Prucalopride

Catalog No.S2875 Synonyms: R-93877

For research use only.

Prucalopride (R-93877) 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 Chemical Structure

CAS No. 179474-81-8

Selleck's Prucalopride has been cited by 5 Publications

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Biological Activity

Description Prucalopride (R-93877) 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]
2.5 nM(Ki) 8 nM(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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 367.87
Formula

C18H26ClN3O3

CAS No. 179474-81-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04838522 Recruiting Other: No Intervention Chronic Constipation Takeda December 31 2021 --
NCT04429802 Completed Drug: Prucalopride|Drug: Placebo Gastrointestinal Motility Disorder|Dyspepsia Universitaire Ziekenhuizen Leuven September 26 2013 Not Applicable
NCT01807000 Completed Drug: Radiolabeled Prucalopride Succinate Healthy Shire|Takeda March 18 2013 Phase 1
NCT01692132 Withdrawn Drug: Prucalopride Chronic Constipation Janssen Pharmaceutica February 2013 --
NCT03279341 Completed Drug: polyethylene glycol|Drug: Bisacodyl|Drug: Prucalopride Chronic Constipation University Hospital Gasthuisberg December 3 2012 Phase 4
NCT01117051 Terminated Drug: placebo|Drug: prucalopride Non-cancer Pain|Opioid Induced Constipation Shire|Takeda May 19 2010 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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