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Titolo:
Development and evaluation of high throughput functional assay methods forhERG potassium channel
Autore:
Tang, WM; Kang, JS; Wu, XY; Rampe, D; Wang, L; Shen, H; Li, ZY; Dunnington, D; Garyantes, T;
Indirizzi:
Aventis Pharmaceut, Dept Profiling & High Screening, Bridgewater, NJ 08807USA Aventis Pharmaceut Bridgewater NJ USA 08807 ing, Bridgewater, NJ 08807USA Aventis Pharmaceut, Dept Safety Pharmacol, Bridgewater, NJ 08807 USA Aventis Pharmaceut Bridgewater NJ USA 08807 ol, Bridgewater, NJ 08807 USA Aventis Pharmaceut, Dept Analyt Chem, Bridgewater, NJ 08807 USA Aventis Pharmaceut Bridgewater NJ USA 08807 em, Bridgewater, NJ 08807 USA
Titolo Testata:
JOURNAL OF BIOMOLECULAR SCREENING
fascicolo: 5, volume: 6, anno: 2001,
pagine: 325 - 331
SICI:
1087-0571(200110)6:5<325:DAEOHT>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
RESONANCE ENERGY-TRANSFER; HIGH-AFFINITY BLOCKADE; CARDIAC-ARRHYTHMIA; I-KR; FLUORESCENCE; TERFENADINE; ASTEMIZOLE; MEMBRANE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Tang, WM Aventis Pharmaceut, Dept Profiling & Screening, Route 206 N, Bridgewater, NJ 08807 USA Aventis Pharmaceut Route 206 N Bridgewater NJ USA 08807 08807 USA
Citazione:
W.M. Tang et al., "Development and evaluation of high throughput functional assay methods forhERG potassium channel", J BIOMOL SC, 6(5), 2001, pp. 325-331

Abstract

Three functional hERG channel assay methods have been developed and evaluated. The methods were tested against five known hERG channel inhibitors: dofetilide, terfenadine (Seldane), sertindole (Serdolect), astemizole (Hismanal), and cisapride (Propulsid). The DiBAC(4)(3)-based assays were found to be the most economical but had high false-hit rates as a result of the interaction of dye with the test compounds. The membrane potential dye assay had fewer color-quenching problems but was expensive and still gave false hits. The nonradioactive Rb+ efflux assay was the most sensitive of all the assays evaluated and had the lowest false-hit rate.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 16:04:41