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a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
the 13th letter of the Roman alphabet (同)m
the imperial dynasty of China from 1368 to 1644 (同)Ming dynasty
a measure of the money supply; includes currency in circulation plus demand deposits or checking account balances

PrepTutorEJDIC

=sense organ / 受信装置
Mach number / mark[s] / Monsieur
(中国の)明,明朝(1368‐1644)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/03/16 03:21:10」(JST)

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The muscarinic acetylcholine receptor M₁, also known as the cholinergic receptor, muscarinic 1, is a muscarinic receptor.

This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve,^[1]^{[dead link]} is common in exocrine glands and in the CNS.^[2]^[3]

It is predominantly found bound to G proteins of class G_q^[4]^[5] that use upregulation of phospholipase C and, therefore, inositol trisphosphate and intracellular calcium as a signalling pathway. A receptor so bound would not be susceptible to CTX or PTX. However, G_i (causing a downstream decrease in cAMP) and G_s (causing an increase in cAMP) have also been shown to be involved in interactions in certain tissues, and so would be susceptible to PTX and CTX respectively.

§Effects

EPSP in autonomic ganglia^{[citation needed]}
Secretion from salivary glands
Gastric acid secretion from stomach^[6]
In CNS (memory?)^[7]
Vagally-induced bronchoconstriction^[6]

§Mechanism

It couples to G_q, and, to a small extent, G_i and G_s. This results in slow EPSP and decreased K⁺ conductance^[7]^[8] It is preassembled to the Gq heterotrimer through a polybasic c-terminal domain.^[4]

§Ligands

§Agonists

acetylcholine
carbachol^[7]
CDD-0097
Cevimeline
McN-A-343 - mixed M1/M4 agonist^[7]
L-689,660 - mixed M1/M3 agonist
Oxotremorine
Vedaclidine
Xanomeline
Muscarine
77-LH-28-1 - brain penetrant selective M₁ allosteric agonist

§Allosteric modulators

benzylquinolone carboxylic acid^[9]
VU-0090157^[10]
VU-0029767^[10]

§Antagonists

atropine^[7]
Hyoscyamine^[11]
dicycloverine^[7]
tolterodine^[7]
oxybutynin^[7]
ipratropium^[7]
mamba toxin muscarinic toxin 7 (MT7)^[7]
olanzapine
pirenzepine
telenzepine

§Gene

The receptor is encoded by human gene CHRM1.^[6] It is localized to 11q13.^[6]

§See also

Muscarinic acetylcholine receptor

§References

^ Messer, Jr, WS (2000-01-20). "Acetylcholine". University of Toledo. Retrieved 2007-10-27. ^{[dead link]}
^ Johnson, Gordon (2002). PDQ Pharmacology (2nd ed.). Hamilton, Ontario: BC Decker Inc. pp. 311 pages. ISBN 1-55009-109-3.
^ Richelson, Elliott (2000). "Cholinergic Transduction, Psychopharmacology - The Fourth Generation of Progress". American College of Neuropsychopharmacology. Retrieved 2007-10-27.
^ ^a ^b Qin K, Dong C, Wu G, Lambert N (August 2011). "Inactive-state preassembly of Gq-coupled receptors and Gq heterotrimers". Nature Chemical Biology 7 (11): 740–747. doi:10.1038/nchembio.642. PMC 3177959. PMID 21873996.
^ Burford N, Nahorski S (1996). "Muscarinic m1 receptor-stimulated adenylate cyclase activity in Chinese hamster ovary cells is mediated by Gs alpha and is not a consequence of phosphoinositidase C activation". Biochem. J. 315 (Pt 3): 883–8. PMC 1217289. PMID 8645172.
^ ^a ^b ^c ^d "Entrez Gene: CHRM1 cholinergic receptor, muscarinic 1".
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j Rang HP, Dale MM, Ritter JM, Moore PK (2003). "10". Pharmacology (5th ed.). Elsevier Churchill Livingstone. p. 139. ISBN 0-443-07145-4.
^ Uchimura N, North R (1 March 1990). "Muscarine reduces inwardly rectifying potassium conductance in rat nucleus accumbens neurones". J. Physiol. (Lond.) 422 (1): 369–80. PMC 1190137. PMID 1693682.
^ Shirey J, Brady A, Jones P, Davis A, Bridges T, Kennedy J et al. (November 2009). "A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning". J. Neurosci. 29 (45): 14271–86. doi:10.1523/JNEUROSCI.3930-09.2009. PMC 2811323. PMID 19906975.
^ ^a ^b Marlo J, Niswender C, Days E, Bridges T, Xiang Y, Rodriguez A et al. (2008). "Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity". Mol. Pharmacol. 75 (3): 577–88. doi:10.1124/mol.108.052886. PMC 2684909. PMID 19047481.
^ Edwards Pharmaceuticals, Inc.; Belcher Pharmaceuticals, Inc. (May 2010), DailyMed, U.S. National Library of Medicine, retrieved January 13, 2013

§Further reading

Goyal R (1989). "Muscarinic receptor subtypes. Physiology and clinical implications.". N. Engl. J. Med. 321 (15): 1022–9. doi:10.1056/NEJM198910123211506. PMID 2674717.
Brann M, Ellis J, Jørgensen H, Hill-Eubanks D, Jones S (1994). "Muscarinic acetylcholine receptor subtypes: localization and structure/function.". Prog. Brain Res. 98: 121–7. doi:10.1016/S0079-6123(08)62388-2. PMID 8248499.
Nitsch R, Slack B, Wurtman R, Growdon J (1992). "Release of Alzheimer amyloid precursor derivatives stimulated by activation of muscarinic acetylcholine receptors.". Science 258 (5080): 304–7. doi:10.1126/science.1411529. PMID 1411529.
Arden J, Nagata O, Shockley M, Philip M, Lameh J, Sadée W (1992). "Mutational analysis of third cytoplasmic loop domains in G-protein coupling of the HM1 muscarinic receptor.". Biochem. Biophys. Res. Commun. 188 (3): 1111–5. doi:10.1016/0006-291X(92)91346-R. PMID 1445347.
Gutkind J, Novotny E, Brann M, Robbins K (1991). "Muscarinic acetylcholine receptor subtypes as agonist-dependent oncogenes.". Proc. Natl. Acad. Sci. U.S.A. 88 (11): 4703–7. doi:10.1073/pnas.88.11.4703. PMC 51734. PMID 1905013.
Chapman C, Browne M (1990). "Isolation of the human ml (Hml) muscarinic acetylcholine receptor gene by PCR amplification.". Nucleic Acids Res. 18 (8): 2191. doi:10.1093/nar/18.8.2191. PMC 330717. PMID 2336407.
Ashkenazi A, Ramachandran J, Capon D (1989). "Acetylcholine analogue stimulates DNA synthesis in brain-derived cells via specific muscarinic receptor subtypes.". Nature 340 (6229): 146–50. doi:10.1038/340146a0. PMID 2739737.
Bonner T, Buckley N, Young A, Brann M (1987). "Identification of a family of muscarinic acetylcholine receptor genes.". Science 237 (4814): 527–32. doi:10.1126/science.3037705. PMID 3037705.
Peralta E, Ashkenazi A, Winslow J, Smith D, Ramachandran J, Capon D (1988). "Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors.". EMBO J. 6 (13): 3923–9. PMC 553870. PMID 3443095.
Allard W, Sigal I, Dixon R (1988). "Sequence of the gene encoding the human M1 muscarinic acetylcholine receptor.". Nucleic Acids Res. 15 (24): 10604. doi:10.1093/nar/15.24.10604. PMC 339984. PMID 3697105.
Svoboda P, Milligan G (1994). "Agonist-induced transfer of the alpha subunits of the guanine-nucleotide-binding regulatory proteins Gq and G11 and of muscarinic m1 acetylcholine receptors from plasma membranes to a light-vesicular membrane fraction.". Eur. J. Biochem. 224 (2): 455–62. doi:10.1111/j.1432-1033.1994.00455.x. PMID 7925360.
Crespo P, Xu N, Daniotti J, Troppmair J, Rapp U, Gutkind J (1994). "Signaling through transforming G protein-coupled receptors in NIH 3T3 cells involves c-Raf activation. Evidence for a protein kinase C-independent pathway.". J. Biol. Chem. 269 (33): 21103–9. PMID 8063729.
Russell M, Winitz S, Johnson G (1994). "Acetylcholine muscarinic m1 receptor regulation of cyclic AMP synthesis controls growth factor stimulation of Raf activity.". Mol. Cell. Biol. 14 (4): 2343–51. doi:10.1128/mcb.14.4.2343. PMC 358601. PMID 8139539.
Offermanns S, Wieland T, Homann D, Sandmann J, Bombien E, Spicher K et al. (1994). "Transfected muscarinic acetylcholine receptors selectively couple to Gi-type G proteins and Gq/11.". Mol. Pharmacol. 45 (5): 890–8. PMID 8190105.
Mullaney I, Mitchell F, McCallum J, Buckley N, Milligan G (1993). "The human muscarinic M1 acetylcholine receptor, when express in CHO cells, activates and downregulates both Gq alpha and G11 alpha equally and non-selectively.". FEBS Lett. 324 (2): 241–5. doi:10.1016/0014-5793(93)81401-K. PMID 8508928.
Courseaux A, Grosgeorge J, Gaudray P, Pannett A, Forbes S, Williamson C et al. (1997). "Definition of the minimal MEN1 candidate area based on a 5-Mb integrated map of proximal 11q13. The European Consortium on Men1, (GENEM 1; Groupe d'Etude des Néoplasies Endocriniennes Multiples de type 1).". Genomics 37 (3): 354–65. doi:10.1006/geno.1996.0570. PMID 8938448.
Ishiyama A, López I, Wackym P (1998). "Molecular characterization of muscarinic receptors in the human vestibular periphery. Implications for pharmacotherapy.". The American journal of otology 18 (5): 648–54. PMID 9303164.
Ishizaka N, Noda M, Yokoyama S, Kawasaki K, Yamamoto M, Higashida H (1998). "Muscarinic acetylcholine receptor subtypes in the human iris.". Brain Res. 787 (2): 344–7. doi:10.1016/S0006-8993(97)01554-0. PMID 9518684.

§External links

"Acetylcholine receptors (muscarinic): M₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

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「M1受容体」

Cholinergic receptor, muscarinic 1
Identifiers
Symbols	CHRM1 ; HM1; M1; M1R
External IDs	OMIM: 118510 MGI: 88396 HomoloGene: 20189 IUPHAR: M1 ChEMBL: 216 GeneCards: CHRM1 Gene
Gene ontology
Molecular function	• phosphatidylinositol phospholipase C activity; • drug binding; • G-protein coupled acetylcholine receptor activity;
Cellular component	• plasma membrane; • integral component of plasma membrane; • postsynaptic density; • membrane; • cell junction; • dendrite; • asymmetric synapse; • axon terminus; • postsynaptic membrane;
Biological process	• cellular protein modification process; • signal transduction; • G-protein coupled receptor signaling pathway; • protein kinase C-activating G-protein coupled receptor signaling pathway; • phospholipase C-activating G-protein coupled acetylcholine receptor signaling pathway; • G-protein coupled acetylcholine receptor signaling pathway; • neuromuscular synaptic transmission; • nervous system development; • cell proliferation; • positive regulation of cell proliferation; • regulation of locomotion; • positive regulation of ion transport; • saliva secretion; • cognition; • positive regulation of intracellular protein transport;
	Sources: Amigo / QuickGO
Orthologs
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