Each receptor complex has 2 GABA-binding sites but only 1 BZD-binding site. GABA-A receptors contain 2 α subunits, 2 β subunits, and 1 γ subunit. The GABA-A receptor complex is composed of 5 glycoprotein subunits, each with multiple isoforms ( Figure 1). This article focuses primarily on the GABA-A receptor, with which BZDs interact. 2 The 3 GABA receptors are designated A, B, and C.
GABA produces a calming effect on the brain. GABA is inhibitory in nature and thus reduces the excitability of neurons.
GABA is the most common neurotransmitter in the central nervous system, found in high concentrations in the cortex and limbic system. The GABA-A receptor is a ligand-gated chloride-selective ion channel.
BZDs act as positive allosteric modulators on the gamma amino butyric acid (GABA)-A receptor.
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