Prucalopride Succinate

Catalog No.S4247

Prucalopride Succinate Chemical Structure

Molecular Weight(MW): 485.96

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.

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Cited by 2 Publications

1 Customer Review

  • Prucalopride in the presence of IBMX on the S2/S1 ratio of electrically induced total tritium outflow. Tissues were stimulated twice (S1 and S2; 1 millisecond, 15 V, 4 Hz, 2 minutes); IBMX was added 36 minutes and prucalopride 15 minutes before S2. Mean S2/S1±SEM; one‐way ANOVA followed by Bonferroni corrected t test with ns not significant, *P<.05 and ***P<.001.

    Neurogastroenterol Motil, 2018, 30(2). Prucalopride Succinate purchased from Selleck.

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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

Solubility (25°C)

In vitro DMSO 97 mg/mL (199.6 mM)
Water 97 mg/mL (199.6 mM)
Ethanol 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 Information

Molecular Weight 485.96
Formula

C18H26ClN3O3.C4H6O4

CAS No. 179474-85-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03676374 Recruiting GERD Universitaire Ziekenhuizen Leuven December 2018 Phase 4
NCT03676374 Recruiting GERD Universitaire Ziekenhuizen Leuven December 2018 Phase 4
NCT03572790 Not yet recruiting Molecular Mechanisms of Pharmacological Action|Depression|Depressive Disorder|Mood Disorders|Mental Disorders|Antidepressive Agents|Cognition University of Oxford June 2018 Not Applicable
NCT03572790 Not yet recruiting Molecular Mechanisms of Pharmacological Action|Depression|Depressive Disorder|Mood Disorders|Mental Disorders|Antidepressive Agents|Cognition University of Oxford June 2018 Not Applicable
NCT02947269 Recruiting Postoperative Ileus|Colorectal Surgery|Postoperative Complications University of Auckland New Zealand October 25 2017 Phase 3
NCT03244553 Enrolling by invitation Ineffective Esophageal Motility|Dysphagia University of Calgary October 20 2017 Phase 2

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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.

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID