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Keywords:

  • GABAC receptors;
  • ligand-gated ion channels;
  • site-directed mutagenesis;
  • structure–activity relationship studies

SUMMARY

1. The present review gives an overview of studies conducted on GABAC receptors over the past 10 years since the author started at the University of Sydney. It concentrates on the structure–activity relationship profiles of the receptor and how these studies were used to: (i) develop selective GABAC receptor ligands; and (ii) understand the impact of amino acid changes on GABAC receptor pharmacology and function.

2. Structure–activity relationship studies involving variations of both ligands and their receptor targets are vital to the discovery of drugs that interact selectively with particular native and mutant receptor subtypes. Such agents may be useful for treating anxiety, depression, epilepsyand memory related disorders, such as Alzheimer's disease.