Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is also an hERG blocker with an IC50 value of 9.4 nM. It functions as a gastroprokinetic agent, stimulating gastrointestinal motor activity[1][2][3][4].
体内研究
Cisapride (0.1-1 mg/kg; i.v., once) enhances antral and colonic motility in conscious dogs[3].
Cisapride (2 mg/kg (i.p.); 4 mg/kg, (oral administration); once) does not exhibit significant differences in macroscopic features, histopathological features, cytokine profile, or bodyweight changes compared to TNBS-treated rats[4].
体外研究
Cisapride (1-100 nM) exhibits potent hERG blockade with an IC50 value of 9.4 nM[1].
Cisapride (1-100 nM) demonstrates efficacy at the 5-HT4 receptor with an EC50 value of 140 nM[1].
Cisapride demonstrates dose-dependent inhibition of Kv4.3 potassium channels expressing CHO cells, with an IC50 value of 9.8 μM, across concentrations of 0.3, 1, 3, 10, and 30 μM[2].
Cisapride/西沙必利 细胞实验
Cell Line
Concentration
Treated Time
Description
References
human liver microsomes
5 μM
30 min
To investigate the metabolism pathways and major metabolites of cisapride. Results showed that cisapride is primarily metabolized by CYP3A4, forming the major metabolite norcisapride.
Br J Pharmacol. 2000 Apr;129(8):1655-67
Rat proximal colon mucosa-submucosa or mucosa-only preparations
100 μM
To investigate the effects of luminal 5-HT on colonic anion secretion, it was found that luminal 5-HT increased HCO3− secretion via 5-HT4 receptor activation, and was not affected by TTX or atropine.
Evaluate the inhibitory effect of Cisapride on hERG channels, IC50 value was 938 nM
Br J Pharmacol. 2016 Oct;173(19):2819-32
HEK293 cells
0.1, 0.3, 1, 3, 10, 30, 100 nM
Evaluate the inhibitory effect of Cisapride on hERG channels, IC50 value was 6.8 nM
Br J Pharmacol. 2016 Oct;173(19):2819-32
iPSC-derived cardiomyocytes
0.1 μM, 1 μM, 10 μM, 100 μM
24 h
To evaluate the effects of cisapride on calcium flux and QT prolongation in cardiomyocytes. Results showed that cisapride induced changes in calcium flux, manifested as QT prolongation, with some cells exhibiting Torsade's-like arrhythmias.
ALTEX. 2018;35(4):441-452
Oocytes expressing HERG channels
0.133 µM
To study the blocking effect of Cisapride on HERG channels, showing an IC50 of 0.133 µM.
Proc Natl Acad Sci U S A. 2000 Oct 24;97(22):12329-33
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