Abstract
The biliary and urinary metabolites of a new morpholine derivative Y-8894 were investigated in rats and rabbits after oral administration of Y-8894.
Unchanged Y-8894 and eight metabolites were purified and isolated using an Amberlite XAD-2 resin column, preparative thin-layer chromatography and high pressure liquid chromatography. The structures of these metabolites were identified by their mass, infrared and nuclear magnetic resonance spectra.
The major metabolic pathways of Y-8894 in rats and rabbits are considered to be as follows: a) hydroxylation of phenyl ring and successively oxidation of morpholine ring, b) hydroxylation of thiophene and N atom of morpholine ring, and these hydroxylated derivatives were excreted in urine or bile mainly as glucuronides, c) opening of thiophene ring and sulphoconjugation at N atom of morpholine ring.
