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The correct title of this article is Muscarinic acetylcholine receptor M1. It appears incorrectly here because of technical restrictions.



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.

Effects[edit | edit source]

Mechanism[edit | edit source]

It couples to Gq, and, to a small extent, Gi andGs. This results in slow EPSP and decreasedK+ conductance [6][7]

Ligands[edit | edit source]

Agonists[edit | edit source]

Allosteric modulators[edit | edit source]

Antagonists[edit | edit source]

Gene[edit | edit source]

The receptor is encoded by human gene CHRM1.[5] It is localized to 11q13.[5]

See also[edit | edit source]

References[edit | edit source]

  1. Messer, Jr, WS. Acetylcholine. University of Toledo. URL accessed on 2007-10-27.
  2. Johnson, Gordon (2002). PDQ Pharmacology, 2nd ed., 311 pages, Hamilton, Ontario: BC Decker Inc.
  3. Richelson, Elliott. Cholinergic Transduction, Psychopharmacology - The Fourth Generation of Progress. American College of Neuropsychopharmacology. URL accessed on 2007-10-27.
  4. 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.
  5. 5.0 5.1 5.2 5.3 Entrez Gene: CHRM1 cholinergic receptor, muscarinic 1.
  6. 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). "Ch. 10" Pharmacology, 5th edition, page 139, Elsevier Churchill Livingstone. ISBN 0-443-07145-4.
  7. PUBMED - Muscarine reduces inwardly rectifying potassium conductance in rat ...
  8. 8.0 8.1 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..

External links[edit | edit source]

Further reading[edit | edit source]

  • Goyal RK (1989). Muscarinic receptor subtypes. Physiology and clinical implications.. N. Engl. J. Med. 321 (15): 1022–9.
  • Brann MR, Ellis J, Jørgensen H, et al. (1994). Muscarinic acetylcholine receptor subtypes: localization and structure/function.. Prog. Brain Res. 98: 121–7.
  • 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.
  • 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.
  • 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.
  • Chapman CG, Browne MJ (1990). Isolation of the human ml (Hml) muscarinic acetylcholine receptor gene by PCR amplification.. Nucleic Acids Res. 18 (8): 2191.
  • 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.
  • Bonner TI, Buckley NJ, Young AC, Brann MR (1987). Identification of a family of muscarinic acetylcholine receptor genes.. Science 237 (4814): 527–32.
  • 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.
  • Allard WJ, Sigal IS, Dixon RA (1988). Sequence of the gene encoding the human M1 muscarinic acetylcholine receptor.. Nucleic Acids Res. 15 (24): 10604.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • Ishizaka N, Noda M, Yokoyama S, et al. (1998). Muscarinic acetylcholine receptor subtypes in the human iris.. Brain Res. 787 (2): 344–7.

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


es:Receptor muscarínico M1

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