Target intelligence / Profile preview

Muscarinic Acetylcholine Receptor M2 (Cardiac) (M2R (Cardiac))

Target
M2R (Cardiac)
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

The muscarinic acetylcholine receptor in the heart is primarily the M2 subtype, a G protein-coupled receptor (GPCR) that mediates parasympathetic nervous system effects on cardiac tissue. Activation of cardiac M2 receptors by acetylcholine results in slowing heart rate, decreasing AV conduction, and reducing atrial contractility. This is achieved through Gi/o coupling, which inhibits adenylate cyclase and activates inward rectifier K+ channels. Drugs targeting this pathway are used clinically for arrhythmias or bradycardia management. Alterations or dysfunctions can contribute to arrhythmias or abnormal autonomic regulation.

Other names
Cholinergic Receptor, Muscarinic 2 (Cardiac)CHRM2 (Cardiac)
02

Mechanism of action

Gi/o protein activation, inhibition of adenylate cyclase, decreased cAMP levels, activation of inward rectifier K+ channels (I_{K,ACh})

03

Biological functions

Signal transductionRegulation of heart rateRegulation of AV conductionRegulation of atrial contraction
04

Disease associations

ArrhythmiasBradycardiaCardiovascular diseaseAutonomic dysfunction
05

Safety considerations

Potential for bradycardia with agonistsPotential for tachycardia with antagonistsOff-target effects due to receptor distribution in other tissues
06

Interacting drugs

Acetylcholine

3 more in the full profile.

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