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Target intelligence / Profile preview
Muscarinic Acetylcholine Receptor M4 (CHRM4)
- Target
- CHRM4
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The muscarinic acetylcholine receptor M4 (CHRM4) is a G protein-coupled receptor that functions as an inhibitory autoreceptor for acetylcholine. It is highly expressed in the forebrain, particularly in the striatum, and plays a role in regulating neurotransmitter release and modulating dopaminergic neurotransmission. CHRM4 is implicated in several neurological disorders, including Parkinson's disease, schizophrenia, and Alzheimer's disease, and is a potential therapeutic target for these conditions. Drug development efforts focus on achieving subtype-selective modulation to minimize off-target cholinergic side effects.
- Other names
- M4 receptormAChR4
02
Mechanism of action
Gi/o-coupled receptor activation; inhibits adenylate cyclase; modulates potassium channels; inhibits acetylcholine release.
03
Biological functions
Signal transductionRegulation of neurotransmitter releaseInhibitory autoreceptor functionModulation of dopaminergic neurotransmission
04
Disease associations
Alzheimer's diseaseParkinson's diseaseSchizophreniaMyelodysplastic syndromeAnemiaMovement disorders
05
Safety considerations
Off-target cholinergic side effectsSelectivity challenges due to high homology among mAChR subtypes
06
Interacting drugs
Xanomeline
3 more in the full profile.
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