Blockade of HERG channels expressed in <i>Xenopus</i> oocytes by the histamine receptor antagonists terfenadine and astemizole
書誌事項
- 公開日
- 1996-04-29
- 権利情報
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- http://onlinelibrary.wiley.com/termsAndConditions#vor
- DOI
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- 10.1016/0014-5793(96)00355-9
- 公開者
- Wiley
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説明
<jats:p>The widely used histamine receptor antagonists terfenadine and astemizole were shown to prolong the QT interval in electrocardiographic recordings in cases of overdose or inappropriate co‐medications, indicating a possible interaction with cardiac K<jats:sup>+</jats:sup> channels. Here, terfenadine and astemizole both inhibited the <jats:italic>h</jats:italic>uman <jats:italic>e</jats:italic>ther‐a‐go‐go <jats:italic>r</jats:italic>elated gene (HERG) encoded channels expressed in <jats:italic>Xenopus</jats:italic> oocytes at nanomolar concentrations in a use‐ and voltage‐dependent fashion. In contrast, inhibition of other delayed rectifier (Kvl.1 and I<jats:sub>sK</jats:sub>) or inward rectifier K<jats:sup>+</jats:sup> channels (IRK1) was much weaker and occurred only at high micromolar concentrations. These results suggest that blockade of HERG channels by terfenadine and astemizole might contribute to the cardiac side effects of these compounds.</jats:p>
収録刊行物
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- FEBS Letters
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FEBS Letters 385 (1-2), 77-80, 1996-04-29
Wiley