Chemical Property of Prucalopride
Chemical Property:
- Vapor Pressure:2E-09mmHg at 25°C
- Melting Point:90.7°
- Refractive Index:1.599
- Boiling Point:481.369 °C at 760 mmHg
- PKA:13.65±0.20(Predicted)
- Flash Point:244.923 °C
- PSA：76.82000
- Density:1.286 g/cm3
- LogP:2.99780
- Storage Temp.:2-8°C
- XLogP3:2
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:6
- Exact Mass:367.1662694
- Heavy Atom Count:25
- Complexity:445
- Purity/Quality:
-
99% *data from raw suppliers
Prucalopride 99% *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Gastrointestinal Agents
- Canonical SMILES:COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
- Recent ClinicalTrials:A Study of Prucalopride For Functional Constipation in Children and Teenagers
- Recent EU Clinical Trials:Characterization of nerve-modulated macrophage population in the gastrointestinal tract
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Description
Prucalopride is a potent and selective agonist of the serotonin (5-HT) receptor subtype 5-HT4 (Kis = 2.5 and 8 nM for human 5-HT4A and 5-HT4B, respectively). Prucalopride is greater than 250-fold selective for 5-HT4 over a panel of 53 overexpressed receptors, including 5-HT subtypes, but does bind to human dopamine D4 and sigma-1 (σ1) receptors and mouse 5-HT3 receptors (Kis = 2.3, 3.7, and 3.8 μM, respectively). It induces contractions in guinea pig colon with an EC50 value of 33 nM, an effect that is blocked by the 5-HT4 antagonist GR113808 but not the 5-HT2A and 5-HT3 antagonists ketanserin and granisetron , respectively. It also facilitates non-cholinergic contractions induced by electrical stimulation. In fasted dogs, oral administration of prucalopride increases colonic motility by inhibiting distal colon contractions (ED50 = 0.04 mg/kg), an effect that is blocked by pretreatment with the 5-HT4 antagonist GR125487. Prucalopride (5-10 mg/kg, s.c.) increases acetylcholine and histamine levels in the rat prefrontal cortex by 2.4-fold and 3-fold, respectively, and increases the power of hippocampal theta oscillations. Formulations containing prucalopride have been used in the treatment of chronic idiopathic constipation.
