gamma-Aminobutyric acid (GABA), which is the main inhibitory neurotransmitter in the mammalian brain, exerts its effects through the activation of a ligand-gated ion channel, the GABAA receptor, leading to the inhibition of the activity of neurons. A family of GABAA receptors has been identified, some of which are targets for therapeutic agents such as benzodiazepines, barbiturates and general anesthetics. Recently, novel transgenic approaches have been used to understand the function of receptor subtypes and, thereby, their therapeutic utility. Additionally, progress has been made in the development of novel receptor subtype-selective compounds. In this review, we will primarily focus on progress achieved in the understanding of the function of this receptor family, and potential exploitation for drug development.