Muscarinic acetylcholine receptor M1
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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] is common in exocrine glands and in the CNS.[2][3]
It is predominantly found bound to G proteins of class Gq[4] which 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, Gi (causing a downstream decrease in cAMP) and Gs (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.
Contents
Effects
- EPSP in autonomic ganglia
- secretion from salivary glands
- gastric acid secretion from stomach[5]
- In CNS (memory?) [6]
- vagally-induced bronchoconstriction[5]
Mechanism
It couples to Gq, and, to a small extent, Gi andGs. This results in slow EPSP and decreasedK+ conductance [6][7]
Ligands
Agonists
- acetylcholine
- carbachol[6]
- CDD-0097
- McN-A-343 - mixed M1/M4 agonist [6]
- L-689,660 - mixed M1/M3 agonist
- Oxotremorine
- Vedaclidine
- Xanomeline
- Muscarine
Allosteric modulators
Antagonists
- atropine[6]
- dicycloverine[6]
- tolterodine[6]
- oxybutynin[6]
- ipratropium[6]
- mamba toxin MT7[6]
- pirenzepine
- telenzepine
Gene
The receptor is encoded by human gene CHRM1.[5] It is localized to 11q13.[5]
See also
References
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<references />, or <references group="..." />External links
- "Acetylcholine receptors (muscarinic): M1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Further reading
- Goyal RK; Underhill, Lisa H.; Goyal, Raj K. (1989). "Muscarinic receptor subtypes. Physiology and clinical implications". N. Engl. J. Med. 321 (15): 1022–9. doi:10.1056/NEJM198910123211506. PMID 2674717.
- Brann MR, Ellis J, Jørgensen H; et al. (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 RM, Slack BE, Wurtman RJ, Growdon JH (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 JR, Nagata O, Shockley MS; et al. (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 JS, Novotny EA, Brann MR, Robbins KC (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 Freely accessible. PMID 1905013.
- Chapman CG, Browne MJ (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 Freely accessible. PMID 2336407.
- Ashkenazi A, Ramachandran J, Capon DJ (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 TI, Buckley NJ, Young AC, Brann MR (1987). "Identification of a family of muscarinic acetylcholine receptor genes". Science. 237 (4814): 527–32. doi:10.1126/science.3037705. PMID 3037705.
- Peralta EG, Ashkenazi A, Winslow JW; et al. (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 Freely accessible. PMID 3443095.
- Allard WJ, Sigal IS, Dixon RA (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 Freely accessible. 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 JL; et al. (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 GL (1994). "Acetylcholine muscarinic m1 receptor regulation of cyclic AMP synthesis controls growth factor stimulation of Raf activity". Mol. Cell. Biol. 14 (4): 2343–51. PMC 358601 Freely accessible. PMID 8139539.
- Offermanns S, Wieland T, Homann D; 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 FM, McCallum JF; et al. (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; 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. PMID 8938448.
- Ishiyama A, López I, Wackym PA (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; et al. (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.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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- ↑ Messer, Jr, WS (2000-01-20). "Acetylcholine". University of Toledo. Retrieved 2007-10-27.
- ↑ 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.
- ↑ Burford NT, Nahorski SR (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 Freely accessible. PMID 8645172.
- ↑ 5.0 5.1 5.2 5.3 "Entrez Gene: CHRM1 cholinergic receptor, muscarinic 1".
- ↑ 6.0 6.1 6.2 6.3 6.4 6.5 6.6 6.7 6.8 6.9 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 RA (1 March 1990). "Muscarine reduces inwardly rectifying potassium conductance in rat nucleus accumbens neurones". J. Physiol. (Lond.). 422 (1): 369–80. PMC 1190137 Freely accessible. PMID 1693682.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ 9.0 9.1 Marlo JE, Niswender CM, Days EL; et al. (2008). "Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity". Mol. Pharmacol. 75 (3): 577. doi:10.1124/mol.108.052886. PMC 2684909 Freely accessible. PMID 19047481.
