Muscarinic acetylcholine receptor M1

Protein-coding gene in the species Homo sapiens From Wikipedia, the free encyclopedia

Muscarinic acetylcholine receptor M1

The muscarinic acetylcholine receptor M1, also known as the cholinergic receptor, muscarinic 1, is a muscarinic receptor that in humans is encoded by the CHRM1 gene.[5] It is localized to 11q13.[5]

Quick Facts CHRM1, Available structures ...
CHRM1
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesCHRM1, HM1, M1, M1R, cholinergic receptor muscarinic 1
External IDsOMIM: 118510; MGI: 88396; HomoloGene: 20189; GeneCards: CHRM1; OMA:CHRM1 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_000738

NM_001112697
NM_007698

RefSeq (protein)

NP_000729

NP_001106167
NP_031724

Location (UCSC)Chr 11: 62.91 – 62.92 MbChr 19: 8.64 – 8.66 Mb
PubMed search[3][4]
Wikidata
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This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve,[6] is common in exocrine glands and in the CNS.[7][8]

It is predominantly found bound to G proteins of class Gq[9][10] 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

Occurrence in free living amoebae

A structural but not sequential homolog of the human M1 receptor has been reported in Acanthamoeba castellanii[15] and Naegleria fowleri.[16] Antagonists of human M1 receptors (e.g. atropine, diphenhydramine) have been shown to exert anti-proliferative effects on these pathogens.

Mechanism

It couples to Gq, and, to a small extent, Gi and Gs. This results in slow EPSP and decreased K+ conductance.[12][17] It is preassembled to the Gq heterotrimer through a polybasic c-terminal domain.[9]

Ligands

Agonists

Allosteric modulators

  • benzylquinolone carboxylic acid[19]
  • BQZ-12[20]
  • VU-0090157[21]
  • VU-0029767[21]
  • VU0467319[22]
  • [3H]PT-1284- M1-selective PAM Radioligand[23]

Antagonists

See also

References

Further reading

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