Article
Ranolazine inhibition of hERG potassium channels: drug-pore interactions and reduced potency against inactivation mutants.
Journal of molecular and cellular cardiology - 1 Sept 2014
Du Chunyun, Zhang Yihong, El Harchi Aziza, Dempsey Christopher E, Hancox Jules C
Abstract excerpt
The antianginal drug ranolazine, which combines inhibitory actions on rapid and sustained sodium currents with inhibition of the hERG/IKr potassium channel, shows promise as an antiarrhythmic agent. This study investigated the structural basis of hERG block by ranolazine, with lidocaine used as a low potency, structurally similar comparator. Recordings of hERG current (IhERG) were made from cell lines expressing...
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