Muscarinic acetylcholine receptor M1
Lua error in Module:Infobox_gene at line 33: attempt to index field 'wikibase' (a nil value). 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][5] 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.
Contents
Effects
- EPSP in autonomic ganglia[citation needed]
- Secretion of catecholamines from the adrenal medulla[6]
- Secretion from salivary glands
- Gastric acid secretion from stomach[7]
- In CNS (memory?)[8]
- Vagally-induced bronchoconstriction[7]
- Mediating olfactory behaviors (e.g aggression, mating) [9]
Mechanism
It couples to Gq, and, to a small extent, Gi and Gs. This results in slow EPSP and decreased K+ conductance[8][10] It is preassembled to the Gq heterotrimer through a polybasic c-terminal domain.[4]
Ligands
Agonists
- Acetylcholine
- Carbachol[8]
- Cevimeline
- Pilocarpine[11]
- CDD-0097
- McN-A-343 - mixed M1/M4 agonist[8]
- L-689,660 - mixed M1/M3 agonist
- Oxotremorine
- Vedaclidine
- Xanomeline
- Muscarine
- 77-LH-28-1 - brain penetrant selective M1 allosteric agonist
Allosteric modulators
Antagonists
- atropine[8]
- Hyoscyamine[14]
- dicycloverine[8]
- tolterodine[8]
- oxybutynin[8]
- ipratropium[8]
- mamba toxin muscarinic toxin 7 (MT7)[8]
- olanzapine
- pirenzepine
- telenzepine
Gene
The receptor is encoded by human gene CHRM1.[7] It is localized to 11q13.[7]
See also
References
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Further reading
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External links
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.
