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Prucalopride Succinate 5-HT Receptor agonist

Cat.No.S4247

Prucalopride(R-108512) is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.
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Quality Control

Batch: Purity: 99.89%
99.89

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (199.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 97 mg/mL

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 485.96 Formula

C18H26ClN3O3.C4H6O4

Storage (From the date of receipt)
CAS No. 179474-85-2 Download SDF Storage of Stock Solutions

Synonyms R-108512 SMILES COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl.C(CC(=O)O)C(=O)O

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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. 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. Prucalopride (0.1 μM) concentration-dependently increases the amplitude of submaximal cholinergic contractions and of acetylcholine release induced by electrical field stimulation in pig gastric circular muscle, and the effect is induced and enhanced IBMX (10 μM). Prucalopride (1 μM) significantly enhances the electrically induced cholinergic contractions in pig descending colon, and the facilitating effect is significantly enhanced by Rolipram.

In vivo

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.

References
  • [4] 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
NCT04759833 TERMINATED
Constipation
Takeda
2021-07-13 PHASE3

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