| Name | Prucalopride Succinate |
| Description | Prucalopride Succinate (Resolor Succinate) is a selective, high affinity 5-HT4 receptor agonist, inhibiting human 5-HT(4a) and 5-HT(4b) receptor with Ki value of 2.5 nM and 8 nM, respectively. |
| 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 89 mg/mL (183.1 mM)
DMSO : 90 mg/mL (185.2 mM)
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| Keywords | inhibit | 5-HT Receptor | Inhibitor | Serotonin Receptor | Prucalopride Succinate | 5-hydroxytryptamine Receptor | R108512 | Prucalopride | R 108512 |
| Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Trazodone hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
