Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes

Hisakazu Ohtani, Erika Hanada, Michiko Hirota, Hitoshi Sato, Hajime Kotaki, Yasufumi Sawada, Hiroko Uemura, Haruaki Nakaya, Tatsuji Iga

研究成果: Article査読

12 被引用数 (Scopus)

抄録

We examined and compared the inhibitory effects of three non-sedating antihistamines, terfenadine, ebastine, and epinastine, on delayed rectifier potassium current (I(K)) and transient outward potassium current (I(to)) of rat isolated ventricular myocytes, using a patch clamp technique. Terfenadine, ebastine and epinastine were found to inhibit I(K) with IC50 values of 5.96, 15.3 and 145 μM, respectively. I(to) was suppressed by epinastine with an IC50 value of 69.5 μM. The order of arrhythmogenicity, assessed by the inhibition of I(K), was ranked as terfenadine > ebastine > epinastine, consistent with that of the potencies of each drug for QT prolongation reported in rats.

本文言語English
ページ(範囲)1059-1063
ページ数5
ジャーナルJournal of Pharmacy and Pharmacology
51
9
DOI
出版ステータスPublished - 1999 9
外部発表はい

ASJC Scopus subject areas

  • 薬理学
  • 薬科学

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