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Cisapride-d6 is intended for use as an internal standard for the quantification of cisapride (Item No. 21657) by GC- or LC-MS. Cisapride is an agonist of serotonin (5-HT) receptor subtype 5-HT4 (IC50 = 0.483 μM in COS-7 cells expressing the human receptor).1 It induces relaxation of precontracted isolated rat esophageal thoracic muscularis mucosae preparations (EC50 = 102.33 nM). Cisapride (0.5 mg/kg) increases the rate of gastric emptying in rats. It is also a human ether-a-go-go related gene (hERG) channel blocker that binds to hERG channels with an IC50 value of less than 1 μM in a fluorescence polarization assay. Formulations containing cisapride have previously been used in the treatment of nocturnal heartburn associated with gastroesophageal reflux disease.
WARNING This product is not for human or veterinary use.
1. Discovery and SAR of N-