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

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1059-1063
Number of pages5
JournalJournal of Pharmacy and Pharmacology
Volume51
Issue number9
DOIs
Publication statusPublished - 1999 Sep
Externally publishedYes

Fingerprint

Terfenadine
Histamine Antagonists
Muscle Cells
Potassium
Inhibitory Concentration 50
Patch-Clamp Techniques
epinastine
ebastine
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

Cite this

Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes. / Ohtani, Hisakazu; Hanada, Erika; Hirota, Michiko; Sato, Hitoshi; Kotaki, Hajime; Sawada, Yasufumi; Uemura, Hiroko; Nakaya, Haruaki; Iga, Tatsuji.

In: Journal of Pharmacy and Pharmacology, Vol. 51, No. 9, 09.1999, p. 1059-1063.

Research output: Contribution to journalArticle

Ohtani, Hisakazu ; Hanada, Erika ; Hirota, Michiko ; Sato, Hitoshi ; Kotaki, Hajime ; Sawada, Yasufumi ; Uemura, Hiroko ; Nakaya, Haruaki ; Iga, Tatsuji. / Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes. In: Journal of Pharmacy and Pharmacology. 1999 ; Vol. 51, No. 9. pp. 1059-1063.
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AU - Sato, Hitoshi

AU - Kotaki, Hajime

AU - Sawada, Yasufumi

AU - Uemura, Hiroko

AU - Nakaya, Haruaki

AU - Iga, Tatsuji

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