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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related 5-HT Receptor Products |
|---|
| TC-2153
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP). TC-2153 also inhibits 5-HT2A receptor-mediated signaling. |
| Gentisein
Gentisein (NSC-329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM. |
| MM120
MM120 is a synthetic tryptamine that is also a partial agonist at the 5-hydroxytryptamine 2A (5-HT2A) receptor. It can be used in studies related to GAD and attention deficit hyperactivity disorder (ADHD). |
| SB 258741 hydrochloride
SB 258741 hydrochloride is a specific 5-HT7 receptor antagonist for schizophrenia. |
| 5-HT1A antagonist 1
5-HT1A antagonist 1 is a potent and selective 5-HT1A receptor antagonist with a Ki value of 35 nM.5-HT1A antagonist 1 can be used in the study of central nervous system disorders. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
