Identification of binding sites contributing to volatile anesthetic effects on GABA type A receptors.

ABSTRACT: Most general anesthetics enhance GABA type A (GABA_A) receptor activity at clinically relevant concentrations. Sites of action of volatile anesthetics on the GABA_A receptor remain unknown, whereas sites of action of many intravenous anesthetics have been identified in GABA_A receptors by using photolabeling. Here, we used photoactivatable analogs of isoflurane (AziISO) and sevoflurane (AziSEVO) to locate their sites on α₁β₃γ_2L and α₁β₃ GABA_A receptors. As with isoflurane and sevoflurane, AziISO and AziSEVO enhanced the currents elicited by GABA. AziISO and AziSEVO each labeled 10 residues in α₁β₃ receptors and 9 and 8 residues, respectively, in α₁β₃γ<

SUBMITTER: Woll KA 

PROVIDER: S-EPMC6044061 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature