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].
Verweise:
- [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 Verwandte Produkte (39)
Verwandte Produkte (39)
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4-DAMP
0 Images4-DAMP (4-DAMP methiodide) is a potent and selective antagonist of M3 receptors and also has a high affinity for the closely-related M5 receptors. 4-DAMP combined with 5-Fluorouracil (5-Fu) (HY-90006) could significantly reduce the cell viability and enhance apoptosis in MKN45 and BGC823 gastric cancer cells. 4-DAMP inhibits lipopolysaccharide (LPS)- and tobacco-induced pulmonary inflammation and reduces mucin 5AC (MUC5AC), oligomeric mucus/gel-forming secretion.
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Bethanechol chloride
0 ImagesSynonyms: Carbamyl-β-methylcholine chloride
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Fesoterodine fumarate
0 ImagesArt. -Nr.: HY-A0030CAS. Nr.: 286930-03-8Fesoterodine Fumarate 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 Fumarate is used for the overactive bladder (OAB).
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VU6019650
0 ImagesVU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA).
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Sabcomeline hydrochloride
0 ImagesSynonyms: SB-202026 hydrochloride; Memric hydrochlorideSabcomeline (SB-202026; Memric) hydrochloride is a muscarinic receptor agonist capable of crossing the blood-brain barrier. Sabcomeline hydrochloride exhibits affinity for all hM1 to hM5 subtypes (pKi=6.72-7.23), and shows near-full agonism at the hM3 receptor, inducing extracellular acidification. Sabcomeline hydrochloride alters the binding kinetics of dopamine D2 receptors through neural network regulation. Sabcomeline hydrochloride also causes minimal cardiovascular changes, effectively reverses spatial memory deficits in rodents and induces conditioned taste aversion. Sabcomeline hydrochloride is an important tool compound in studies of Alzheimer's disease and related neurodegenerative diseases.
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Vedaclidine
0 ImagesArt. -Nr.: HY-183144CAS. Nr.: 141575-50-0Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states.
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THRX160209
0 ImagesArt. -Nr.: HY-189013CAS. Nr.: 832082-44-7THRX160209 is a dual-site antagonist of the M2 muscarinic acetylcholine receptor with M2 receptor subtype selectivity. THRX160209 binds simultaneously to the orthosteric site and a spatially distinct allosteric site, competitively inhibiting receptor activation at the acetylcholine binding pocket. THRX160209 exhibits affinity for all five muscarinic receptor subtypes. THRX160209 can be used in research related to neurological disorders.
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M1/M4 muscarinic agonist 4
0 ImagesArt. -Nr.: 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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(Rac)-5-Hydroxymethyl Tolterodine
0 ImagesSynonyms: (Rac)-Desfesoterodine; (Rac)-PNU-200577(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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Sofpironium bromide
0 ImagesSynonyms: BBI 4000Sofpironium 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.
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VU 0238429
0 ImagesVU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
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VU 6008667
0 ImagesVU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
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(Rac)-VU 6008667
0 Images(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride
0 ImagesArt. -Nr.: HY-76570ACAS. Nr.: 250214-40-5Synonyms: (Rac)-Desfesoterodine hydrochloride; (Rac)-PNU-200577 hydrochloride(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, 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 hydrochloride can be used for overactive bladder research.
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