Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel.

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Chachin M, Katayama Y, Yamada M, Horio Y, Ohmura T, Kitagawa H, Uchida S, Kurachi Y

Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel.

Eur J Pharmacol. 1999 Jun 25;374(3):457-60.

PubMed ID

10422790 [ View in PubMed

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Abstract

Terfenadine and astemizole rarely cause cardiac arrhythmias by suppressing the cardiac rapid delayed rectifier K+ channel encoded by the human ether-a-go-go-related gene (HERG). Epinastine, however, has not been reported to have the adverse effect. We have therefore compared the effects of epinastine, terfenadine and astemizole on HERG channels expressed in Xenopus oocytes. Terfenadine and astemizole suppressed the HERG current with IC50 of 431 nM and 69 nM, respectively. In contrast, 100 microM epinastine inhibited the HERG current by only 11+/-2.1%. These results may provide an explanation for the difference in the cardiotoxicity between different nonsedating histamine H1 receptor antagonists.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Astemizole	Potassium voltage-gated channel subfamily H member 2	Protein	Humans	Unknown	Inhibitor	Details