M2受容体、M2レセプター

WordNet

a measure of the money supply; M1 plus net time deposits (other than large certificates of deposit)
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

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）』「2012/06/16 09:11:14」(JST)

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The muscarinic acetylcholine receptor M₂, also known as the cholinergic receptor, muscarinic 2, is a muscarinic acetylcholine receptor.

Function

Heart

The M2 muscarinic receptors are located in the heart, where they act to slow the heart rate down to normal sinus rhythm after stimulatory actions of the sympathetic nervous system, by slowing the speed of depolarization. They also reduce contractile forces of the atrial cardiac muscle, and reduce conduction velocity of the atrioventricular node (AV node). However, they have no effect on the contractile forces of the ventricular muscle.

IQ

A 2006 Dutch family study found that there is "a highly significant association" between the CHRM2 gene and intelligence. The study concluded that there was an association between the CHRM2 gene on chromosome 7 and Performance IQ, as measured by the Wechsler Adult Intelligence Scale-Revised. The Dutch family study used a sample of 667 individuals from 304 families.^[2] A similar association was found independently in the Minnesota Twin and Family Study (Comings et al. 2003) and by the Department of Psychiatry at the Washington University.^[3] However, a larger 2009 study attempting to replicate this claim instead found no significant association between the CHRM2 gene and intelligence in a Scottish cohort of 2,091 individuals over age 50, nor an English sample of 758 non-cognitively-impaired elderly individuals, nor an Australian family-based sample of 1,537 adolescents.^[4]

Mechanism

M2 muscarinic receptors act via a G_i type receptor, which causes a decrease in cAMP in the cell, generally leading to inhibitory-type effects.

In addition, they modulate muscarinic potassium channels.^[5]^[6] In the heart, this contributes to a decreased heart rate.

Gene

Muscarinic acetylcholine receptor M2 is encoded by the gene CHRM2.^[7]

Multiple alternatively spliced transcript variants have been described for this gene.^[7]

Ligands

Few highly selective M2 agonists are available at present, although there are several non-selective muscarinic agonists that stimulate M2, and a number of selective M2 antagonists are available.

Agonists

Bethanechol (nonselective muscarinic agonist)
(2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide (selective for M2 but only partial agonist)^[8]

Antagonists

Dimethindene - N,N-Dimethyl-3-[(1S)-1-(2-pyridinyl)ethyl]-1H-indene-2-ethanamine, CAS# 121367-05-3, mixed M2 / histamine H1 antagonist
Otenzepad - 11-([2-[(Diethylamino)methyl]-1-piperidinyl]acetyl)-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, CAS# 102394-31-0
AQRA-741 - 11-([4-[4-(Diethylamino)butyl]-1-piperidinyl]acetyl)-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, CAS# 123548-16-3
AFDX-384 (mixed M2/M4 antagonist) - N-[2-[2-[(Dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide, CAS# 118290-27-0

References

^ Haga, K.; Kruse, A. C.; Asada, H.; Yurugi-Kobayashi, T.; Shiroishi, M.; Zhang, C.; Weis, W. I.; Okada, T. et al. (2012). "Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist". Nature 482 (7386): 547–551. DOI:10.1038/NATURE10753. PMID 22278061. edit
^ Gosso MF, van Belzen M, de Geus EJ, et al. (2006). "Association between the CHRM2 gene and intelligence in a sample of 304 Dutch families". Genes, Brain and Behavior 5 (8): 577–584. DOI:10.1111/j.1601-183X.2006.00211.x. PMID 17081262.
^ Dick DM, Aliev F, Kramer J, et al. (2007). "Association of CHRM2 with IQ: converging evidence for a gene influencing intelligence". Behav. Genet. 37 (2): 265–272. DOI:10.1007/s10519-006-9131-2. PMID 17160701.
^ Lind PA, Luciano M, Horan MA, et al. (September 2009). "No association between Cholinergic Muscarinic Receptor 2 (CHRM2) genetic variation and cognitive abilities in three independent samples". Behav. Genet. 39 (5): 513–23. DOI:10.1007/s10519-009-9274-z. PMID 19418213.
^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
^ Boron, W. F and Boulpaep, E. L. (2005). Medical Physiology. Philadelphia: Elsevier Saunders. pp. 387. ISBN 1-4160-2328-3.
^ ^a ^b "Entrez Gene: CHRM2 cholinergic receptor, muscarinic 2". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1129.
^ Scapecchi S, Matucci R, Bellucci C, Buccioni M, Dei S, Guandalini L, Martelli C, Manetti D, Martini E, Marucci G, Nesi M, Romanelli MN, Teodori E, Gualtieri F (March 2006). "Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist". J. Med. Chem. 49 (6): 1925–31. DOI:10.1021/jm0510878. PMID 16539379.

External links

"Acetylcholine receptors (muscarinic): M₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2141.

CHRM2+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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「M2受容体」

Cholinergic receptor, muscarinic 2
	; Human M2 muscarinic acetylcholine receptor/lysozyme fusion protein. PDB 3uon
Available structures
PDB	Ortholog search: PDBe, RCSB
List of PDB id codes
	3UON
Identifiers
Symbols	CHRM2; HM2
External IDs	OMIM: 118493 MGI: 88397 HomoloGene: 20190 IUPHAR: M2 ChEMBL: 211 GeneCards: CHRM2 Gene
Gene Ontology
Molecular function	• signal transducer activity; • receptor activity; • G-protein coupled receptor activity; • drug binding; • G-protein coupled acetylcholine receptor activity;
Cellular component	• membrane fraction; • plasma membrane; • plasma membrane; • integral to plasma membrane; • cell junction; • dendrite; • asymmetric synapse; • symmetric synapse; • neuronal cell body; • axon terminus; • postsynaptic membrane;
Biological process	• regulation of smooth muscle contraction; • G-protein coupled receptor signaling pathway; • G-protein signaling, coupled to cyclic nucleotide second messenger; • G-protein signaling, coupled to cAMP nucleotide second messenger; • activation of phospholipase C activity by G-protein coupled acetylcholine receptor signaling pathway; • synaptic transmission; • nervous system development; • regulation of heart contraction; • response to virus;
	Sources: Amigo / QuickGO
Orthologs
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