Prucalopride Succinate

China [CN]

I. Basic Information

Item | Details

English Name | Prucalopride Succinate; Motegrity/Resolor (Trade Name)

Chinese Name | Prucalopride Succinate

CAS No. | 741779-01-1 (Succinate); 179474-85-2 (Free Base)

Chemical Name | 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide succinate

Molecular Formula | Free Base C₁₈H₂₆ClN₃O₃; Succinate C₁₈H₂₆ClN₃O₃・C₄H₆O₄

Molecular Weight | Free Base 367.87; Succinate 485.96

Target | 5-hydroxytryptamine 4 (5-HT₄) receptor (Ki = 0.1 nM, selectivity > 150 times)

Developer | Janssen

Market Launch | 2009 (EU EMA); December 2012 (China NMPA); 2018 (US FDA)

Dosage Form and Strength | Film-coated tablets: 1mg, 2mg (calculated as prucalopride)

II. Physicochemical Properties

Parameter | Data (Succinate)

Appearance | White to off-white crystalline powder

Solubility | Easily soluble in water (approximately 100 mg/mL, 25℃), methanol, slightly soluble in ethanol, practically insoluble in diethyl ether, dichloromethane

Dissociation Constant (pKa) | 8.8 (piperidine amino), 9.5 (benzofuran amino) (predicted value)

Melting Point | 195-197℃ (decomposition)

Stability | Stable for 36 months at 25℃/60% RH, store in a sealed, cool, and dry place (20-25℃), avoid high temperature, light, and moisture

Chiral Characteristics | Contains 1 chiral center (piperidine 4-position), is a single R-isomer Configuration (active configuration), optical purity > 99.5%

Partition coefficient (logP): 2.8 (free base, predicted value)