Biotransformation in the monkey of cartazolate (SQ 65,396), a substituted pyrazolopyridine having anxiolytic activity

Abstract

1. The metabolism of cartazolate (SQ 65,396), an anxiolytic agent, was studied in four male rhesus monkeys after oral administration.

2. Seven metabolites were identified in the pooled urine of the four monkeys. These resulted from a combination of (1) hydrolysis of the 5-carboxylic acid ethyl ester; (2) N-deethylation of the pyrazole ring; (3) γ-hydroxylation of the n-butylamino side-chain; (4) removal of the n-butyl group; and (5) conjugation with β-glucuronic acid.