Structural Determination of Rat and Dog Urinary Metabolites of a New Antidepressant RS-8359

Haruo IWABUCHI, Wataru TAKASAKI, Harumitsu KUWANO, Takashi KOBAYASHI, Yorihisa TANAKA
1998 Drug Metabolism and Pharmacokinetics  
RS-8359 is a selective and reversible inhibitor of A type monoamine oxidase. In order to eluci date the metabolism of RS-8359, the metabolites were isolated from the urine after oral administration to rats and dogs. The chemical structures of the seven isolated metabolites, including the unchanged form, were determined by NMR and mass spectrometry. Hydroxylation on the cyclopentanol moiety and oxidation on the pyrimidine moiety of the molecule were preferentially responsible for the phase I
more » ... bolism. The ten tative main metabolic pathways of RS-8359 in the rat and dog are proposed and discussed.
doi:10.2133/dmpk.13.351 fatcat:mboqtqfzwje5dh3i7ke6347apy