Muscarinic acetylcholine receptor M1

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Cholinergic receptor, muscarinic 1
Identifiers
Symbols CHRM1 ; HM1; M1; M1R
External IDs OMIM118510 MGI88396 HomoloGene20189 IUPHAR: M1 ChEMBL: 216 GeneCards: CHRM1 Gene
Orthologs
Species Human Mouse
Entrez 1128 12669
Ensembl ENSG00000168539 ENSMUSG00000032773
UniProt P11229 P12657
RefSeq (mRNA) NM_000738 NM_001112697
RefSeq (protein) NP_000729 NP_001106167
Location (UCSC) Chr 11:
62.68 – 62.69 Mb
Chr 19:
8.66 – 8.68 Mb
PubMed search [1] [2]

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] 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.

Effects[edit]

Mechanism[edit]

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

Ligands[edit]

Agonists[edit]

Allosteric modulators[edit]

  • benzylquinolone carboxylic acid[8]
  • VU-0090157[9]
  • VU-0029767[9]

Antagonists[edit]

Gene[edit]

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

See also[edit]

References[edit]

  1. ^ Messer, Jr, WS (2000-01-20). "Acetylcholine". University of Toledo. Retrieved 2007-10-27. 
  2. ^ Johnson, Gordon (2002). PDQ Pharmacology (2nd ed.). Hamilton, Ontario: BC Decker Inc. pp. 311 pages. ISBN 1-55009-109-3. 
  3. ^ Richelson, Elliott (2000). "Cholinergic Transduction, Psychopharmacology - The Fourth Generation of Progress". American College of Neuropsychopharmacology. Retrieved 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. PMC 1217289. PMID 8645172. 
  5. ^ a b c d "Entrez Gene: CHRM1 cholinergic receptor, muscarinic 1". 
  6. ^ a b c d e f g h i j Rang HP, Dale MM, Ritter JM, Moore PK (2003). "10". Pharmacology (5th ed.). Elsevier Churchill Livingstone. p. 139. ISBN 0-443-07145-4. 
  7. ^ 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. PMID 1693682. 
  8. ^ Shirey JK, Brady AE, Jones PJ, Davis AA, Bridges TM, Kennedy JP, Jadhav SB, Menon UN, Xiang Z, Watson ML, Christian EP, Doherty JJ, Quirk MC, Snyder DH, Lah JJ, Levey AI, Nicolle MM, Lindsley CW, Conn PJ (November 2009). "A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning". J. Neurosci. 29 (45): 14271–86. doi:10.1523/JNEUROSCI.3930-09.2009. PMC 2811323. PMID 19906975. 
  9. ^ a b 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): 577–88. doi:10.1124/mol.108.052886. PMC 2684909. PMID 19047481. 
  10. ^ Edwards Pharmaceuticals, Inc.; Belcher Pharmaceuticals, Inc. (May 2010), DailyMed, U.S. National Library of Medicine, retrieved January 13, 2013 

External links[edit]

Further reading[edit]

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