Prucalopride Succinate

Catalog No.S4247

For research use only.

Prucalopride 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.

Prucalopride Succinate Chemical Structure

CAS No. 179474-85-2

Selleck's Prucalopride Succinate has been cited by 4 Publications

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Biological Activity

Description Prucalopride 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.
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] 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). [2] Prucalopride (1 μM) significantly enhances the electrically induced cholinergic contractions in pig descending colon, and the facilitating effect is significantly enhanced by Rolipram. [3]

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. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 97 mg/mL
(199.6 mM)
Water 97 mg/mL
(199.6 mM)
Ethanol Insoluble

Chemical Information

Molecular Weight 485.96
Formula

C18H26ClN3O3.C4H6O4

CAS No. 179474-85-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl.C(CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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