Journal of Pharmacological Sciences
Online ISSN : 1347-8648
Print ISSN : 1347-8613
ISSN-L : 1347-8613
Short Communications
The 5-HT4 Agonists Cisapride, Mosapride, and CJ-033466, a Novel Potent Compound, Exhibit Different Human Ether-a-go-go-Related Gene (hERG)-Blocking Activities
Tetsuo TogaYumi KohmuraRyoichi Kawatsu
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2007 Volume 105 Issue 2 Pages 207-210

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Abstract

The blocking effect of three 5-HT4 agonists, cisapride, mosapride, and the newly discovered CJ-033466 on the human ether-a-go-go-related gene (hERG) channel was studied using a whole cell patch-clamp technique in HEK293 cells. Cisapride was found to be the most potent of the hERG blockers. CJ-033466 had the widest safety margin between its hERG blocking activity and 5-HT4 agonism among the tested compounds. This suggests a lower clinical risk of cardiac arrhythmia in CJ-033466 compared with the other 2 agonists. Therefore, CJ-033466 has the potential to be a drug with higher therapeutic efficacy and less cardiac risk than both cisapride and mosapride.

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© The Japanese Pharmacological Society 2007
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