Cisapride is a drug that increases motility in the upper gastrointestinal tract and is used as a Gastroprokinetic. It acts directly as a serotonin 5-HT4 receptor agonist and indirectly as a parasympathomimetic. It is also a potent human ether-à-go-go-related gene (hERG) potassium channel inhibitor. It showed higher inhibitory effects on a hERG current with IC50 of 9.4 × 10-9 M in vitro. It inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM. It could not bring about more colitis damages through 5HT(4) receptors. It was discovered by Janssen Pharmaceutica in 1980. It has been withdrawn from the market.
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