Recent advances in the molecular biology of GABAA receptors is described along with the impact of these advances on drug design for this family of receptors. The receptor molecular structure is described with particular emphasis on the sites to which the transmitter GABA and modulatory drugs, such as the benzodiazepines, bind. The relationship of subunit structure to the electrophysiological properties of GABAA receptors is detailed with emphasis on the functional subtyping of GABAA receptor responses. The behavioral pharmacological results of knockout and knockin models are described, along with the effects of specific drugs on sleep, anxiety, and learning in normal animals.
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