Muscarinic acetylcholine receptor M1

The muscarinic acetylcholine receptor M1, also known as the cholinergic receptor, muscarinic 1, is a is_associated_with::muscarinic receptor.

This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve, is common in is_associated_with::exocrine glands and in the CNS.

It is predominantly found bound to G proteins of class Gq that use upregulation of is_associated_with::phospholipase C and, therefore, is_associated_with::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

 * EPSP in is_associated_with::autonomic ganglia
 * Secretion of is_associated_with::catecholamines from the is_associated_with::adrenal medulla
 * Secretion from is_associated_with::salivary glands
 * is_associated_with::Gastric acid secretion from is_associated_with::stomach
 * In CNS (memory?)
 * Vagally-induced is_associated_with::bronchoconstriction

Mechanism
It couples to Gq, and, to a small extent, Gi and Gs. This results in slow is_associated_with::EPSP and decreased K+ conductance It is preassembled to the Gq heterotrimer through a polybasic c-terminal domain.

Agonists

 * is_associated_with::acetylcholine
 * is_associated_with::carbachol
 * is_associated_with::CDD-0097
 * is_associated_with::Cevimeline
 * is_associated_with::McN-A-343 - mixed M1/M4 agonist
 * is_associated_with::L-689,660 - mixed M1/M3 agonist
 * is_associated_with::Oxotremorine
 * is_associated_with::Vedaclidine
 * is_associated_with::Xanomeline
 * is_associated_with::Muscarine
 * is_associated_with::77-LH-28-1 - brain penetrant selective M1 allosteric agonist
 * is_associated_with::pilocarpine

Allosteric modulators

 * benzylquinolone carboxylic acid
 * VU-0090157
 * VU-0029767

Antagonists

 * is_associated_with::atropine
 * is_associated_with::Hyoscyamine
 * is_associated_with::dicycloverine
 * is_associated_with::tolterodine
 * is_associated_with::oxybutynin
 * is_associated_with::ipratropium
 * is_associated_with::mamba toxin is_associated_with::muscarinic toxin 7 (MT7)
 * is_associated_with::olanzapine
 * is_associated_with::pirenzepine
 * is_associated_with::telenzepine

Gene
The receptor is encoded by human is_associated_with::gene CHRM1. It is localized to is_associated_with::11q13.