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The 5-HT(4) agonists cisapride, mosapride, and CJ-033466, a Novel potent compound, exhibit different human ether-a-go-go-related gene (hERG)-blocking activities.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Toga, Tetsuo Kohmura, Yumi Kawatsu, Ryoichi |
| Copyright Year | 2007 |
| Abstract | The blocking effect of three 5-HT(4) 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-HT(4) 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. |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | https://www.jstage.jst.go.jp/article/jphs/105/2/105_2_207/_pdf |
| PubMed reference number | 17928736v1 |
| Volume Number | 105 |
| Issue Number | 2 |
| Journal | Journal of pharmacological sciences |
| Language | English |
| Access Restriction | Open |
| Subject Keyword | Adverse Event Associated with Cardiac Arrhythmia CJ 033466 Cisapride Etherum, ether, Homeopathic preparation KCNH2 gene Patch-Clamp Techniques mosapride |
| Content Type | Text |
| Resource Type | Article |