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. 2015 Jul 31;3(5):e00160. doi: 10.1002/prp2.160

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© 2015 The Authors. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics.

This is an open access article under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non-commercial and no modifications or adaptations are made.

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(A) Structures of mexiletine and its hydroxylated metabolite m-hydroxymexiletine (MHM). (B) Representative hERG currents obtained before (control) and after addition of 50 μmol/L mexiletine, recorded using the pulse protocol shown. The arrow indicates zero current level. (C) Time course of mexiletine-induced hERG tail current inhibition from the same cell shown in (B). (D) Concentration–response relationship (mean ± SEM) for block of hERG tail current by mexiletine and MHM. A Hill equation fit yielded an IC₅₀ of 3.7 ± 0.7 and 22.4 ± 1.2 μmol/L and a Hill slope of 0.93 ± 0.09 and 1.3 ± 0.08, for mexiletine and MHM, respectively (n ≥ 5 per data point).