Distribution of
35S-labeled 2-amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno-[2, 3-c]pyridine (
35S-Y-3642) in mice and rats was investigated. When this compound was given to mice, the highest tissue level of radioactivity was observed at after 30 minutes and radioactivity was highly distributed in the liver, brawn fat, Harderian gland, bile, gastrointestinal tract, and urine.
35S-Y-3642 was mainly distributed without debenzylation in mouse tissues with the exception of the lung, and more than 80% of radioactivity in the brain and brawn fat was found to be in unchanged form. When this compound was given to rats, tissue level of radioactivity increased slowly and was highly distributed in the liver, kidney, peripheral fat, lung, adrenals, and spleen. Almost all of radioactivity in the peripheral fat was identified as unchanged form, but most of radioactivity in other tissues of rats was debenzylated metabolites of
35S-Y-3642. These results revealed that
35S-Y-3642 absorbed from the administration sites was incorporated in the adipose tissue and then re-mobilized to other tissues, and that the debenzylated metabolites contributed to the anti-inflammatory actions of the original compound in rats. Binding with serum protein of
35S-Y-3642 and its radioactive metabolites was relativelv low and no remarkable accumulation of these compounds was observed in the carrageenin-induced edema of rats.
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