 ImagesCat. No.: HY-135329SCAS No.: 1217810-85-9(1R,3S-)Solifenacin-d5 hydrochloride is the deuterium labeled Solifenacin hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
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NPC-14695
0 ImagesCat. No.: HY-183932CAS No.: 146561-59-3NPC-14695 is a competitive and selective M3 muscarinic receptor antagonist, with a Kd value of 15 nM for guinea pig M3, 60 nM for guinea pig M2, and 25 nM for rabbit M1. NPC-14695 exhibits higher activity towards M3 receptors in bronchial smooth muscle than towards those regulating salivary secretion. NPC-14695 inhibits Carbachol (HY-B1208)-induced contraction of isolated rabbit iris smooth muscle.
