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• W2108385394 abstract "The purpose of this review is to summarize current knowledge of detailed biochemical evidence for the role of γ-aminobutyric acid type A receptors (GABAA–Rs) in the mechanisms of general anesthesia. With the knowledge that all general anesthetics positively modulate GABAA-R-mediated inhibitory transmission, site-directed mutagenesis comparing sequences of GABAA-R subunits of varying sensitivity led to identification of amino acid residues in the transmembrane domain that are critical for the drug actions in vitro. Using a photo incorporable analogue of the general anesthetic, R(+)etomidate, we identified two transmembrane amino acids that were affinity labelled in purified bovine brain GABAA-R. Homology protein structural modelling positions these two residues, αM1-11’ and βM3-4’, close to each other in a single type of intersubunit etomidate binding pocket at the β/α interface. This position would be appropriate for modulation of agonist channel gating. Overall, available information suggests that these two etomidate binding residues are allosterically coupled to sites of action of steroids, barbiturates, volatile agents, and propofol, but not alcohols. Residue α/βM2-15’ is probably not a binding site but allosterically coupled to action of volatile agents, alcohols, and intravenous agents, and α/βM1-(-2’) is coupled to action of intravenous agents. Establishment of a coherent and consistent structural model of the GABAA-R lends support to the conclusion that general anesthetics can modulate function by binding to appropriate domains on the protein. Genetic engineering of mice with mutation in some of these GABAA-R residues are insensitive to general anesthetics in vivo, suggesting that further analysis of these domains could lead to development of more potent and specific drugs." @default.
• W2108385394 created "2016-06-24" @default.
• W2108385394 creator A5027334799 @default.
• W2108385394 creator A5066912472 @default.
• W2108385394 date "2010-12-31" @default.
• W2108385394 modified "2023-10-07" @default.
• W2108385394 title "GABAA receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation" @default.
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• W2108385394 doi "https://doi.org/10.1007/s12630-010-9429-7" @default.
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