1991 年 6 巻 5 号 p. 781-792
Biotransformation of (4R)-3-benzoyl-N-[(1R)-1-phenylethyl]-4-thiazolidinecarboxamide (RS-0481), developed as a host mediated antitumor activator, was studied in rats and dogs. Twelve metabolites, M1 to M12, were isolated from urine, bile and plasma samples of rats or dogs after oral administration of RS-0481 or 14C-RS-0481 as a tracer. The structures of these metabolites were characterized by GC/EI/MS and 1H-NMR, and were comfirmed by comparison with corresponding authentic standards. The applicabilities of LC/APCI/MS for the identification of metabolites and the plausible metabolic pathways in these animals involving stereospecific oxidation of RS-0481 were also discussed.