Effects of acehytisine hydrochloride on the F656C mutation of HERG K~+ channel
Abstract：Objective: To evaluate the electrophysiogical effects of acehytisine hydrochloride on the rapidly activating delayed rectifier potassium current (I(_Kr)) encoded by the F656C mutation of HERG gene, and on the HERG protein trafficking. Methods: The whole-cell patch clamp method was used to evaluate the effects of acehy-tisine hydrochloride on the I_(Kr). Western blot analysis was used to observe the effects of acehytisine hydrochloride on the protein expression. Results: Acehytisine hydrochloride produced a concentration-dependent blockage of the I_(HERG) and I_(tail). The activation curve was shifted in a negative direction by acehytisine hydrochloride. High concen-tration of acehytisine hydrochloride inhibited HERG K~+ channel protein trafficking, and F656C mutation enhanced the inhibition of protein trafficking. Conclusion: Acehytisine hydrochloride inhibits HERG K~+ channel current via S6 domain. In addtition, it does not inhibit protein synthesis but inhibits protein trafficking.
Keywords：acehytisine hydrochloridepotassium channelHERG genewestern blotmutation protein
Publication Date：2010-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)