Gamma-aminobutyric acid type A receptor subunit alpha 1 (GABRA1) (GABRA1)

The Gamma-aminobutyric acid type A receptor subunit alpha 1 (GABRA1) is a fundamental component of the GABA-A receptor, which serves as the primary inhibitory neurotransmitter receptor in the mammalian central nervous system (UniProt, Wikipedia). As a member of the Cys-loop family of ligand-gated ion channels, GABRA1-containing receptors are pentameric complexes that facilitate the influx of chloride ions into neurons upon binding with GABA, resulting in membrane hyperpolarization and reduced neuronal firing (NIH, Wikipedia). This subunit is the most abundant alpha subunit in the brain and is primarily localized at synapses, where it mediates fast phasic inhibition (UniProt, NIH). Dysregulation or mutations in the GABRA1 gene are associated with several neurological disorders, most notably idiopathic generalized epilepsies such as juvenile myoclonic epilepsy (NIH, Wikipedia). Pharmacologically, GABRA1 is a major therapeutic target; it is the specific site of action for sedative-hypnotic "Z-drugs" like zolpidem and is a key component of the benzodiazepine binding site, mediating the sedative and anticonvulsant effects of drugs like diazepam (Wikipedia, NIH).

Other names

GABAA1GABRA1GABA(A) receptor subunit alpha-1GABAAR subunit alpha-1EJMEJM1ECA4

Positive allosteric modulation of the GABA-A receptor complex, which increases the frequency or duration of chloride channel opening, leading to hyperpolarization of the postsynaptic neuron (Wikipedia, NIH).