IndraLab
Statements
Mexiletine inhibits KCNH2. 12 / 12
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"However, some of the above were attenuated by the fact that two strictly related compounds were considered where the only structural difference was an OH group in the meta-position of the xylyloxy moiety.Finally, in the light of our results, it is important to observe that, even though our data show that mexiletine inhibits hERG at physiologically relevant concentration, mexiletine has not been documented to significantly affect cardiac repolarization (normal QT-interval in the ECG) and is generally a drug well tolerated in man at low doses."
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"The study demonstrated that i) Mexiletine inhibited the hERG channel current in a time- and voltage dependent way; ii) Its inhibitory effect was strongly reduced by Y652A and F656A mutants; iii) It reduced the time constant of activation but increased the time constant of deactivation, meaning that it accelerated activation and decelerated deactivation; iv) Mexiletine did not influence the channel inactivation."
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"Given these observations, we conclude that mexiletine blocks the hERG channel preferentially in an open state, with features similar to those of other open-channel blockers, for example, miconazole, mesoridazine, and ketanserin (Su et al. 2004; Kikuchi et al. 2005; Tang et al. 2008)."