The muscarinic acetylcholine receptor M1, also known as the cholinergic receptor, muscarinic 1, is a muscarinic receptor that in humans is encoded by the CHRM1gene.[1] It is localized to 11q13.[1]
This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve,[2] is common in exocrine glands and in the CNS.[3][4]
It is predominantly found bound to G proteins of class Gq[5][6] 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, 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.
In search of evolutionary origins of cholinergic system and muscarinic receptors in eukaryotes, a structural homolog of M1 receptor has been reported in Acanthamoeba castellanii.[9] and Naegleria fowleri.[10] The receptor antagonists of M1 receptors have shown to be exert anti-proliferative effects on these amoebae.
It couples to Gq, and, to a small extent, Gi and Gs. This results in slow EPSP and decreased K+ conductance.[7][11] It is preassembled to the Gq heterotrimer through a polybasic c-terminal domain.[5]
↑Messer WS (2000-01-20). "Acetylcholine". University of Toledo. Archived from the original on 14 October 2007. Retrieved 2007-10-27.
↑Johnson G (2002). PDQ Pharmacology (2nd ed.). Hamilton, Ontario: BC Decker Inc. pp. 311 pages. ISBN1-55009-109-3.
↑Richelson E (1995). "Cholinergic Transduction". In Bloom FE, Kupfer DJ. Psychopharmacology: the fourth generation of progress: an official publication of the American College of Neuropsychopharmacology (Fourth ed.). New York: Lippincott Williams & Wilkins. ISBN978-0781701662. Retrieved 2007-10-27.
↑Edwards Pharmaceuticals, Inc.; Belcher Pharmaceuticals, Inc. (May 2010). "DailyMed". U.S. National Library of Medicine. Retrieved January 13, 2013.
↑Eltze M, Figala V (December 1988). "Affinity and selectivity of biperiden enantiomers for muscarinic receptor subtypes". European Journal of Pharmacology. 158 (1–2): 11–9. PMID3220113.
Goyal RK (October 1989). "Muscarinic receptor subtypes. Physiology and clinical implications". The New England Journal of Medicine. 321 (15): 1022–9. doi:10.1056/NEJM198910123211506. PMID2674717.
Brann MR, Ellis J, Jørgensen H, Hill-Eubanks D, Jones SV (1994). "Muscarinic acetylcholine receptor subtypes: localization and structure/function". Progress in Brain Research. 98: 121–7. doi:10.1016/S0079-6123(08)62388-2. PMID8248499.
Nitsch RM, Slack BE, Wurtman RJ, Growdon JH (October 1992). "Release of Alzheimer amyloid precursor derivatives stimulated by activation of muscarinic acetylcholine receptors". Science. 258 (5080): 304–7. doi:10.1126/science.1411529. PMID1411529.
Arden JR, Nagata O, Shockley MS, Philip M, Lameh J, Sadée W (November 1992). "Mutational analysis of third cytoplasmic loop domains in G-protein coupling of the HM1 muscarinic receptor". Biochemical and Biophysical Research Communications. 188 (3): 1111–5. doi:10.1016/0006-291X(92)91346-R. PMID1445347.
Ashkenazi A, Ramachandran J, Capon DJ (July 1989). "Acetylcholine analogue stimulates DNA synthesis in brain-derived cells via specific muscarinic receptor subtypes". Nature. 340 (6229): 146–50. doi:10.1038/340146a0. PMID2739737.
Bonner TI, Buckley NJ, Young AC, Brann MR (July 1987). "Identification of a family of muscarinic acetylcholine receptor genes". Science. 237 (4814): 527–32. doi:10.1126/science.3037705. PMID3037705.
Svoboda P, Milligan G (September 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". European Journal of Biochemistry. 224 (2): 455–62. doi:10.1111/j.1432-1033.1994.00455.x. PMID7925360.
Crespo P, Xu N, Daniotti JL, Troppmair J, Rapp UR, Gutkind JS (August 1994). "Signaling through transforming G protein-coupled receptors in NIH 3T3 cells involves c-Raf activation. Evidence for a protein kinase C-independent pathway". The Journal of Biological Chemistry. 269 (33): 21103–9. PMID8063729.
Offermanns S, Wieland T, Homann D, Sandmann J, Bombien E, Spicher K, Schultz G, Jakobs KH (May 1994). "Transfected muscarinic acetylcholine receptors selectively couple to Gi-type G proteins and Gq/11". Molecular Pharmacology. 45 (5): 890–8. PMID8190105.
Mullaney I, Mitchell FM, McCallum JF, Buckley NJ, Milligan G (June 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 Letters. 324 (2): 241–5. doi:10.1016/0014-5793(93)81401-K. PMID8508928.
Courseaux A, Grosgeorge J, Gaudray P, Pannett AA, Forbes SA, Williamson C, Bassett D, Thakker RV, Teh BT, Farnebo F, Shepherd J, Skogseid B, Larsson C, Giraud S, Zhang CX, Salandre J, Calender A (November 1996). "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. PMID8938448.
Ishiyama A, López I, Wackym PA (September 1997). "Molecular characterization of muscarinic receptors in the human vestibular periphery. Implications for pharmacotherapy". The American Journal of Otology. 18 (5): 648–54. PMID9303164.
Ishizaka N, Noda M, Yokoyama S, Kawasaki K, Yamamoto M, Higashida H (March 1998). "Muscarinic acetylcholine receptor subtypes in the human iris". Brain Research. 787 (2): 344–7. doi:10.1016/S0006-8993(97)01554-0. PMID9518684.
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