mAChR1
mAChR1 (M1 muscarinic acetylcholine receptor) mediates acetylcholine-induced neurotransmission and is widely expressed in the central nervous system[1]. Mechanistically, M1 activates multiple signaling cascades, including Gαq/11-dependent inositol phosphate signaling, while orthosteric and allosteric agonists can produce distinct downstream coupling profiles[2]. In experimental models, M1 knockout ablates muscarinic receptor-dependent M-current regulation and reduces pilocarpine-induced seizure activity, supporting its use in neuronal excitability studies[3]. In Alzheimer’s disease research, M1 activation links cholinergic hypofunction to APP processing, Aβ production, tau phosphorylation, and learning and memory pathways[1]. Compared with related isoforms, M1 and M4 have distinct orthosteric and allosteric binding-site features, but the conserved acetylcholine pocket makes subtype-selective orthosteric ligand design difficult[4]. For experimental applications, M1 positive allosteric modulators such as BQCA and BQZ-12 restored memory loss and slowed disease progression in mouse prion disease models[5].
References:
- [1]. Jiang S, et al. M1 muscarinic acetylcholine receptor in Alzheimer's disease. Neurosci Bull. 2014 Apr;30(2):295-307. [Content Brief]
- [2]. Thomas RL, et al. G protein coupling and signaling pathway activation by m1 muscarinic acetylcholine receptor orthosteric and allosteric agonists. J Pharmacol Exp Ther. 2008 Nov;327(2):365-74. [Content Brief]
- [3]. Hamilton SE, et al. Disruption of the m1 receptor gene ablates muscarinic receptor-dependent M current regulation and seizure activity in mice. Proc Natl Acad Sci U S A. 1997 Nov 25;94(24):13311-6. [Content Brief]
- [4]. Thal DM, et al. Crystal structures of the M1 and M4 muscarinic acetylcholine receptors. Nature. 2016 Mar 17;531(7594):335-40. [Content Brief]
- [5]. Bradley SJ, et al. M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss. J Clin Invest. 2017 Feb 1;127(2):487-499. [Content Brief]
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mAChR1 Related Products (121)
Related Products (121)
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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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Clozapine dihydrochloride
0 ImagesCat. No.: HY-14539BCAS No.: 2711603-38-0Synonyms: HF 1854 dihydrochlorideClozapine (HF 1854) dihydrochloride 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).
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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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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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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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PF-06764427
0 ImagesCat. No.: HY-123852CAS No.: 1842371-08-7PF-06764427 is a selective M1 muscarinic acetylcholine receptor positive allosteric modulator. PF-06764427 exhibits robust M1 agonist activity. PF-06764427 can be used in the research of Alzheimer's disease and schizophrenia.
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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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rel-Biperiden-d5
0 ImagesCat. No.: HY-13204S1rel-Biperiden-d5 is deuterium labeled Biperiden (hydrochloride).
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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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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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M1 receptor modulator-1
0 ImagesCat. No.: HY-184057CAS No.: 34099-70-2M1 receptor modulator-1 is a low-efficacy positive allosteric modulator of the muscarinic M1 receptor (mAChR1), with an EC50 of 71 nM for the human M1 receptor. M1 receptor modulator-1 enables use-dependent attenuation of neurotransmitter signals and exhibits excellent in vivo properties without pseudo-agonist activity. M1 receptor modulator-1 can be used in research related to Alzheimer's disease and schizophrenia.
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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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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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Scotanamine D
0 ImagesCat. No.: HY-N12302CAS No.: 1698873-84-5Synonyms: N1-Dihydrocaffeoyl, N10-caffeoyl spermidineScotanamine D (N1-Dihydrocaffeoyl, N10-caffeoyl spermidine) is a spermidine alkaloid. It can be isolated from S. tangutica. Scotanamine D potently and selectively inhibits the activity of the M1 muscarinic acetylcholine receptor, with an IC50 of 32 nM. It can be used in studies related to Parkinson's disease.
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Rispenzepine
0 ImagesCat. No.: HY-U00030CAS No.: 96449-05-7Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.
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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.
