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Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole
Abstract
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.
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Citations
Cited by
Roth, B. L., Sheffler, D. J., & Kroeze, W. K. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1346 · Cited by 1,155
H1‐antihistamines: inverse agonism, anti‐inflammatory actions and cardiac effects
Leurs, R., Church, M. K., & Taglialatela, M. (2002) · Clinical & Experimental Allergy · doi:10.1046/j.0954-7894.2002.01314.x · Cited by 450
Oncogenic potential of EAG K+ channels
Pardo, L. A., del Camino, D., Sánchez, A., Alves, F., Brüggemann, A., Beckh, S., & Stühmer, W. (1999) · The EMBO Journal · doi:10.1093/emboj/18.20.5540 · Cited by 446
MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes
Kramer, J., Obejero-Paz, C. A., Myatt, G., Kuryshev, Y. A., Bruening-Wright, A., Verducci, J. S., & Brown, A. M. (2013) · Scientific Reports · doi:10.1038/srep02100 · Cited by 347
Recanatini, M., Poluzzi, E., Masetti, M., Cavalli, A., & De Ponti, F. (2005) · Medicinal Research Reviews · doi:10.1002/med.20019 · Cited by 285
Metadata
- Authors
- Suessbrich, H., Waldegger, S., Lang, F., & Busch, A. E.
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1996-04-29
- Volume
- 385
- Issue
- 1-2
- Pages
- 77-80
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2025043418
- Cited by
- 222
- References
- 0
- FWCI
- 3.71
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. https://app.cochat.ai/papers/10.1016/0014-5793(96)00355-9
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- Suessbrich, H., Waldegger, S., Lang, F., & Busch, A. E. (1996). Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. FEBS Letters. https://doi.org/10.1016/0014-5793(96)00355-9
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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