Gamma-Aminobutyric Acid Type A Receptor (GABA_A Receptor)

The GABA_A receptor is a major inhibitory neurotransmitter receptor in the mammalian central nervous system. It mediates fast synaptic inhibition by functioning as a ligand-gated chloride ion channel, activated primarily by gamma-aminobutyric acid (GABA). It is a pentameric transmembrane protein composed of various subunits, resulting in diverse isoforms with distinct properties. Modulation by various endogenous compounds and drugs such as benzodiazepines, barbiturates and neurosteroids makes it a major drug target.

Binding of GABA or agonists leads to conformational change, opening of the chloride channel, influx of chloride ions, and hyperpolarization of the neuron, resulting in inhibition.