For research use only.
Catalog No.S2875 Synonyms: R-93877
CAS No. 179474-81-8
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, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
Selleck's Prucalopride has been cited by 5 publications
2 Customer Reviews
Concentration-dependent facilitation by prucalopride of electrically induced submaximal cholinergic contractions. Influence of 0.003, 0.01 and 0.03 μmol/L prucalopride, administered to separate strips (A-C) and of 0.3 nmol/L to 1 μmol/L prucalopride, added cumulatively (D-F) on submaximal electrically induced cholinergic contractions at V50% (10 seconds trains at 4 Hz [fundus] or 8 Hz [jejunum and colon], 0.5 milliseconds, interval of 5 [fundus and colon] or 10 minutes [jejunum]) in murine fundus (A,D), jejunum (B,E) and colon (C,F). Contractions are expressed as percentage of the mean of the five contractions before adding prucalopride. Experiments were performed in the continuous presence of 4 μmol/L guanethidine, 300 μmol/L l-NAME and for colon also 1 μmol/L MRS 2500. Means±SEM; ns not significant, *P<.05, **P<.01, ***P<.001 vs control (one-way ANOVA with Bonferroni corrected t test)
Neurogastroenterol Motil, 2017, doi: 10.1111/nmo.13064. Prucalopride purchased from Selleck.
Comparison of gastrointestinal transit tracked over 12 h for animals treated with different concentrations of loperamide, prucalopride, and for DMSO-treated/control animals (dotted line) at 4 h (black), 9 h (light grey), and 12 h (dark grey) (n = 6-13 animals per group). (A) Transit scores for 6 solid beads, and (B) Location of the leading bead. Transit scoring is detailed in Table 1. Asterisks indicate the significance of each treatment relative to controls (*p < 0.05; **p < 0.01). Data show mean ± SEM.
Neurogastroenterol Motil, 2016, 28(8):1241-51.. Prucalopride purchased from Selleck.
Purity & Quality Control
Choose Selective 5-HT Receptor Inhibitors
|Description||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, exhibits >290-fold selectivity against other 5-HT receptor subtypes.|
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. 
|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 Prucalopride, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of Prucalopride and 46.6% of those receiving 4 mg of Prucalopride 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. Prucalopride (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.  Prucalopride (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. Prucalopride (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying.  Higher proportions of patients on prucalopride 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). Prucalopride 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.  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. |
-  Briejer MR, et al. Eur J Pharmacol, 2001, 423(1), 71-83.
-  Camilleri M, et al. N Engl J Med, 2008, 358(22), 2344-2354.
-  Bouras EP, et al. Gastroenterology, 2001, 120(2), 354-360.
|In vitro||DMSO||60 mg/mL (163.1 mM)|
|Ethanol||38 mg/mL (103.29 mM)|
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04838522||Recruiting||Other: No Intervention||Chronic Constipation||Takeda||September 30 2021||--|
|NCT04429802||Completed||Drug: Prucalopride||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|
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.