Fluorine-19 NMR and computational quantification of isoflurane binding to the voltage-gated sodium channel NaChBac.

ABSTRACT: Voltage-gated sodium channels (Na_V) play an important role in general anesthesia. Electrophysiology measurements suggest that volatile anesthetics such as isoflurane inhibit Na_V by stabilizing the inactivated state or altering the inactivation kinetics. Recent computational studies suggested the existence of multiple isoflurane binding sites in Na_V, but experimental binding data are lacking. Here we use site-directed placement of ¹⁹F probes in NMR experiments to quantify isoflurane binding to the bacterial voltage-gated sodium channel NaChBac. ¹⁹F probes were introduced individually to S129 and L150 near the S4-S5 linker, L179 and S208 at the extracellular surface, T189 in the ion selectivity filter, and all phenylalanine residues. Qua

SUBMITTER: Kinde MN 

PROVIDER: S-EPMC5137747 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature