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Prucalopride 5-HT Receptor agonist

Cat.No.S2875

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, and exhibits >290-fold selectivity against other 5-HT receptor subtypes.
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Quality Control

Batch: Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (201.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 74 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 367.87 Formula

C18H26ClN3O3

Storage (From the date of receipt)
CAS No. 179474-81-8 Download SDF Storage of Stock Solutions

Synonyms R-93877 SMILES COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl

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Mechanism of Action

Targets/IC50/Ki
5-HT4A
2.5 nM(Ki)
5-HT4B
8 nM(Ki)
In vitro
Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. This compound (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. It 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 this compound, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of this compound and 46.6% of those receiving 4 mg of it 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. This compound (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. It (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. This chemical (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying. Higher proportions of patients on this compound 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). It 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. This compound 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. It also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of this chemical, the first GMC generally occurres within the first half-hour after treatment.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/18987031/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11696108/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-08-11)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06883175 RECRUITING
Dysphagia; Achalasia, Esophageal; Ineffective Esophageal Motility
Northwestern University
2024-09-01
NCT05455359 RECRUITING
Esophageal Motility Disorders; Gastric Motor Dysfunction; Aspiration Pneumonia; Gastro Esophageal Reflux
Boston Children's Hospital
2025-02-13 PHASE4
NCT06474286 NOT_YET_RECRUITING
Schizophrenia
University of Pittsburgh
2026-07-31
NCT07127237 NOT_YET_RECRUITING
Bowel Preparation
Hospital de Clínicas Dr. Manuel Quintela
2025-09 EARLY_PHASE1
NCT06816407 RECRUITING
Post-Op Complication
Future University in Egypt
2025-03-02 PHASE3
NCT05220228 COMPLETED
Depression in Remission
University of Oxford
2022-01-04

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