Prucalopride , ≥99% , 179474-81-8
Synonym(s):
4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide
CAS NO.：179474-81-8
Empirical Formula: C18H26ClN3O3
Molecular Weight: 367.87
MDL number: MFCD09837787
EINECS: 1312995-182-4
| Pack Size | Price | Stock | Quantity |
| 10MG | RMB445.60 | In Stock |
|
| 50MG | RMB576.00 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 90.7° |
| Boiling point: | 481.4±45.0 °C(Predicted) |
| Density | 1.28 |
| storage temp. | 2-8°C |
| solubility | DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml; DMSO: 10 mg/ml; Ethanol: 10 mg/ml |
| pka | 13.65±0.20(Predicted) |
| form | powder |
| color | white to beige |
| InChI | InChI=1S/C18H26ClN3O3/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14/h11-12H,2-10,20H2,1H3,(H,21,23) |
| InChIKey | ZPMNHBXQOOVQJL-UHFFFAOYSA-N |
| SMILES | O1C2=C(C(NC3CCN(CCCOC)CC3)=O)C=C(Cl)C(N)=C2CC1 |
Description and Uses
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.
Safety
| Symbol(GHS) |   GHS07,GHS09 |
| Signal word | Warning |
| Hazard statements | H315-H319-H335-H400 |
| Precautionary statements | P273-P302+P352-P305+P351+P338 |
| RIDADR | UN 3077 9 / PGIII |
