Home Neuronal Signaling 5-HT Receptor agonist Prucalopride Succinate For research use only.

Prucalopride Succinate

Synonyms: R-108512

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.

Prucalopride Succinate Chemical Structure

Prucalopride Succinate Chemical Structure

CAS No. 179474-85-2

Purity & Quality Control

Prucalopride Succinate Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description 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.
Targets
5-HT4A [1] 5-HT4B [1]
2.5 nM(Ki) 8 nM(Ki)
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04838522 Recruiting
Chronic Constipation
Takeda|UC San Diego Human Milk Research Biorepository
 March 2 2022 --
NCT04429802 Completed
Gastrointestinal Motility Disorder|Dyspepsia
Universitaire Ziekenhuizen KU Leuven
 September 26 2013 Not Applicable
NCT01807000 Completed
Healthy
Shire|Takeda
 March 18 2013 Phase 1
NCT01692132 Withdrawn
Chronic Constipation
Janssen Pharmaceutica
 February 2013 --
NCT03279341 Completed
Chronic Constipation
University Hospital Gasthuisberg
 December 3 2012 Phase 4
NCT01117051 Terminated
Non-cancer Pain|Opioid Induced Constipation
Shire|Takeda
 May 19 2010 Phase 3

Chemical Information & Solubility

Molecular Weight 485.96 Formula

C18H26ClN3O3.C4H6O4
CAS No. 179474-85-2 SDF Download Prucalopride Succinate SDF
Smiles COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl.C(CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (199.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 97 mg/mL

Ethanol : Insoluble


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In vivo
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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.

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