Gamma-aminobutyric acid type A receptor (GABA\(_A\) receptor) (GABA\(_A\)R)

The gamma-aminobutyric acid type A receptor is a ligand-gated chloride channel widely distributed in the central nervous system. It is assembled as a pentameric complex of subunits (most commonly 2α, 2β, 1γ), and upon the binding of its principal endogenous ligand, GABA, the channel opens to allow chloride ions (Cl\(^-\|)) to flow into the neuron. This influx typically hyperpolarizes the neuron, producing an inhibitory effect on neuronal firing and stabilizing network excitability. The GABA\(_A\) receptor is the principal mediator of fast inhibitory synaptic transmission in the brain, and is the target of several classes of clinically important drugs, including benzodiazepines, barbiturates, Z-drugs, and various anesthetics. Alterations in GABA\(_A\) receptor function or expression are linked to a range of neurological and psychiatric disorders, making it a major therapeutic target in medicine and research.

Other names

GABA-gated chloride channelGABA\(_A\) receptorIonotropic GABA receptorGABA-activated Cl\(^-\) channel

Positive allosteric modulation (benzodiazepines, barbiturates), Direct agonism (GABA, muscimol), Antagonism (bicuculline, picrotoxin), Channel blockade, Negative allosteric modulation