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

@article{Zhou1999BlockOH,
  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},
  year={1999},
  volume={10}
}
  • 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
    View on Wiley
    ncbi.nlm.nih.gov
    187 Citations
    Highly Influencial Citations
    6
    Background Citations
    49
    Methods Citations
    6
    Results Citations
    3
    187 Citations
    Citation Type

    Citation Type

    The anti-malarial drug halofantrine and its metabolite N-desbutylhalofantrine block HERG potassium channels.
    • 34
    • PDF
    Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK and HERG.
    • 65
    • PDF
    Clemastine, a conventional antihistamine, is a high potency inhibitor of the HERG K+ channel.
    • 39
    Interactions of the 5-hydroxytryptamine 3 antagonist class of antiemetic drugs with human cardiac ion channels.
    • 150
    • PDF
    Inhibition of hERG K+ currents by antimalarial drugs in stably transfected HEK293 cells.
    • 109
    • PDF
    Mechanism of Block of hEag1 K+ Channels by Imipramine and Astemizole
    • 120
    • Highly Influenced
    • PDF
    Blockade of the Human Ether A-Go-Go–Related Gene (hERG) Potassium Channel by Fentanyl
    • 9
    • PDF
    Flunarizine is a Highly Potent Inhibitor of Cardiac hERG Potassium Current
    • 22
    Effect of trazodone on hERG channel current and QT-interval.
    • 41
    Effect of H1 antihistamines upon the cardiovascular system.
    • 28
    • PDF

    References

    SHOWING 1-10 OF 44 REFERENCES
    Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole.
    • 95
    Antiallergic effects of major metabolites of astemizole in rats and guinea pigs.
    • 16
    Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole
    • 220
    Molecular basis for the lack of HERG K+ channel block-related cardiotoxicity by the H1 receptor blocker cetirizine compared with other second-generation antihistamines.
    • 124
    • PDF
    Effects of nonsedating antihistamine, astemizole, on the in situ canine heart assessed by cardiohemodynamic and monophasic action potential monitoring.
    • 40
    Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine.
    • 211
    Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride.
    • 171
    • PDF
    HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine.
    • 276
    Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers
    • 55
    Suppression of mammalian K+ channel family by ebastine.
    • 47