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Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole
Author(s) -
Suessbrich H.,
Waldegger S.,
Lang F.,
Busch A.E.
Publication year - 1996
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(96)00355-9
Subject(s) - astemizole , terfenadine , herg , pharmacology , chemistry , blockade , histamine h1 receptor , histamine , xenopus , antagonist , potassium channel , medicine , endocrinology , receptor , biochemistry , gene
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 + channels. Here, terfenadine and astemizole both inhibited the h uman e ther‐a‐go‐go r elated gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use‐ and voltage‐dependent fashion. In contrast, inhibition of other delayed rectifier (Kvl.1 and I sK ) or inward rectifier K + 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.