Target intelligence / Profile preview

Muscarinic Acetylcholine Receptor (Peripheral) (mAChR (Peripheral))

Target
mAChR (Peripheral)
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Muscarinic acetylcholine receptors (mAChRs) are a family of G protein-coupled receptors (GPCRs) that mediate the actions of the neurotransmitter acetylcholine in peripheral tissues. Primarily responsible for transmitting signals from postganglionic fibers of the parasympathetic nervous system, regulating a wide range of physiological functions including heart rate, smooth muscle contraction, and glandular secretion. There are five known subtypes: M1, M2, M3, M4, and M5. Each is encoded by a separate gene and exhibits distinct tissue distribution and physiological roles. Odd-numbered subtypes (M1, M3, M5) typically couple to Gq/11 proteins leading to phospholipase C activation, while even-numbered subtypes (M2, M4) typically couple to Gi/o proteins leading to inhibition of adenylyl cyclase and decreased cAMP production.

Other names
Peripheral Muscarinic ReceptormAChRMuscarinic Receptor
02

Mechanism of action

Activation of G proteins leading to phospholipase C activation (Gq/11) or inhibition of adenylyl cyclase (Gi/o), depending on the receptor subtype.

03

Biological functions

Signal transductionSmooth muscle contractionGlandular secretionHeart rate regulationNeurotransmission
04

Disease associations

BradycardiaTachycardiaAsthmaCOPDOveractive bladderGastrointestinal disorders
05

Safety considerations

Side effects associated with non-selective muscarinic receptor targeting
06

Interacting drugs

Pilocarpine

2 more in the full profile.

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