Target intelligence / Profile preview

Gamma Aminobutyric Acid Type A Receptor Alpha Subunit (GABAA Receptor Alpha Subunit)

Target
GABAA Receptor Alpha Subunit
Molecular classification
Receptor, Ion channel, Ligand-gated ion channel
01

Overview

The GABAA receptor is a major inhibitory neurotransmitter receptor in the mammalian brain. It is an ionotropic, ligand-gated chloride channel that mediates fast synaptic inhibition upon activation by its endogenous ligand, gamma-aminobutyric acid (GABA). The alpha subunit is one of several types of subunits that assemble to form functional GABAA receptors. Different combinations of alpha isoforms confer distinct pharmacological properties. Synaptic receptors containing α(1/2/3) mediate phasic inhibition, while extrasynaptic receptors with certain alpha isoforms like α4 or α6 contribute to tonic inhibition due to higher sensitivity for ambient GABA concentrations.

Other names
GABAA Receptor α SubunitGABAA Receptor Alpha1 SubunitGABAA Receptor Alpha2 SubunitGABAA Receptor Alpha3 SubunitGABAA Receptor Alpha4 SubunitGABAA Receptor Alpha5 SubunitGABAA Receptor Alpha6 Subunit
02

Mechanism of action

Binding of GABA to the α/β subunit interface leads to chloride channel opening and neuronal hyperpolarization.

03

Biological functions

Neuronal inhibitionNeurotransmissionRegulation of neuronal excitability
04

Disease associations

EpilepsyAnxiety disordersInsomniaSchizophrenia
05

Safety considerations

ToleranceDependenceRespiratory depressionSedation
06

Interacting drugs

GABA

4 more in the full profile.

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