hERG potassium channel assay.

CT Christopher M. Tan
CG Charles J. Gill
JW Jin Wu
NT Nathalie Toussaint
JY Jingjun Yin
TT Takayuki Tsuchiya
CG Charles G. Garlisi
DK David Kaelin
PM Peter T. Meinke
LM Lynn Miesel
DO David B. Olsen
AL Armando Lagrutta
HF Hideyuki Fukuda
RK Ryuta Kishii
MT Masaya Takei
KO Kouhei Oohata
TT Tomoko Takeuchi
TS Taku Shibue
HT Hisashi Takano
AN Akinori Nishimura
YF Yasumichi Fukuda
SS Sheo B. Singh
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To determine the in vitro test article effects on cardiac ion channel current (IKr), the rapidly activating, delayed rectifier potassium current was studied using Chinese hamster ovary (CHO) cells stably expressing the hERG channel encoded by human ether-à-go-go-related gene. Briefly, channel activity was functionally assessed using a high-throughput planar voltage-clamp technology (PatchXpress 7000A). Signal amplitudes were quantified at steady state during control (vehicle) treatment and in the presence of (i) a fixed concentration or (ii) increasing concentrations of the test article. Concentration-dependent changes of signal in response to the test article were expressed as percent block relative to control (predrug/−trigger) and are reported as the means ± standard errors of the means (SEM) of the indicated number of tested cells per wells. IC50s were determined where applicable by fitting the averaged concentration-response data (means ± SEM) with a Hill equation (12).

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