Prucalopride

Catalog No.S2875

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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Prucalopride Chemical Structure

Prucalopride Chemical Structure
Molecular Weight: 367.87

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Related Compound Libraries

Prucalopride is available in the following compound libraries:

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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]

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IC50 2.5 nM(Ki) 8 nM(Ki) 3.822 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Binding assay Membrane fractions from cells or from tissue homogenates are incubated with a radioactively labelled ligand with high affinity for a particular receptor. Specific receptor binding of the radioligand is distinguished from the nonspecific labelling by addition of an excess of an unlabelled compound, known to compete with the radioligand for binding to the receptor sites. The remaining nonspecific labelling is subtracted from total binding values obtained without the competitor. To determine the receptor binding affinity of unlabelled prucalopride, the ligand is added at various concentrations to the incubation mixture. Following an incubation period necessary to reach equilibrium at a given temperature, the membranes are harvested by rapid filtration and filters are placed in counting vials, 2 mL of Ultima Gold MV are added and filter-bound radioactivity is counted after shaking and resting in a Packard liquid scintillation counter.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Briejer MR, et al. Eur J Pharmacol, 2001, 423(1), 71-83.

[2] Camilleri M, et al. N Engl J Med, 2008, 358(22), 2344-2354.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
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 People  ...more Shandong University|Binzhou Peoples Hospital|Taian Peoples Hospital|Linyi Peoples Hospital June 2016 Phase 4
NCT02538367 Recruiting Functional Constipation Yuhan Corporation August 2015 Phase 1|Phase 2
NCT02228616 Recruiting Constipation Xian-Janssen Pharmaceutical Ltd. October 2014 Phase 4
NCT02425774 Recruiting Postoperative Ileus Katholieke Universiteit Leuven|Universitaire Ziekenhuizen  ...more Katholieke Universiteit Leuven|Universitaire Ziekenhuizen Leuven July 2014 Phase 4

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Chemical Information

Download Prucalopride SDF
Molecular Weight (MW) 367.87
Formula

C18H26ClN3O3

CAS No. 179474-81-8
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms R-93877
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 Name 7-Benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-

Tech Support

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