Prucalopride

SKU: orb1305339

Description

Prucalopride (R-93877) is a potent and selective agonist for the 5-HT4A and 5-HT4B receptors, exhibiting over 290-fold selectivity versus other 5-HT subtypes. It is widely used in gastrointestinal motility research, including in vitro receptor studies and in vivo models of colonic dysmotility and constipation.

Research Area

Cell Biology, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 179474-81-8
• MW: 367.87
• Purity: 99.99%
• Formula: C₁₈H₂₆ClN₃O₃
• SMILES: COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(N)c2CCOc12
• Target: 5-HT Receptor,Apoptosis,Autophagy
• Solubility: DMSO:56 mg/mL (152.23 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:36 mg/mL (97.86 mM)

Bioactivity

• Target IC50:
  5-HT4A:2.5 nM(Ki)|5-HT4B:8 nM(Ki)
• In Vivo:
  Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea pig's proximal colon following electrical stimulation. It induces contractions in a concentration-dependent manner (pEC50: 7.5). Additionally, Prucalopride induces relaxation in the muscularis mucosae of the rat esophagus (pEC50: 7.8), demonstrating a monophasic concentration-response curve.
• In Vitro:
  Administration of prucalopride at dosages of 2/4 mg resulted in complete spontaneous bowel movements per week at rates of 30.9% and 28.4%, respectively, compared to 12.0% in the placebo group. Patients treated with 2 mg of prucalopride (47.3%) and those receiving 4 mg (46.6%) experienced an increase in the frequency of spontaneous bowel movements, with an average of one or more complete bowel movements per week, versus 25.8% in the placebo group. Prucalopride (2/4 mg) significantly enhanced other secondary efficacy endpoints, including patient satisfaction with their bowel functions and treatment, as well as their perception of the severity of constipation symptoms. At a dosage of 4 mg/day, prucalopride accelerated overall gastric emptying and small intestinal transit without causing intestinal evacuation disorders. It also sped up overall colonic transit and increased the colonic emptying rate.

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

pseudo-intestinal obstruction, Prucalopride, Serotonin Receptor, R 93877, R-93877, R93877, chronic constipation, A427, A549, 5-HT Receptor, 5-HT4A, 5-HT4B, 5HTReceptor, 5HT Receptor, 5-hydroxytryptamine Receptor, Inhibitor, Lung cancer, inhibit

Compound Identifiers

PubChem CID

3052762