Metabolism of RS-0481, a New Host Mediated Antitumor Activator. (1): Identification of Metabolites in Rat and Dog.
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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, M<SUB>1</SUB> to M<SUB>12</SUB>, were isolated from urine, bile and plasma samples of rats or dogs after oral administration of RS-0481 or <SUP>14</SUP>C-RS-0481 as a tracer. The structures of these metabolites were characterized by GC/EI/MS and <SUP>1</SUP>H-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.
- 日本薬物動態学会の論文
日本薬物動態学会 | 論文
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