[3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen.

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Finlayson K, Turnbull L, January CT, Sharkey J, Kelly JS

[3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen.

Eur J Pharmacol. 2001 Oct 26;430(1):147-8.

PubMed ID

11698075 [ View in PubMed

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Abstract

The pharmacological characteristics of [3H]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-1H-benzimidazol-2-yl)amino]ethyl]-4-[(methylsulfo nyl)amino]benzene-sulfonamide (WAY-123,398) and d-sotalol all inhibited [3H]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 [3H]dofetilide binding assay using HERG membranes may help identify compounds that prolong the QT interval.

DrugBank Data that Cites this Article

Drug Targets

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