Metabolism of the non-narcotic analgesic, Wy-535

Abstract Hexahydro-1,3-dimethyl-4-phenylazepine-4- 14 C-carboxylic acid, ethyl ester (Wy-535), was administered to dogs and rats both orally and intramuscularly. Tissue levels were determined in the rat, and plasma levels as well as urinary and fecal excretion rates were determined in both species. The drug appeared to be well absorbed; significant plasma levels were found at 1 2 hr in both species after both routes of administration. It was well distributed to all organs studied and gave no evidence of any long-term retention in tissue. In addition to unchanged drug, three metabolites were excreted. These were, as anticipated from a previous study of the chemically related ethoheptazine, the products of N-demethylation and hydrolysis, namely, nor-Wy-535 and the de-esterified products of both Wy-535 and nor-Wy-535.