METABOLIC FATE OF TE-031 (A-56268)(IV):METABOLISM OF <SUP>14</SUP>C-TE-031 IN RATS AND DOGS
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Five metabolites, N-demethyl TE-031 (M-1), N, N-didemethyl TE-031 (M-2), TE-031 N-oxide (M-3), decladinosyl TE-031 (M-4) and (14 R)-14-hydroxy TE-031 (M-5) as well as unchanged TE-031 were found in urine after oral administration to dogs. The concentration of TE-031 in plasma was considerably higher in rats than in dogs, and systemic availability in rats and dogs was 20.8% and 79.1%. Both plasma and principal tissues contained mainly unchanged TE-031, followed by M-1.<BR>The ratio of unchanged TE-031 to the total radioactivity was highest in lung, namely c. 70%, but was low in plasma and liver. In urine, roughly equal amounts of unchanged TE- 031 and M- 1 were found, and small amounts of other metabolites were also detected in both species. On the other hand, M-1 was the main metabolite both in bile and feces.
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