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In vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M. Cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM In vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs. Cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis.
| Cell Experiment | |
|---|---|
| Cell lines | Chinese hamster ovary cells |
| Preparation method | The effects of mosapride and cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Mosapride and cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 and 9.8 μM, respectively. |
| Concentrations | 9.8 μM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Dogs |
| Formulation | 10% gelatin solution |
| Dosages | 1mg/kg, 3mg/kg |
| Administration | p.o. |
| Molecular Weight | 465.95 |
| Formula | C23H29ClFN3O4 |
| CAS Number | 81098-60-4 |
| Solubility (25°C) | 20 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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