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. 2006 May 26;8(2):E353–E361. doi: 10.1007/BF02854906

Modulating inhibitory ligand-gated ion channels

Michael Cascio 1,✉
PMCID: PMC3231573  PMID: 16796386

Abstract

The glycine and γ-aminobutyric acid receptors (GlyR and GABAAR, respectively) are the major inhibitory neurotransmitter-gated receptors in the central nervous system of animals. Given the important role of these receptors in neuronal inhibition, they are prime targets of many therapeutic agents and are the object of intense studies aimed at correlating their structure and function. In this review, the structure and dynamics of these and other homologous members of the nicotinicoid superfamily are described. The modulatory actions of the major biological macromolecules that bind and allosterically affect these receptors are also discussed.

Keywords: Glycinereceptor, GABAAreceptor, nicotinicoid, anesthetics, therapeutics

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