Target intelligence / Profile preview

Nicotinic Acetylcholine Receptor Alpha4 Subunit (nAChRα4)

Target
nAChRα4
Molecular classification
Ligand-gated ion channel, Nicotinic acetylcholine receptor subunit, Receptor
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Overview

The nicotinic acetylcholine receptor alpha4 subunit (nAChRα4) is a protein encoded by the CHRNA4 gene in humans. It is a critical subunit of nicotinic acetylcholine receptors (nAChRs), which are ligand-gated ion channels that mediate fast signal transmission at synapses. The most common configuration in the brain consists of two alpha4 (α4) subunits and three beta2 (β2) subunits, forming the α4β2 receptor, which exists in two distinct stoichiometries with varying nicotine sensitivities and calcium permeabilities. The alpha4 subunit can also combine with beta4 subunits. Upon binding to acetylcholine or nicotine, the receptor undergoes a conformational change, opening an ion-conducting channel across the plasma membrane, allowing ions like calcium, sodium, and potassium to cross the cell membrane. Alpha4-containing nAChRs play a crucial role in nicotine addiction, learning, attention, and growth hormone secretion. They are implicated in epilepsy, movement disorders, and cardiovascular conditions, making them therapeutic targets for smoking cessation, cognitive disorders, epilepsy, and movement disorders.

Other names
CHRNA4Nicotinic receptor subunit alpha-4Alpha4 subunit of nicotinic acetylcholine receptor
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Mechanism of action

Agonist binding leading to ion channel opening and ion flux across the cell membrane.

03

Biological functions

Mediating fast signal transmission at synapsesControlling neurotransmitter release and uptakeMediating addictive response to nicotineContributing to learning and attentional performanceInfluencing growth hormone secretionIon channel activity
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Disease associations

EpilepsyMovement disorders (Paroxysmal kinesogenic dyskinesia)ObesityNicotine addictionCardiovascular conditions (Aneurysm/dissection, hypertensive crisis, hypotension)
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Safety considerations

Potential for seizures (epilepsy)Cardiovascular effects
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Interacting drugs

Acetylcholine

3 more in the full profile.

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