Constipation, IBS and the 5-HT4 receptor: What role for prucalopride? Academic Article uri icon


MeSH Major

  • Gastroenterology
  • Societies, Medical


  • After the problems associated with the non-selective 5-HT4 receptor agonists cisapride and tegaserod, the 5-HT4 receptor is now beginning to come in from the cold. Thus, prucalopride is now the first of a new class of drug defined by selectivity and high intrinsic activity at the 5-HT4 receptor. Prucalopride has been developed for treatment of chronic constipation rather than constipation-predominant irritable bowel syndrome (IBS). This follows the trend of first evaluating new gastrointestinal (GI) prokinetic drugs in disorders where disrupted GI motility is known to exist, rather than in a functional bowel disorder where changes in motility are uncertain. If prucalopride is not progressed towards the IBS indication, it has at least shown the way for other selective 5-HT4 receptor agonists. Most notable among these is TD-5108 (velusetrag), also characterized by good selectivity at the 5-HT4 receptor, high intrinsic activity and efficacy in patients with chronic constipation.

publication date

  • January 2010



  • Academic Article


Digital Object Identifier (DOI)

  • 10.4137/CGast.S4136

Additional Document Info

start page

  • 21

end page

  • 33


  • 3