The Biotransformation of 3-(γ-Morpholino-β-3′,4′,5′-trimethoxybenzoxypropyl)-4-methyl-7,8-dimethoxy- coumarin hydrochloride in the Rabbit

Abstract

1. Following single oral doses (50 mg/kg) of 3-(γ-morpholino-β-3′,4′,5′-trimethoxybenzoxypropyl)-4-methyl-7,8-dimethoxy[4-¹⁴C]courmarin hydrochloride (ABBOTT-37624) to female New Zealand white rabbits, the major metabolite found in urine and faeces was the 7-O-demethylated, de-esterified compound (54.9% of dose). Another major fraction consisted of polar compounds, evenly distributed between urine and faeces (14.8% and 14.3% of dose respectively). Trace amounts of parent compound and the product of its de-esterification were found in rabbit faeces.

2. Glucuronide formation appears to be the principal form of conjugation of the metabolites in this species.