• Source: 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. It is localized to 11q13.
This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve, is common in exocrine glands and in the CNS.
It is predominantly found bound to G proteins of class Gq 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


EPSP in autonomic ganglia
Secretion from salivary glands
Gastric acid secretion from stomach
Via the central nervous system (especially within the brain); mediating certain core aspects of perception, attention, cognitive functioning and likely; memory consolidation. This is a notable component in regards to the M1 receptor since it helps explain how pharmacological compounds which antagonize the receptor site can consistently produce mental states like delirium (a major disruption in attention and decrease in baseline-level cognitive functioning), as well as the perceptual alterations and conspicuous hallucinations experienced with deliriant drugs like Datura. As of 2015, the M1 receptor remains the only known muscarinic receptor to have this effect of hallucinogenic delirium when its functionality is inhibited or antagonized.
Cognitive flexibility
Synaptic plasticity modulation
Anxiety-like behavior and spontaneous working memory
Salivation
Task switching
Vagally-induced bronchoconstriction
Mediating olfactory behaviors and detection of "social odors" which have implications (for rodents) in aggression, mating, and social behavior.




Occurrence in free living amoebae


A structural but not sequential homolog of the human M1 receptor has been reported in Acanthamoeba castellanii and Naegleria fowleri. 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. It is preassembled to the Gq heterotrimer through a polybasic c-terminal domain.




Ligands






= Agonists

=




= Allosteric modulators

=
benzylquinolone carboxylic acid
BQZ-12
VU-0090157
VU-0029767
VU0467319
[3H]PT-1284- M1-selective PAM Radioligand




= Antagonists

=




See also


Muscarinic acetylcholine receptor




References






Further reading






External links


"Acetylcholine receptors (muscarinic): M1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2 January 2015. Retrieved 25 November 2008.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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