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Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole.
FEBS Lett. 1996 Apr 29; 385(1-2):77-80.FL

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 human ether-a-go-go related 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 (Kv1.1 and IsK) 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.

Authors+Show Affiliations

Physiologisches Institut I, Eberhard-Karls-Universität Tübingen, Germany.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

8641472

Citation

Suessbrich, H, et al. "Blockade of HERG Channels Expressed in Xenopus Oocytes By the Histamine Receptor Antagonists Terfenadine and Astemizole." FEBS Letters, vol. 385, no. 1-2, 1996, pp. 77-80.
Suessbrich H, Waldegger S, Lang F, et al. Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. FEBS Lett. 1996;385(1-2):77-80.
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, 385(1-2), 77-80.
Suessbrich H, et al. Blockade of HERG Channels Expressed in Xenopus Oocytes By the Histamine Receptor Antagonists Terfenadine and Astemizole. FEBS Lett. 1996 Apr 29;385(1-2):77-80. PubMed PMID: 8641472.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. AU - Suessbrich,H, AU - Waldegger,S, AU - Lang,F, AU - Busch,A E, PY - 1996/4/29/pubmed PY - 1996/4/29/medline PY - 1996/4/29/entrez SP - 77 EP - 80 JF - FEBS letters JO - FEBS Lett VL - 385 IS - 1-2 N2 - 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 human ether-a-go-go related 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 (Kv1.1 and IsK) 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. SN - 0014-5793 UR - https://www.unboundmedicine.com/medline/citation/8641472/Blockade_of_HERG_channels_expressed_in_Xenopus_oocytes_by_the_histamine_receptor_antagonists_terfenadine_and_astemizole_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0014-5793(96)00355-9 DB - PRIME DP - Unbound Medicine ER -