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Gene Review

Chrm1  -  cholinergic receptor, muscarinic 1, CNS

Mus musculus

Synonyms: AW495047, Chrm-1, M1, M1R, Muscarinic acetylcholine receptor M1, ...
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Disease relevance of Chrm1


Psychiatry related information on Chrm1

  • We report that M1 deficiency leads to elevated dopaminergic transmission in the striatum and significantly increased locomotor activity [6].
  • In the present study, we examined whether the memory deficits and brain cholinergic deficiency of apoE-deficient mice can be ameliorated by the M1-selective agonist 1-methylpiperidine-4-spiro-(2'-methylthiazoline), [AF150(S)] [7].
  • The data show that the selective M1 agonist AF102B can restore AF64A-induced cognitive impairments, without producing adverse central and peripheral side effects at the effective doses and this can indicate its potential use for the treatment of Alzheimer's disease [8].
  • 2,8-Dimethyl-1-oxa-8-azaspiro[4,5]decan-3-one (17), designed by incorporating the tetrahydrofuran ring moiety of muscarone into an 8-azaspiro[4,5]decane skeleton, and related 1-oxa-8-azaspiro[4.5]decanes were synthesized and assessed as M1 muscarinic agonists for the symptomatic treatment of dementia of Alzheimer's type [9].
  • Although the data show that central nicotinic and muscarinic antagonists both modulate working memory performance, they indicate first, that scopolamine-induced "amnesia" results, not from selective post-synaptic M1 muscarinic blockade but from indirect over-activation of nicotinic receptors [10].

High impact information on Chrm1


Chemical compound and disease context of Chrm1


Biological context of Chrm1


Anatomical context of Chrm1

  • Quantitative reverse transcriptase-polymerase chain reaction studies with salivary gland tissue showed that the inactivation of the M(1) or M(3) mAChR genes did not lead to significantly altered mRNA levels of the remaining mAChR subtypes [24].
  • Direct coupling of M1 receptors in CHO cells to inhibitory G proteins was demonstrated using an anti-Galphai(1-3) antibody, and this binding was inhibited by 76% following PTX treatment [1].
  • 3-Cl-propylthio-TZTP and propoxy-TZTP had virtually no effect at the M1 receptor subtype as measured by the human m1 clone expressed in baby hamster kidney cells or the rabbit vas deferens assay [25].
  • Maximal carbachol-induced secretion from M1R-/- mouse gastric glands was decreased by 25% [26].
  • Cholinergic agonist-induced pepsinogen secretion from murine gastric chief cells is mediated by M1 and M3 muscarinic receptors [26].

Associations of Chrm1 with chemical compounds


Physical interactions of Chrm1


Regulatory relationships of Chrm1


Other interactions of Chrm1


Analytical, diagnostic and therapeutic context of Chrm1


  1. Determination of [35S]guanosine-5'-O-(3-thio)triphosphate binding mediated by cholinergic muscarinic receptors in membranes from Chinese hamster ovary cells and rat striatum using an anti-G protein scintillation proximity assay. DeLapp, N.W., McKinzie, J.H., Sawyer, B.D., Vandergriff, A., Falcone, J., McClure, D., Felder, C.C. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  2. Intrathecal clonidine inhibits mechanical allodynia via activation of the spinal muscarinic M1 receptor in streptozotocin-induced diabetic mice. Koga, K., Honda, K., Ando, S., Harasawa, I., Kamiya, H.O., Takano, Y. Eur. J. Pharmacol. (2004) [Pubmed]
  3. Regulation of muscarinic acetylcholine receptor number in cultured neuronal cells by chronic membrane depolarization. Liles, W.C., Nathanson, N.M. J. Neurosci. (1987) [Pubmed]
  4. Novel fragments of the Sjögren's syndrome autoantigens alpha-fodrin and type 3 muscarinic acetylcholine receptor generated during cytotoxic lymphocyte granule-induced cell death. Nagaraju, K., Cox, A., Casciola-Rosen, L., Rosen, A. Arthritis Rheum. (2001) [Pubmed]
  5. Ribonucleotide reductase gene expression during cyclic AMP-induced cell cycle arrest in T lymphocytes. Albert, D.A., Nodzenski, E. Exp. Cell Res. (1992) [Pubmed]
  6. Hyperactivity, elevated dopaminergic transmission, and response to amphetamine in M1 muscarinic acetylcholine receptor-deficient mice. Gerber, D.J., Sotnikova, T.D., Gainetdinov, R.R., Huang, S.Y., Caron, M.G., Tonegawa, S. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  7. M1 muscarinic agonist treatment reverses cognitive and cholinergic impairments of apolipoprotein E-deficient mice. Fisher, A., Brandeis, R., Chapman, S., Pittel, Z., Michaelson, D.M. J. Neurochem. (1998) [Pubmed]
  8. (+-)-cis-2-methyl-spiro(1,3-oxathiolane-5,3')quinuclidine, an M1 selective cholinergic agonist, attenuates cognitive dysfunctions in an animal model of Alzheimer's disease. Fisher, A., Brandeis, R., Karton, I., Pittel, Z., Gurwitz, D., Haring, R., Sapir, M., Levy, A., Heldman, E. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  9. Synthesis and structure-activity studies of a series of 1-oxa-8-azaspiro[4.5]decanes as M1 muscarinic agonists. Tsukamoto, S., Fujii, M., Yasunaga, T., Matsuda, K., Wanibuchi, F., Hidaka, K., Furuya, T., Tamura, T. Chem. Pharm. Bull. (1995) [Pubmed]
  10. Role of central cholinergic receptor sub-types in spatial working memory: a five-arm maze task in mice provides evidence for a functional role of nicotinic receptors in mediating trace access processes. Maviel, T., Durkin, T.P. Neuroscience (2003) [Pubmed]
  11. Antipsychotics block muscarinic acetylcholine receptor-mediated cyclic GMP formation in cultured mouse neuroblastoma cells. Richelson, E. Nature (1977) [Pubmed]
  12. Muscarinic acetylcholine receptor knockout mice: novel phenotypes and clinical implications. Wess, J. Annu. Rev. Pharmacol. Toxicol. (2004) [Pubmed]
  13. Selective cognitive dysfunction in acetylcholine M1 muscarinic receptor mutant mice. Anagnostaras, S.G., Murphy, G.G., Hamilton, S.E., Mitchell, S.L., Rahnama, N.P., Nathanson, N.M., Silva, A.J. Nat. Neurosci. (2003) [Pubmed]
  14. Human anti-p68 autoantibodies recognize a common epitope of U1 RNA containing small nuclear ribonucleoprotein and influenza B virus. Guldner, H.H., Netter, H.J., Szostecki, C., Jaeger, E., Will, H. J. Exp. Med. (1990) [Pubmed]
  15. Regulation of acetylcholine release by muscarinic receptors at the mouse neuromuscular junction depends on the activity of acetylcholinesterase. Minic, J., Molgó, J., Karlsson, E., Krejci, E. Eur. J. Neurosci. (2002) [Pubmed]
  16. Dendritic cells presenting pyruvate kinase M1/M2 isozyme peptide can induce experimental allergic myositis in BALB/c mice. Kawachi, I., Tanaka, K., Tanaka, M., Tsuji, S. J. Neuroimmunol. (2001) [Pubmed]
  17. Prediction of drug-induced catalepsy based on dopamine D1, D2, and muscarinic acetylcholine receptor occupancies. Haraguchi, K., Ito, K., Kotaki, H., Sawada, Y., Iga, T. Drug Metab. Dispos. (1997) [Pubmed]
  18. Membrane Ig cross-linking regulates phosphatidylinositol 3-kinase in B lymphocytes. Gold, M.R., Chan, V.W., Turck, C.W., DeFranco, A.L. J. Immunol. (1992) [Pubmed]
  19. Disruption of the murine gammaherpesvirus 68 M1 open reading frame leads to enhanced reactivation from latency. Clambey, E.T., Virgin, H.W., Speck, S.H. J. Virol. (2000) [Pubmed]
  20. Role of muscarinic receptor subtypes in the constriction of peripheral airways: studies on receptor-deficient mice. Struckmann, N., Schwering, S., Wiegand, S., Gschnell, A., Yamada, M., Kummer, W., Wess, J., Haberberger, R.V. Mol. Pharmacol. (2003) [Pubmed]
  21. Novel alkoxy-oxazolyl-tetrahydropyridine muscarinic cholinergic receptor antagonists. Shannon, H.E., Bymaster, F.P., Hendrix, J.C., Quimby, S.J., Mitch, C.H. Psychopharmacology (Berl.) (1995) [Pubmed]
  22. Role of specific muscarinic receptor subtypes in cholinergic parasympathomimetic responses, in vivo phosphoinositide hydrolysis, and pilocarpine-induced seizure activity. Bymaster, F.P., Carter, P.A., Yamada, M., Gomeza, J., Wess, J., Hamilton, S.E., Nathanson, N.M., McKinzie, D.L., Felder, C.C. Eur. J. Neurosci. (2003) [Pubmed]
  23. Presynaptic muscarinic acetylcholine receptors suppress GABAergic synaptic transmission in the intermediate grey layer of mouse superior colliculus. Li, F., Endo, T., Isa, T. Eur. J. Neurosci. (2004) [Pubmed]
  24. Cholinergic stimulation of salivary secretion studied with M1 and M3 muscarinic receptor single- and double-knockout mice. Gautam, D., Heard, T.S., Cui, Y., Miller, G., Bloodworth, L., Wess, J. Mol. Pharmacol. (2004) [Pubmed]
  25. M1 receptor agonist activity is not a requirement for muscarinic antinociception. Sheardown, M.J., Shannon, H.E., Swedberg, M.D., Suzdak, P.D., Bymaster, F.P., Olesen, P.H., Mitch, C.H., Ward, J.S., Sauerberg, P. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  26. Cholinergic agonist-induced pepsinogen secretion from murine gastric chief cells is mediated by M1 and M3 muscarinic receptors. Xie, G., Drachenberg, C., Yamada, M., Wess, J., Raufman, J.P. Am. J. Physiol. Gastrointest. Liver Physiol. (2005) [Pubmed]
  27. Specific Gq protein involvement in muscarinic M3 receptor-induced phosphatidylinositol hydrolysis and Ca2+ release in mouse duodenal myocytes. Morel, J.L., Macrez, N., Mironneau, J. Br. J. Pharmacol. (1997) [Pubmed]
  28. Intrathecal alpha2 adrenoceptor agonist clonidine inhibits mechanical transmission in mouse spinal cord via activation of muscarinic M1 receptors. Honda, K., Koga, K., Moriyama, T., Koguchi, M., Takano, Y., Kamiya, H.O. Neurosci. Lett. (2002) [Pubmed]
  29. Role of G proteins in mouse egg activation: stimulatory effects of acetylcholine on the ZP2 to ZP2f conversion and pronuclear formation in eggs expressing a functional m1 muscarinic receptor. Williams, C.J., Schultz, R.M., Kopf, G.S. Dev. Biol. (1992) [Pubmed]
  30. Muscarinic receptors participation in angiogenic response induced by macrophages from mammary adenocarcinoma-bearing mice. de la Torre, E., Davel, L., Jasnis, M.A., Gotoh, T., de Lustig, E.S., Sales, M.E. Breast Cancer Res. (2005) [Pubmed]
  31. Isolation, sequence, and functional expression of the mouse M1 muscarinic acetylcholine receptor gene. Shapiro, R.A., Scherer, N.M., Habecker, B.A., Subers, E.M., Nathanson, N.M. J. Biol. Chem. (1988) [Pubmed]
  32. M1 muscarinic acetylcholine receptors activate extracellular signal-regulated kinase in CA1 pyramidal neurons in mouse hippocampal slices. Berkeley, J.L., Gomeza, J., Wess, J., Hamilton, S.E., Nathanson, N.M., Levey, A.I. Mol. Cell. Neurosci. (2001) [Pubmed]
  33. Elucidating the role of muscarinic receptors in psychosis. Felder, C.C., Porter, A.C., Skillman, T.L., Zhang, L., Bymaster, F.P., Nathanson, N.M., Hamilton, S.E., Gomeza, J., Wess, J., McKinzie, D.L. Life Sci. (2001) [Pubmed]
  34. A region of the muscarinic-gated atrial K+ channel critical for activation by G protein beta gamma subunits. Takao, K., Yoshii, M., Kanda, A., Kokubun, S., Nukada, T. Neuron (1994) [Pubmed]
  35. Quantitative analysis of binding parameters of [3H]N-methylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice. Oki, T., Takagi, Y., Inagaki, S., Taketo, M.M., Manabe, T., Matsui, M., Yamada, S. Brain Res. Mol. Brain Res. (2005) [Pubmed]
  36. Regulation of muscarinic acetylcholine receptor function in acetylcholinesterase knockout mice. Li, B., Duysen, E.G., Volpicelli-Daley, L.A., Levey, A.I., Lockridge, O. Pharmacol. Biochem. Behav. (2003) [Pubmed]
  37. The effects of some porphyrinogenic drugs on the brain cholinergic system. Rodriguez, J.A., Buzaleh, A.M., Fossati, M., Azcurra, J., Batlle, A.M. Cell. Mol. Biol. (Noisy-le-grand) (2002) [Pubmed]
  38. Dopaminergic and cholinergic interaction in cataleptic responses in mice. Ushijima, I., Kawano, M., Kaneyuki, H., Suetsugi, M., Usami, K., Hirano, H., Mizuki, Y., Yamada, M. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  39. Synthesis of new cardioselective M2 muscarinic receptor antagonists. Mandelli, G.R., Maiorana, S., Terni, P., Lamperti, G., Colibretti, M.L., Imbimbo, B.P. Chem. Pharm. Bull. (2000) [Pubmed]
  40. Disruption of the m1 receptor gene ablates muscarinic receptor-dependent M current regulation and seizure activity in mice. Hamilton, S.E., Loose, M.D., Qi, M., Levey, A.I., Hille, B., McKnight, G.S., Idzerda, R.L., Nathanson, N.M. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  41. Activation of protein kinase C induces rapid internalization and subsequent degradation of muscarinic acetylcholine receptors in neuroblastoma cells. Liles, W.C., Hunter, D.D., Meier, K.E., Nathanson, N.M. J. Biol. Chem. (1986) [Pubmed]
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