Presented at the 37th Annual Scientific Meeting of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, Sydney, 29 November−3 December 2003.
GABAC RECEPTOR ION CHANNELS
Article first published online: 25 NOV 2004
Clinical and Experimental Pharmacology and Physiology
Volume 31, Issue 11, pages 800–804, November 2004
How to Cite
Chebib, M. (2004), GABAC RECEPTOR ION CHANNELS. Clinical and Experimental Pharmacology and Physiology, 31: 800–804. doi: 10.1111/j.1440-1681.2004.04083.x
- Issue published online: 25 NOV 2004
- Article first published online: 25 NOV 2004
- Received 25 March 2004; revision 6 August 2004; accepted 17 August 2004.
- GABAC receptors;
- ligand-gated ion channels;
- site-directed mutagenesis;
- structure–activity relationship studies
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.