Journal
JOURNAL OF PHARMACOLOGICAL SCIENCES
Volume 105, Issue 2, Pages 207-210Publisher
JAPANESE PHARMACOLOGICAL SOC
DOI: 10.1254/jphs.SC0070243
Keywords
human ether-a-go-go-related gene (hERG); 5-HT4 agonist; patch-clamp
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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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