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. 2016 Sep 28;17(10):1648. doi: 10.3390/ijms17101648

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© 2016 by the authors; licensee MDPI, Basel, Switzerland.

This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).

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F656C-hERG abrogates the stereospecific differences between quinidine and quinine. (A) Representative currents of WT-hERG and F656C-hERG after quinidine or quinine treatment. The protocol is illustrated in Figure 2A. Quinidine 10 μM exhibited no significant blockage and quinine 100 μM exhibited slight blockage of F656C-hERG; (B) The extent of blockage of WT-hERG or F656C-hERG by quinidine and quinine. IC₅₀ of quinidine and quinine for F656C-hERG was 771 ± 81 μM and 391 ± 40 μM, respectively. Quinine is more potent than quinidine in blocking F656C-hERG in comparison to blocking WT-hERG. Abbreviations: ctl, control; WT-hERG, wild type hERG; F656C-hERG, phenylalanine in 656 mutanted to cysteine.