Target intelligence / Profile preview

Nicotinic Acetylcholine Receptor Alpha4Beta2 Subtype (α4β2 nAChR)

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

Overview

The nicotinic acetylcholine receptor alpha4beta2 subtype (α4β2 nAChR) is a heteromeric ligand-gated ion channel composed of α4 and β2 subunits. It is the most abundant neuronal nicotinic receptor subtype in the human brain and plays a critical role in modulating neurotransmission, particularly in pathways related to learning, attention, addiction, and reward. Upon binding acetylcholine or agonists like nicotine, the channel opens to allow cations—primarily Na⁺ and K⁺—to flow across the membrane, resulting in depolarization of neurons and subsequent excitation. This receptor is a primary mediator of nicotine’s addictive properties.

02

Mechanism of action

Cation channel activation leading to neuronal depolarization and excitation

03

Biological functions

Signal transductionNeurotransmissionModulation of dopamine releaseRegulation of growth hormone secretion
04

Disease associations

AddictionCognitive impairmentObesityShort stature
05

Safety considerations

Potential for addictionSide effects associated with nicotinic receptor agonists
06

Interacting drugs

Acetylcholine

1 more in the full profile.

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