Gamma-aminobutyric acid type A receptor (GABA-A receptor) (GABA-A receptor)

The Gamma-aminobutyric acid type A (GABA-A) receptor is a pentameric ligand-gated ion channel that serves as the primary mediator of inhibitory neurotransmission in the mammalian central nervous system (StatPearls). Upon the binding of the neurotransmitter GABA, the receptor undergoes a conformational change that allows the influx of chloride ions into the neuron, leading to membrane hyperpolarization and a subsequent reduction in neuronal firing (UniProt). This receptor is the primary therapeutic target for various sedative-hypnotic drugs, including the tertiary acetylenic alcohol ethchlorvynol, which acts as a positive allosteric modulator to enhance the inhibitory effects of GABA (NIH). Beyond sedation, the receptor plays a critical role in managing anxiety, muscle spasms, and seizure disorders. However, pharmacological modulation of this target is associated with significant safety concerns, including the development of physical dependence, tolerance, and potentially fatal respiratory depression in cases of overdose or drug-drug interactions (PubChem).

Other names

GABAA receptorGABA(A) receptorGamma-aminobutyric acid receptor subunit alpha-1Ligand-gated chloride channel

Positive allosteric modulation of the receptor channel to increase the frequency or duration of chloride channel opening in response to GABA binding