Catalog No.S2875 Synonyms: R-93877
Molecular Weight(MW): 367.87
Prucalopride is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
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Concentration-dependent facilitation by prucalopride of electrically induced submaximal cholinergic contractions. Influence of 0.003, 0.01 and 0.03 μmol/L prucalopride, administered to separate strips (A-C) and of 0.3 nmol/L to 1 μmol/L prucalopride, added cumulatively (D-F) on submaximal electrically induced cholinergic contractions at V50% (10 seconds trains at 4 Hz [fundus] or 8 Hz [jejunum and colon], 0.5 milliseconds, interval of 5 [fundus and colon] or 10 minutes [jejunum]) in murine fundus (A,D), jejunum (B,E) and colon (C,F). Contractions are expressed as percentage of the mean of the five contractions before adding prucalopride. Experiments were performed in the continuous presence of 4 μmol/L guanethidine, 300 μmol/L l-NAME and for colon also 1 μmol/L MRS 2500. Means±SEM; ns not significant, *P<.05, **P<.01, ***P<.001 vs control (one-way ANOVA with Bonferroni corrected t test)
Neurogastroenterol Motil, 2017. Prucalopride purchased from Selleck.
Comparison of gastrointestinal transit tracked over 12 h for animals treated with different concentrations of loperamide, prucalopride, and for DMSO-treated/control animals (dotted line) at 4 h (black), 9 h (light grey), and 12 h (dark grey) (n = 6-13 animals per group). (A) Transit scores for 6 solid beads, and (B) Location of the leading bead. Transit scoring is detailed in Table 1. Asterisks indicate the significance of each treatment relative to controls (*p < 0.05; **p < 0.01). Data show mean ± SEM.
Neurogastroenterol Motil, 2016, 28(8):1241-51.. Prucalopride purchased from Selleck.
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|Description||Prucalopride is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.|
Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve. 
|In vivo||Complete bowel movements per week is 30.9% of those receiving 2 mg of Prucalopride and 28.4% of those receiving 4 mg of Prucalopride, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of Prucalopride and 46.6% of those receiving 4 mg of Prucalopride has 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. Prucalopride (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.  Prucalopride (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. Prucalopride (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying.  Higher proportions of patients on prucalopride 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). Prucalopride 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.  Prucalopride 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. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment. |
-  Briejer MR, et al. Eur J Pharmacol, 2001, 423(1), 71-83.
-  Camilleri M, et al. N Engl J Med, 2008, 358(22), 2344-2354.
-  Bouras EP, et al. Gastroenterology, 2001, 120(2), 354-360.
|In vitro||DMSO||60 mg/mL (163.1 mM)|
|Ethanol||38 mg/mL (103.29 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02947269||Not yet recruiting||Postoperative Ileus|Colorectal Surgery|Postoperative Complications||University of Auckland, New Zealand||January 2017||Phase 3|
|NCT02806206||Not yet recruiting||Gastrointestinal Hemorrhage|Crohn Disease|Celiac Disease|Intestinal Diseases|Inflammatory Bowel Diseases||University of British Columbia||July 2016||Phase 4|
|NCT02781493||Not yet recruiting||Prucalopride Plus Polyethylene Glycol in Bowel Preparation for Colonoscopyp||Shandong University|Binzhou Peoples Hospital|Taian Peoples Hospital|Linyi Peoples Hospital||June 2016||Phase 4|
|NCT02538367||Completed||Functional Constipation||Yuhan Corporation||August 2015||Phase 1|Phase 2|
|NCT02228616||Completed||Constipation||Xian-Janssen Pharmaceutical Ltd.||October 2014||Phase 4|
|NCT02425774||Recruiting||Postoperative Ileus||Katholieke Universiteit Leuven|Universitaire Ziekenhuizen Leuven||July 2014||Phase 4|
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