1998 Volume 13 Issue 4 Pages 351-361
RS-8359 is a selective and reversible inhibitor of A type monoamine oxidase. In order to elucidate 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 metabolism. The tentative main metabolic pathways of RS-8359 in the rat and dog are proposed and discussed.