IndraLab

Statements

Fexofenadine inhibits KCNH2. 4 / 4
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"In XREF_FIG, application of 10 muM resveratrol and 1 muM fexofenadine rescued hERG tail current reduction in the presence of 10 muM BBR."
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"Testing of terfenadine versus terfenadine carboxylate (fexofenadine) showed that the two similarly structured molecules both rescued hERG trafficking, but while terfenadine also blocked hERG channels [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In this study, we demonstrated that 1) cav-1 participates in BBR induced hERG deficiency on cell surface; 2) residues Tyr652 and Phe656, essential components of hERG binding sites, mediate hERG surface expression inhibition by BBR incubation; and 3) fexofenadine and resveratrol can shorten APD of ventricular cardiomyocytes prolonged by BBR."
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"HERG channel blockers, such as E4031, fexofenadine and astemizole, facilitated maturation of hERG proteins by acting as chemical chaperones XREF_BIBR; however, these agents can not be used clinically for enhancing hERG channel currents, because they acutely block the rapidly activating delayed-rectifier K + channel current (I Kr)."
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