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Chemical Compound Review

Prucalopride     4-amino-5-chloro-N-[1-(3- methoxypropyl)-4...

Synonyms: AC1MHJYO, PubChem22481, SureCN16952, CHEMBL117287, cc-249, ...
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Disease relevance of Prucalopride


High impact information on Prucalopride


Chemical compound and disease context of Prucalopride


Biological context of Prucalopride

  • Prucalopride (10 microM) significantly increased the action potential duration at 50% repolarization (APD50) from 12 +/- 2 to 17 +/- 3 ms (p < 0.05; n = 22 cells, 9 patients) [7].
  • Despite the deficit in synaptic transmission present in these mice, the percentage increase of the CA1 population spike induced by Prucalopride was the same as that observed in wild-type mice [10].
  • As it is intended for treatment of intestinal motility disorders, it is important to note that prucalopride is devoid of anti-cholinergic, anticholinesterase or nonspecific inhibitory activity and does not antagonise 5-HT(2A), 5-HT(2B) and 5-HT(3) receptors or motilin or CCK(1) receptors [11].
  • Prucalopride is a gastrointestinal prokinetic drug that acts through 5-HT4 receptors, but its potential effects on cardiac atrial function are unknown [12].

Anatomical context of Prucalopride


Associations of Prucalopride with other chemical compounds

  • The IC(50) value for prucalopride to block HERG (5.7 10(-6) M) was 20-fold higher than that of cisapride [15].
  • In constipation-predominant IBS the colokinetic effects of the selective 5HT4 agonists prucalopride and tegaserod are of great interest [16].

Gene context of Prucalopride

  • Hypomotility remains an attractive therapeutic target in IBS and the new generation of prokinetics includes several partial agonists at the 5-HT4 receptor, such as tegaserod (HTF-919) and prucalopride (R0-93877) [17].
  • To investigate the potential use of 5-HT(4) agonists in the treatment of AD, Prucalopride was applied to hippocampal slices from a transgenic mouse line that overexpresses the Abeta peptide [10].
  • Prucalopride did not cause relevant inhibition of 5-HT(2A), 5-HT(2B), or 5-HT(3), motilin or cholecystokinin (CCK(1)) receptor-mediated contractions, nor nicotinic or muscarinic acetylcholine receptor-mediated contractions, up to 10 microM [11].
  • We evaluate the tolerability and pilot efficacy of prucalopride in the treatment of CC due to SCL [14].
  • AIMS: Pilot study to compare the efficacy and tolerability of prucalopride and placebo in patients with severe CC referred to a tertiary centre [18].

Analytical, diagnostic and therapeutic context of Prucalopride


  1. Prucalopride accelerates gastrointestinal and colonic transit in patients with constipation without a rectal evacuation disorder. Bouras, E.P., Camilleri, M., Burton, D.D., Thomforde, G., McKinzie, S., Zinsmeister, A.R. Gastroenterology (2001) [Pubmed]
  2. The human serotonin 5-HT4 receptor regulates secretion of non-amyloidogenic precursor protein. Robert, S.J., Zugaza, J.L., Fischmeister, R., Gardier, A.M., Lezoualc'h, F. J. Biol. Chem. (2001) [Pubmed]
  3. Idiopathic constipation: too few stools and too little knowledge. Briejer, M.R., Schuurkes, J.A., Sarna, S.K. Trends Pharmacol. Sci. (1999) [Pubmed]
  4. Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans. Bouras, E.P., Camilleri, M., Burton, D.D., McKinzie, S. Gut (1999) [Pubmed]
  5. Frontocortical 5-HT4 receptors exert positive feedback on serotonergic activity: viral transfections, subacute and chronic treatments with 5-HT4 agonists. Lucas, G., Compan, V., Charnay, Y., Neve, R.L., Nestler, E.J., Bockaert, J., Barrot, M., Debonnel, G. Biol. Psychiatry (2005) [Pubmed]
  6. 5HT(4) agonists inhibit interferon-gamma-induced MHC class II and B7 costimulatory molecules expression on cultured astrocytes. Zeinstra, E.M., Wilczak, N., Wilschut, J.C., Glazenburg, L., Chesik, D., Kroese, F.G., De Keyser, J. J. Neuroimmunol. (2006) [Pubmed]
  7. Electrophysiological effects of prucalopride, a novel enterokinetic agent, on isolated atrial myocytes from patients treated with beta-adrenoceptor antagonists. Pau, D., Workman, A.J., Kane, K.A., Rankin, A.C. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  8. Review article: the complexity of drug development for irritable bowel syndrome. Kamm, M.A. Aliment. Pharmacol. Ther. (2002) [Pubmed]
  9. Treatment of GI dysmotility in scleroderma with the new enterokinetic agent prucalopride. Boeckxstaens, G.E., Bartelsman, J.F., Lauwers, L., Tytgat, G.N. Am. J. Gastroenterol. (2002) [Pubmed]
  10. Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease. Spencer, J.P., Brown, J.T., Richardson, J.C., Medhurst, A.D., Sehmi, S.S., Calver, A.R., Randall, A.D. Neuroscience (2004) [Pubmed]
  11. The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. Briejer, M.R., Bosmans, J.P., Van Daele, P., Jurzak, M., Heylen, L., Leysen, J.E., Prins, N.H., Schuurkes, J.A. Eur. J. Pharmacol. (2001) [Pubmed]
  12. Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants. Krobert, K.A., Brattelid, T., Levy, F.O., Kaumann, A.J. Naunyn Schmiedebergs Arch. Pharmacol. (2005) [Pubmed]
  13. 5-HT(4) receptors on cholinergic nerves involved in contractility of canine and human large intestine longitudinal muscle. Prins, N.H., Akkermans, L.M., Lefebvre, R.A., Schuurkes, J.A. Br. J. Pharmacol. (2000) [Pubmed]
  14. Efficacy and tolerability of prucalopride in patients with constipation due to spinal cord injury. Krogh, K., Jensen, M.B., Gandrup, P., Laurberg, S., Nilsson, J., Kerstens, R., De Pauw, M. Scand. J. Gastroenterol. (2002) [Pubmed]
  15. Gastrointestinal prokinetic drugs have different affinity for the human cardiac human ether-à-gogo K(+) channel. Potet, F., Bouyssou, T., Escande, D., Baró, I. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  16. New developments in the treatment of irritable bowel syndrome. De Schryver, A.M., Samsom, M. Scand. J. Gastroenterol. Suppl. (2000) [Pubmed]
  17. Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. De Ponti, F., Tonini, M. Drugs (2001) [Pubmed]
  18. Prucalopride is effective in patients with severe chronic constipation in whom laxatives fail to provide adequate relief. Results of a double-blind, placebo-controlled clinical trial. Coremans, G., Kerstens, R., De Pauw, M., Stevens, M. Digestion (2003) [Pubmed]
  19. Effect of different prokinetic agents and a novel enterokinetic agent on postoperative ileus in rats. De Winter, B.Y., Boeckxstaens, G.E., De Man, J.G., Moreels, T.G., Schuurkes, J.A., Peeters, T.L., Herman, A.G., Pelckmans, P.A. Gut (1999) [Pubmed]
  20. Effect of prucalopride, a new enterokinetic agent, on gastrointestinal transit and anorectal function in healthy volunteers. Poen, A.C., Felt-Bersma, R.J., Van Dongen, P.A., Meuwissen, S.G. Aliment. Pharmacol. Ther. (1999) [Pubmed]
  21. Prucalopride, a systemic enterokinetic, for the treatment of constipation. Emmanuel, A.V., Roy, A.J., Nicholls, T.J., Kamm, M.A. Aliment. Pharmacol. Ther. (2002) [Pubmed]
  22. Effects of prucalopride on colonic transit, anorectal function and bowel habits in patients with chronic constipation. Sloots, C.E., Poen, A.C., Kerstens, R., Stevens, M., De Pauw, M., Van Oene, J.C., Meuwissen, S.G., Felt-Bersma, R.J. Aliment. Pharmacol. Ther. (2002) [Pubmed]
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