In healthy male individuals, prucalopride decreases the display of esophageal acid and promotes gastric emptying. It is effective, safe and shows good tolerance for the treatment of men with chronic constipation.
Prucalopride is a selective 5-HT4 serotonin receptor agonist with enterokinetic activity. 5-HT4 receptors are GPCRs that are expressed in the CNS and peripheral tissues. The receptor has a role in GI motility disorders such as irritable bowel syndrome and idiopathic constipation. Agonists are prokinetic and of potential use for disoroders of reduced motility. Prucalopride is a selective 5-HT4 serotonin receptor agonist with enterokinetic activities. Prucalopride has pK(i) values of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively, and at least 290-fold selectivity for 5-HT4 over other serotonin and dopamine receptors.