Block of HERG Potassium Channels by the Antihistamine Astemizole and its Metabolites Desmethylastemizole and Norastemizole

  title={Block of HERG Potassium Channels by the Antihistamine Astemizole and its Metabolites Desmethylastemizole and Norastemizole},
  author={Z. Zhou and V. Vorperian and Q. Gong and S. Zhang and C. January},
  journal={Journal of Cardiovascular Electrophysiology},
  • Z. Zhou, V. Vorperian, +2 authors C. January
  • Published 1999
  • Medicine
  • Journal of Cardiovascular Electrophysiology
  • Electrophysiologic Effects of Astemizole Metabolites. Introduction: The selective H1‐receptor antagonist astemizole (Hismanal) causes acquired long QT syndrome. Astemizole blocks the rapidly activating delayed rectifier K+ current IKr and the human ether‐a go‐go‐related gene (HKRG) K+ channels that underlie it. Astemizole also is rapidly metabolized. The principal metabolite is desmethylastemizole, which retains H1‐receptor antagonist properties, has a long elimination time of 9 to 13 days, and… CONTINUE READING
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