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Neuronal acetylcholine receptor subunit alpha-2 (CHRNA2) (CHRNA2)

Target
CHRNA2
Molecular classification
Ion channel, Ligand-gated ion channel, Nicotinic acetylcholine receptor, Receptor
01

Overview

The neuronal acetylcholine receptor subunit alpha-2 (CHRNA2) is a protein that forms part of the pentameric nicotinic acetylcholine receptors (nAChRs), which are ligand-gated ion channels in the central nervous system (UniProt: Q15822). These receptors are primarily composed of alpha and beta subunits and facilitate fast synaptic transmission by allowing the influx of cations such as sodium and calcium upon binding with acetylcholine (PubMed: 22539471). CHRNA2-containing receptors are notably expressed in the cerebral cortex and thalamus, where they contribute to the regulation of neuronal excitability and the modulation of sleep-wake cycles (NCBI Gene: 1135). Genetic variations and mutations in the CHRNA2 gene have been associated with Autosomal Dominant Nocturnal Frontal Lobe Epilepsy (ADNFLE) and nicotine dependence, underscoring its clinical relevance (PubMed: 22539471). Pharmacologically, these receptors are sensitive to nicotine and are targeted by various nicotinic agonists and partial agonists used in smoking cessation and cognitive research (PubChem: CHRNA2). Developing selective modulators for CHRNA2-containing receptors remains a therapeutic interest for treating specific forms of epilepsy and cognitive deficits while minimizing side effects associated with other nAChR subtypes (StatPearls: Nicotinic Receptors).

Other names
Cholinergic receptor nicotinic alpha 2 subunitnAChR alpha 2Nicotinic acetylcholine receptor alpha 2 subunitNeuronal nicotinic acetylcholine receptor alpha 2
02

Mechanism of action

Agonists or partial agonists bind to the receptor's extracellular site, triggering a conformational change that opens the ion channel pore, leading to neuronal depolarization through cation influx (PubMed: 22539471).

03

Biological functions

Synaptic transmissionNeurotransmissionIon transportRegulation of sleepCognitive function
04

Disease associations

EpilepsySleep-related hypermotor epilepsyNicotine dependenceCognitive impairment
05

Safety considerations

Seizure riskSleep disturbancesOff-target effects on other nAChR subtypesPotential for dependence
06

Interacting drugs

Nicotine

4 more in the full profile.

07

Biomarkers

CHRNA2 gene mutationsCHRNA2 polymorphisms

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