Inhibitory Effects of the Antihistamines Epinastine, Terfenadine, and Ebastine on Potassium Currents in Rat Ventricular Myocytes-Reference-Cited by-同舟云学术

Inhibitory Effects of the Antihistamines Epinastine, Terfenadine, and Ebastine on Potassium Currents in Rat Ventricular Myocytes

Published:1999-09 Issue:9 Volume:51 Page:1059-1063
ISSN:0022-3573
Container-title:Journal of Pharmacy and Pharmacology
language:en
Short-container-title:

Author:

Ohtani Hisakazu¹,Hanada Erika¹,Hirota Michiko¹,Sato Hitoshi¹,Kotaki Hajime²,Sawada Yasufumi³,Uemura Hiroko⁴,Nakaya Haruaki⁴,Iga Tatsuji¹

Affiliation:

1. Department of Pharmacy, The University of Tokyo Hospital, Faculty of Medicine, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-8655, Japan

2. Department of Pharmacy, The Research Hospital, The Institute of Medical Sciences, The University of Tokyo, Shirokanedai, Minato-ku, Tokyo 108-0071, Japan

3. Faculty of Pharmaceutical Sciences, Kyushu University, Maidashi, Higashi-ku, Fukoka 812-0054, Japan

4. Faculty of Medicine, Chiba University, Inohana, Chuo-ku, Chiba 260-8670, Japan

Abstract

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

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Link

http://academic.oup.com/jpp/article-pdf/51/9/1059/36785703/0022357991773393.pdf

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