Muscarinic acetylcholine receptor M1

From Self-sufficiency
Jump to: navigation, search
edit
Cholinergic receptor, muscarinic 1
Identifiers
SymbolsCHRM1; HM1; M1; MGC30125
External IDsOMIM118510 MGI88396 HomoloGene20189 IUPHAR: M1 GeneCards: CHRM1 Gene
Orthologs
SpeciesHumanMouse
Entrez112812669
EnsemblENSG00000168539ENSMUSG00000032773
UniProtP11229Q52KQ0
RefSeq (mRNA)NM_000738NM_007698
RefSeq (protein)NP_000729NP_031724
Location (UCSC)Chr 11:
62.43 - 62.45 Mb
Chr 19:
8.73 - 8.75 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] 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

Mechanism

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

Ligands

Agonists

Allosteric modulators

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

Antagonists

Gene

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

See also

References

Cite error: Invalid <references> tag; parameter "group" is allowed only.

Use <references />, or <references group="..." />

External links

Further reading

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


es:Receptor muscarínico M1
  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 1217289Freely accessible. PMID 8645172. 
  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). "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 1190137Freely accessible. PMID 1693682. 
  8. Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  9. 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 2684909Freely accessible. PMID 19047481.