Target intelligence / Profile preview

Neuronal Acetylcholine Receptor Subunit Alpha-4 (nAChRα4)

Target
nAChRα4
Molecular classification
Receptor, Ligand-gated ion channel
01

Overview

The neuronal acetylcholine receptor subunit alpha-4 (nAChRα4) is a subunit of the nicotinic acetylcholine receptor (nAChR), a ligand-gated ion channel that mediates fast synaptic transmission. It forms heteromeric receptors, predominantly α4β2 nAChRs, which are crucial for modulating neurotransmitter release, cognitive processes, and mediating addictive responses to nicotine. Mutations in CHRNA4, the gene encoding α4, are linked to neurological disorders such as ADNFLE and paroxysmal kinesogenic dyskinesia. Alpha-4-containing nAChRs are therapeutic targets for conditions including neurodegenerative diseases, epilepsy, schizophrenia, depression, pain management, and smoking cessation.

Other names
CHRNA4NACRA4NACHRABFNC
02

Mechanism of action

Agonist binding induces conformational change, opening the ion channel and allowing cation influx (primarily Na+).

03

Biological functions

Synaptic transmission modulationNeurotransmitter releaseCognitive processes (learning, memory)Regulation of neuronal excitabilityMediation of addictive responses
04

Disease associations

Autosomal Dominant Nocturnal Frontal Lobe Epilepsy (ADNFLE)Paroxysmal Kinesogenic DyskinesiaNeurodegenerative diseasesEpilepsySchizophreniaDepressionAddiction
05

Safety considerations

Potential for seizures with excessive activationAddictive properties of nicotinePotential for off-target effects due to widespread expression in the brain
06

Interacting drugs

Acetylcholine

1 more in the full profile.

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