Prucalopride 5-HT Receptor agonist

Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. This compound (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. It induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve. [1]

Complete bowel movements per week are 30.9% of those receiving 2 mg of Prucalopride and 28.4% of those receiving 4 mg of this compound, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of this compound and 46.6% of those receiving 4 mg of it have an increase in the number of spontaneous, complete bowel movements of one or more per week, on average, as compared with 25.8% in the placebo group. This compound (2 mg or 4 mg) significantly improves all other secondary efficacy end points, including patients' satisfaction with their bowel function and treatment and their perception of the severity of their constipation symptoms. [2] It (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. This chemical (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying. [3] Higher proportions of patients on this compound 2 mg (19.5%), 4 mg (23.6%) have three or more spontaneous complete bowel movements (SCBM)/week compared with placebo (9.6%). It also significantly improves secondary efficacy and quality of life endpoints, including the proportion of patients with an increase of one or more SCBM/week, evacuation completeness, perceived disease severity and treatment effectiveness and quality of life. [4] This compound alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon and by inhibiting contractile activity in the distal colon of fasted dogs. It also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of this chemical, the first GMC generally occurs within the first half-hour after treatment. [5]