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The two major classes of γ-aminobutyric acid (GABA) receptors are designated GABAA and GABAB.Whereas the GABAA receptor is a pentameric, ligand-gated ion channel, the GABAB site is a heterodimeric, G protein-coupled receptor (GPCR).Both were initially characterized using orthosteric agents, such as muscimol and bicuculline for GABAA and baclofen for GABAB.After the discovery that benzodiazepines interact allosterically with the GABAA site, attention turned to determining whether other agents ad in a similar manner.