muscarinic M3 receptor; muscarinic acetylcholine receptor M3 (CHRM3)
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Function
- activates Gq proteins
- stimulates phosphoinositide hydrolysis & Ca+2 mobilization
- involved in pancreatic endocrine & exocrine secretion[1]
- involved in bladder smooth muscle contraction[4][6]
Structure
belongs to the G-protein coupled receptor 1 family
Compartment
Expression
- expressed in smooth muscle, GI tract, urinary bladder, myocardium[5][6]
Pharmacology
- muscarinic M3 receptor specific antagonists (solifenacin & darifenacin) have been developed to specifically antagonize detrussor hyperactivity associated with urge incontinence
More general terms
References
- ↑ 1.0 1.1 Conkilin et al PNAS 85:8698 (1988)
- ↑ Entrez Gene http://www.ncbi.nlm.nih.gov/sites/entrez?db=gene&cmd=Retrieve&dopt=Graphics&list_uids=1131
- ↑ Mukerji G et al, Localization of M2 and M3 muscarininc receptors in human bladder disorders and their clinical correlations. J Urol. 2006, 176:367 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16753445
- ↑ 4.0 4.1 Gromada J & Hughes TE Ringing the dinner bell for insulin: muscarinic M3 receptor activity in the control of pancreatic beta cell function. Cell Metab. 2006, 3:390 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16753574
- ↑ 5.0 5.1 Wang Z et al Functional M3 muscarinic acetylcholine receptors in mammalian hearts Br J Pharmacol 2004, 142:395 PMID: https://www.ncbi.nlm.nih.gov/pubmed/15148264
- ↑ 6.0 6.1 6.2 Ehlert FJ Pharmacologic analysis of the contractile role of M2 and M3 muscarinic receptors in smooth muscle. Receptors Channels 2003, 9:261 PMID: https://www.ncbi.nlm.nih.gov/pubmed/12893538
- ↑ Kruse AC et al Structure and dynamics of the M3 muscarinic acetylcholine receptor. Nature. 2012 Feb 22;482(7386):552-6. doi:http://dx.doi.org/ 10.1038/nature10867. PMID: https://www.ncbi.nlm.nih.gov/pubmed/22358844