Prucalopride

Catalog No.S2875 Synonyms: R-93877

Prucalopride Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 170 In stock
USD 550 In stock
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1 Customer Review

  • 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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Biological Activity

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.
Targets
5-HT4A [1] 5-HT4B [1] 5-HT3 [1] 5-HT1A [1] 5-HT1B [1]
2.5 nM(Ki) 8 nM(Ki) 3.822 μM(Ki) >10 μM(Ki) >10 μM(Ki)
In vitro

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. [1]

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. [2] 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. [3] 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. [4] 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. [5]

Protocol

Solubility (25°C)

In vitro DMSO 60 mg/mL (163.1 mM)
Ethanol 38 mg/mL (103.29 mM)
Water <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 367.87
Formula

C18H26ClN3O3

CAS No. 179474-81-8
Storage powder
in solvent
Synonyms R-93877

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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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5-HT Receptor Signaling Pathway Map

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