Target intelligence / Profile preview

Gamma-aminobutyric acid type A receptor alpha4 subunit (GABRA4)

Target
GABRA4
Molecular classification
Ligand-gated ion channel, Receptor, GABA receptor subunit
01

Overview

The gamma-aminobutyric acid type A receptor alpha4 subunit (GABRA4) is a protein subunit of the GABA_A receptor, a ligand-gated ion channel that mediates inhibitory neurotransmission in the central nervous system. Alpha4-containing receptors are predominantly located extrasynaptically and contribute to tonic inhibition, playing a critical role in regulating neuronal excitability, particularly in the thalamus and dentate gyrus. These receptors are relatively insensitive to benzodiazepines but sensitive to other sedative-hypnotics like neurosteroids and gaboxadol. GABRA4 has been implicated in autism spectrum disorders.

Other names
GABA(A) receptor subunit alpha-4GABAAR subunit alpha-4
02

Mechanism of action

Forms part of GABA_A receptors that mediate inhibitory neurotransmission by allowing chloride ions to flow into neurons upon activation by gamma aminobutyric acid (GABA), leading to hyperpolarization. Predominantly involved in tonic inhibition through extrasynaptic receptors.

03

Biological functions

Inhibitory neurotransmissionRegulation of neuronal excitabilityTonic inhibition
04

Disease associations

Autism spectrum disorders
05

Safety considerations

Potential for off-target effects due to interaction with other GABA_A receptor subtypesModulation of neural excitability can have broad effects
06

Interacting drugs

Ethanol

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