Journal
EUROPEAN JOURNAL OF PHARMACOLOGY
Volume 430, Issue 1, Pages 147-148Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/S0014-2999(01)01362-0
Keywords
[H-3]dofetilide; HERG; QT-interval
Categories
Ask authors/readers for more resources
The pharmacological characteristics of [H-3]dofetilide binding were examined in membranes prepared from human embryonic kidney (HEK293) cells stably expressing human ether-a-go-go related gene (HERG) K+ channels. The classIII antiarrhythmic compounds dofetilide, clofilium, 4 '-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidyl]carbonyl]methanesulfonanilide (E-4031), N-methyl-N-[2-[methyl-(1-methyl- 1 H-benzimidazol-2-yl)amino]ethyl]-4-[(methylsulfonyl)amino]benzene-sulfonamide (WAY- 123,398) and d-sotalol all inhibited [H-3]dofetilide binding. In addition, the structurally unrelated compounds pimozide, terfenadine and haloperidol, all of which prolong the QT interval in man, also inhibited binding. These data indicate that a [H-3]dofetilide binding assay using HERG membranes may help identify compounds that prolong the QT interval. (C) 2001 Published by Elsevier Science B.V.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available