Target intelligence / Profile preview

Nicotinic Acetylcholine Receptor α4β2 Subtype (nAChR α4β2)

Target
nAChR α4β2
Molecular classification
Ligand-gated ion channel, Receptor
01

Overview

The nicotinic acetylcholine receptor (nAChR) α4β2 subtype is a ligand-gated ion channel composed of α4 and β2 subunits. It is the most abundant nAChR subtype in the mammalian brain and plays critical roles in cognition, reward, mood regulation, nociception, and synaptic transmission. This receptor is also the primary biological target mediating nicotine’s addictive properties due to its high affinity for nicotine.

Other names
alpha4beta2 nAChRα4β2 nAChR
02

Mechanism of action

Activation leads to increased Na⁺ and K⁺ permeability across neuronal membranes, resulting in post- and presynaptic excitation within neural circuits

03

Biological functions

Synaptic transmissionPostsynaptic excitationPresynaptic excitationGrowth hormone secretionModulation of neural circuits
04

Disease associations

Alzheimer’s diseaseParkinson’s diseaseEpilepsySchizophreniaDepressionAnxiety disordersTourette's syndromeStress-related conditionsNicotine addiction
05

Safety considerations

Upregulation by chronic nicotine exposureChanges in subunit composition altering drug responsePotential modulation by inflammatory cytokines
06

Interacting drugs

Acetylcholine

3 more in the full profile.

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