Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

5-HT4 receptor:140 nM(EC50), ERG channel (human):9.4 nM

Cisapride 独立于5-HT4受体激活，抑制血管Kv电流[2]。作为HERG通道阻滞剂，Cisapride 通过改变细胞周期分布并诱导凋亡，抑制胃癌细胞生长，具潜在胃癌治疗价值。Cisapride 能够以时间和剂量依赖的方式，通过HERG通道的特异性阻断抑制人类胃癌细胞系的生长和集落形成，而对GES细胞的影响较小[3]。

Cells in the logarithmic growth phase are harvested and seeded in 96-well plates. The cell number is diluted to 5000/well in 200 microliters of RPMI1640 medium. In vitro experiments are carried out on the gastric cancer cell lines and GES cell line, using an MTT proliferation assay. MTT stains live cells, and the optical density absorbance at 490 nM wavelength correlates with the cell number. Cisapride is added to the cells at concentrations of 0, 12.5, 25, 50, 100 or 200 nM and equivalent volume of ethanol is added as control in order to eliminate the effects of solvent. Twenty microliters of MTT is added to each well of the cell culture 4 h before termination of the culture at 37?C. One hundred and fifty microliters of dimethyl sulfoxide is added to each well at the end of the culture and the plate is agitated for 10 minutes. The absorbency at 490 nm is read by a BIOHIT BP800 plate reader. Growth curve is drawn according to MTT colorimetry. The inhibition rate is calculated.(Only for Reference)