mAChR5
Muscarinic acetylcholine receptor subtype 5 (mAChR5) is a G protein-coupled receptor that regulates intracellular calcium signaling and modulates synaptic plasticity in neural circuits[1][2]. Mechanistically, mAChR5 activation engages the ERK1/2 and cAMP-responsive element-binding protein (CREB) pathways, promoting neurogenesis and neuronal differentiation in precursor cells[1]. In disease models, mAChR5 participates in neuroinflammatory regulation, with agonist stimulation reducing microglial pro-inflammatory phenotypes and conferring neuroprotection in central nervous system inflammation[3]. Compared with related muscarinic isoforms such as M1 and M4, mAChR5 exhibits distinct G protein coupling and intracellular signaling profiles, which confer functional specificity in neuronal and non-neuronal contexts[2][4]. Selective agonists and allosteric modulators of mAChR5 have been developed to enhance receptor-mediated signaling without activating closely related subtypes, enabling refined modulation of neuronal proliferation, synaptic plasticity, and behavioral outcomes[5][4]. These ligands demonstrate brain region-specific efficacy, revealing differential activation of downstream effectors such as phospholipase C, β-arrestin, and MAP kinase cascades, which are critical for experimental applications in cognitive and neurodegenerative disorder research[5][2]. Therefore, mAChR5 represents a precise target for studies aiming to dissect isoform-specific cholinergic signaling and its impact on neurodevelopment, neuroprotection, and synaptic regulation[3][4].
References:
- [1]. Zhao WQ, et al. c-Src protein tyrosine kinase activity is required for muscarinic receptor-mediated DNA synthesis and neurogenesis via ERK1/2 and c-AMP-responsive element-binding protein signaling in neural precursor cells. J Neurosci Res. 2003 May 1;72(3):334-42. [Content Brief]
- [2]. Wang K, et al. The Activation of Muscarinic Acetylcholine Receptors Protects against Neuroinflammation in a Mouse Model through Attenuating Microglial Inflammation. Int J Mol Sci. 2024 Sep 27;25(19):10432. [Content Brief]
- [3]. Digby GJ, et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J Neurosci. 2012 Jun 20;32(25):8532-44. [Content Brief]
- [4]. Sumi T, et al. Muscarinic acetylcholine receptor-dependent and NMDA receptor-dependent LTP and LTD share the common AMPAR trafficking pathway. iScience. 2023 Feb 3;26(3):106133. [Content Brief]
- [5]. Marlo JE, et al. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Mol Pharmacol. 2009 Mar;75(3):577-88. [Content Brief]
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mAChR5 Related Products (38)
Related Products (38)
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p-F-HHSiD hydrochloride
0 ImagesSynonyms: p-Fluorohexahydrosiladifenidol hydrochloridep-F-HHSiD (p-Fluorohexahydrosiladifenidol) hydrochloride is a potent and selective M3 mAChR antagonist. p-F-HHSiD hydrochloride has antagonistic effects on other subtypes of the M receptor and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride 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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(Rac)-5-Hydroxymethyl Tolterodine-d14
0 ImagesCat. No.: HY-76570SCAS No.: 1185071-13-9Synonyms: (Rac)-Desfesoterodine-d14; (Rac)-PNU-200577-d14(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research.
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Lu AE51090
0 ImagesLu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS).
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PTAC oxalate
0 ImagesCat. No.: HY-107656CAS No.: 201939-40-4PTAC 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.
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5-Hydroxymethyl Tolterodine-d14 formate
0 ImagesCat. No.: HY-76570S15-Hydroxymethyl Tolterodine-d14 (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research.
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Bethanechol-d6 chloride
0 ImagesCat. No.: HY-B0406ASSynonyms: Carbamyl-β-methylcholine-d6 chlorideBethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
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M1/M4 muscarinic agonist 4
0 ImagesCat. No.: HY-187957M1/M4 muscarinic agonist 4 is a dual-site muscarinic acetylcholine receptor ligand with potent agonistic activity at M1/M4 muscarinic acetylcholine receptors. M1/M4 muscarinic agonist 4 activates M1R to induce phosphorylation of ERK1/2, and activates M4R to induce GαoB protein activation as well as ERK1/2 phosphorylation. M1/M4 muscarinic agonist 4 exhibits higher binding affinity for M4R than for other muscarinic receptors, while its binding affinity for the W435A mutant M4R is reduced. M1/M4 muscarinic agonist 4 can be used in the research of schizophrenia.
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Umeclidinium-d10 bromide
0 ImagesCat. No.: HY-12100S1Synonyms: GSK573719A-d10Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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M3 mAChR agonist 1
0 ImagesCat. No.: HY-131196CAS No.: 1624297-26-2M3 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.
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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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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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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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rac-Fesoterodine-d14 fumarate
0 ImagesCat. No.: HY-70053SCAS No.: 1185237-08-4(Rac)-Fesoterodine-d14 fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKivalues 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).
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VU6035406
0 ImagesCat. No.: HY-184883CAS No.: 2746405-41-2VU6035406 is a functionally selective mAChR inhibitor, with mAChR IC50 values of 21 nM, 51 nM and 47 nM against human, rat and mouse targets, respectively. VU6035406 does not act as a P-glycoprotein substrate. VU6035406 shows extremely low inhibitory activity against cytochrome P450 1A2, 2C9, 2D6 and 3A4. VU6035406 can be used in the research of neurological and psychiatric disorders.
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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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