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Prucalopride (brand name Resolor) is a selective, high affinity 5-HT4 receptor agonist with Ki of 2.5 nM and 8 nM for 5-HT4A and 5-HT4B receptor, respectively. Prucalopride has >150-fold higher affinity for 5-HT4 receptors than for other receptors. Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (4 mg) significantly reduced the need for straining versus placebo (p < 0.05). In vitro data indicate that prucalopride has a low interaction potential, and therapeutic concentrations of prucalopride are not expected to affect the CYP-mediated metabolism of co-medicated medicinal products. Prucalopride significantly improved bowel function and reduced the severity of symptoms in patients with severe chronic constipation over 12 weeks.
| Molecular Weight | 367.87 |
| Formula | C18H26ClN3O3 |
| CAS Number | 179474-81-8 |
| Solubility (25°C) | DMSO 50 mg/mL Ethanol 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related 5-HT Receptor Products |
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| Tegaserod
Tegaserod is an orally active serotonin receptor 4 (5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. |
| cis-Urocanic acid
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is also an immune modulator that induces immunosuppression. |
| 5-HT2B antagonist-1
5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. |
| AS19
AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. |
| CP94253
CP94253 is a selective, orally active agonist for serotonin receptor 1B (5-HT1B), through competitive binding with iodocyanopindolol (ICP) to the 5-HT1 receptor. |
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