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Structural studies of the actions of anesthetic drugs on the γ-aminobutyric acid type A receptor.

Authors
  • Akk, Gustav
  • Steinbach, Joe Henry
Type
Published Article
Journal
Anesthesiology
Publication Date
Dec 01, 2011
Volume
115
Issue
6
Pages
1338–1348
Identifiers
DOI: 10.1097/ALN.0b013e3182315d93
PMID: 21881491
Source
Medline
License
Unknown

Abstract

The γ-aminobutyric acid type A receptor is the major transmitter-gated inhibitory channel in the central nervous system. The receptor is a target for anesthetics, anticonvulsants, anxiolytics, and sedatives whose actions facilitate the flow of chloride ions through the channel and enhance the inhibitory tone in the brain. Both the kinetic and structural aspects of the actions of modulators of the γ-aminobutyric acid type A receptor are of great importance to understanding the molecular mechanisms of general anesthesia. In this review, the structural rearrangements that take place in the γ-aminobutyric acid type A receptor during channel activation and modulation are described, focusing on data obtained using voltage-clamp fluorometry. Voltage-clamp fluorometry entails the binding of an environmentally sensitive fluorophore molecule to a site of interest in the receptor, and measurement of changes in the fluorescence signal resulting from activation- or modulation-elicited structural changes. Detailed investigations can provide a map of structural changes that underlie or accompany the functional effects of modulators.

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