Cisapride (CED0004489)

Cisapride is an exogenous solid with the formula C23H29ClFN3O4 and an average molecular weight of 465.94 g/mol. Cisapride belongs to the benzoic acids and derivatives, a subclass of benzene and substituted derivatives within the organic compounds. It is used as a gastrointestinal drug, an anti-ulcer drug, and a serotonergic agonist, with oral exposure being the recorded route. It has been found in propulsives within healthcare, pharmaceuticals, and veterinary products, as well as in electrical and electronic equipment including antennas, auxiliary devices, and electric hearing aids. The compound interacts with 13 recorded protein targets, including the Beta-1 adrenergic receptor (ADRB1), D(2) dopamine receptor (DRD2), D(1A) dopamine receptor (DRD1), 5-hydroxytryptamine receptor 3E (HTR3E), 5-hydroxytryptamine receptor 3A (HTR3A), the Voltage-gated inwardly rectifying potassium channel KCNH2, 5-hydroxytryptamine receptor 2A (HTR2A), and 5 other proteins. Cisapride acts through the stimulation of the serotonin 5-HT4 receptors (HTR4), which increases acetylcholine release in the enteric nervous system, specifically the myenteric plexus. This results in increased tone and amplitude of gastric contractions, especially antral, relaxation of the duodenal bulb and the pyloric sphincter, and increased peristalsis of the jejunum and duodenum, which results in accelerated intestinal transit and gastric emptying. In many countries, including Canada, cisapride has been withdrawn or has had its indications limited due to reports about long QT syndrome due to cisapride, which predisposes to arrhythmias. The FDA issued a warning letter regarding this risk to patients and health care professionals.