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Genetically engineered muscarinic acetylcholine receptor (mAChR (when referring generally; individual subtypes are often abbreviated as M1, M2, etc., e.g., "M1 muscarinic acetylcholine receptor"))

Target
mAChR (when referring generally; individual subtypes are often abbreviated as M1, M2, etc., e.g., "M1 muscarinic acetylcholine receptor")
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

Genetically engineered muscarinic acetylcholine receptors refer to muscarinic receptor proteins that have been deliberately modified through genetic engineering to alter their structure, function, or pharmacological properties. The natural muscarinic acetylcholine receptors (mAChRs) are a family of five closely related G protein-coupled receptors (M1–M5) that mediate the effects of acetylcholine at parasympathetic and central synapses. They regulate critical functions in both the central and peripheral nervous systems, including signal transduction, cardiac regulation, glandular secretion, and cognition. Genetically engineered versions are typically used in research to understand receptor function, dissect signaling pathways, or develop subtype-selective drugs, and may include point mutations, chimeric constructs, or other modifications. However, "genetically engineered muscarinic acetylcholine receptors" is not a canonical target but a research tool derived from canonical subtypes such as M1, M2, M3, M4, or M5 receptors [2][3][6].

Other names
mAChRsmuscarinic receptormuscarinic acetylcholine receptormuscarinic GPCR
02

Mechanism of action

Agonists: Stimulate receptor to elicit parasympathetic responses or CNS effects Antagonists: Block receptor to inhibit muscarinic activity, used in multiple therapeutic settings Allosteric modulators: Modulate receptor activity indirectly

03

Biological functions

Signal transductionRegulation of heart rateSmooth muscle contractionGlandular secretionCognitive function such as learning and memoryParasympathetic nervous system regulation
04

Disease associations

Neurodegenerative disease (Alzheimer’s disease)SchizophreniaCardiovascular diseaseOther central nervous system disorders
05

Safety considerations

Broad receptor expression results in off-target effects (e.g., dry mouth, blurred vision, confusion)CNS and peripheral side effectsDose-limiting toxicity for non-selective ligands
06

Interacting drugs

Atropine

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