Target intelligence / Profile preview

Muscarinic Acetylcholine Receptor M1-M5 Subtypes (mAChR M1-M5)

Target
mAChR M1-M5
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Muscarinic acetylcholine receptors (mAChRs) are a family of five G protein-coupled receptor subtypes (M1-M5) that mediate the effects of acetylcholine in the central and peripheral nervous systems. They play critical roles in cognition, heart rate regulation, smooth muscle contraction, glandular secretion, and modulation of neurotransmitter release. Each subtype is encoded by a distinct gene and couples to different G proteins (Gq/11 or Gi/o), leading to activation of phospholipase C or inhibition of adenylyl cyclase, respectively. They represent important therapeutic targets across neurology, psychiatry, cardiology, ophthalmology, and drug addiction, and ongoing advances continue to refine our ability to selectively modulate their activity using structure-based drug design approaches.

Other names
M1 receptorM2 receptorM3 receptorM4 receptorM5 receptorCHRM1CHRM2CHRM3CHRM4CHRM5
02

Mechanism of action

Agonism or antagonism of muscarinic acetylcholine receptors, leading to downstream effects via G protein signaling pathways (Gq/11 activation of phospholipase C or Gi/o inhibition of adenylyl cyclase).

03

Biological functions

Signal transductionRegulation of heart rateSmooth muscle contractionGlandular secretionModulation of neurotransmitter releaseCognitive processingDopamine pathway modulationReward pathway modulation
04

Disease associations

Alzheimer's diseaseSchizophreniaGlaucomaDry mouthDrug addictionPsychosis
05

Safety considerations

Off-target effects due to overlapping tissue distribution among subtypes.Development of highly selective ligands remains challenging.Potential for probe dependence at allosteric sites.
06

Interacting drugs

Pilocarpine

2 more in the full profile.

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