Target intelligence / Profile preview

Neuronal acetylcholine receptor subunit alpha4beta2 (α4β2 nAChR)

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

Overview

The neuronal acetylcholine receptor subunit alpha4beta2 (α4β2 nAChR) is a ligand-gated ion channel predominantly found in the brain. It is one of the most abundant and functionally significant nAChR subtypes in the central nervous system. This receptor mediates fast synaptic transmission by responding to the neurotransmitter acetylcholine and exogenous ligands such as nicotine. It exists in two main stoichiometries, (α4)₂(β2)₃ and (α4)₃(β2)₂, with varying sensitivity to nicotine and calcium permeability. Activation leads to increased permeability primarily for Na⁺ and K⁺ ions, resulting in neuronal excitation at both pre-synaptic and post-synaptic sites. It is implicated in cognitive processes such as learning and attention and involved in growth hormone secretion. Mutations can result in reduced stature and predisposition to obesity due to impaired growth hormone release.

Other names
Alpha-four beta-two nicotinic acetylcholine receptorα₄β₂ nAChR
02

Mechanism of action

Agonist binding leading to increased permeability for Na⁺ and K⁺ ions.

03

Biological functions

Fast synaptic transmissionNeuronal excitationIon channel activityGrowth hormone secretion
04

Disease associations

Autosomal dominant nocturnal frontal lobe epilepsyAneurysm/dissectionHypertensive crisisHypotensionAddiction
05

Safety considerations

Potential for addiction due to high affinity for nicotine.Implicated in epilepsy and cardiovascular disorders.
06

Interacting drugs

Acetylcholine

1 more in the full profile.

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