Benzodiazepine Binding Site on Gamma-Aminobutyric Acid Type A Receptor

The benzodiazepine binding site is a specific allosteric modulatory site located on the gamma-aminobutyric acid type A (GABAA) receptor, a major inhibitory neurotransmitter receptor in the mammalian central nervous system. It is found in the extracellular domain at the interface between an α (typically α1) and γ (typically γ2) subunit. Benzodiazepines bind to this site to enhance GABA-induced chloride ion flux through the channel, leading to neuronal hyperpolarization. This underlies their anxiolytic, anticonvulsant, muscle-relaxant, sedative-hypnotic properties. Other ligands can act as negative allosteric modulators or antagonists at this same site.

Positive allosteric modulation of GABAA receptor activity, increasing chloride ion flux and hyperpolarizing neurons.