Unique general anesthetic binding sites within distinct conformational states of the nicotinic acetylcholine receptor

International Review of Neurobiology
Hugo R AriasM P Blanton

Abstract

General anesthesia is a complex behavioral state provoked by the pharmacological action of a broad range of structurally different hydrophobic molecules called general anesthetics (GAs) on receptor members of the genetically linked ligand-gated ion channel (LGIC) superfamily. This superfamily includes nicotinic acetylcholine (AChRs), type A and C gamma-aminobutyric acid (GABAAR and GABACR), glycine (GlyR), and type 3 5-hydroxytryptamine (5-HT3R) receptors. This review focuses on recent advances in the localization of GA binding sites on conformationally and compositionally distinct AChRs. The experimental evidence outlined in this review suggests that: 1. Several neuronal-type AChRs might be targets for the pharmacological action of distinct GAs. 2. The molecular components of a specific GA binding site on a certain receptor subtype are different from the structural determinants of the locus for the same GA on a different receptor subtype. 3. There are unique binding sites for distinct GAs in the same receptor protein. 4. A GA can activate, potentiate, or inhibit an ion channel, indicating the existence of more than one binding site for the same GA. 5. The affinity of a specific GA depends on the conformational state of the rec...Continue Reading

Citations

Jan 8, 2011·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·Stuart A Forman, Keith W Miller
Mar 8, 2006·The International Journal of Biochemistry & Cell Biology·Hugo R AriasCecilia Bouzat

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