Target intelligence / Profile preview

Gamma-Aminobutyric Acid Type A Receptor Alpha4-Beta3-Gamma Subunit

Molecular classification
Cys-loop ligand-gated ion channels, Receptor, Ion channel
01

Overview

The gamma-aminobutyric acid type A (GABA_A) receptor is a ligand-gated ion channel and the principal mediator of fast inhibitory neurotransmission in the central nervous system (CNS). The specific target described—alpha4-beta3-gamma subunit—refers to a pentameric assembly typically composed of two α4, two β3, and one γ (usually γ2) subunits. This combination determines the receptor’s localization, pharmacology, and physiological function. When activated by GABA binding, these receptors open their intrinsic chloride ion channel. Chloride influx hyperpolarizes neurons, inhibiting action potential firing. Alterations in expression or function of specific GABA_A receptor assemblies have been implicated in epilepsy, anxiety disorders, sleep disturbances, autism spectrum disorders, among others.

02

Mechanism of action

Ligand-gated chloride channel activity; Chloride influx hyperpolarizes neurons, inhibiting action potential firing.

03

Biological functions

Chloride transmembrane transportInhibitory postsynaptic potential generationRegulation of membrane potentialSynaptic transmissionFast inhibitory neurotransmission
04

Disease associations

EpilepsyAnxiety disordersSleep disturbancesAutism spectrum disorders
05

Interacting drugs

Benzodiazepines

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