Tritium-labeled compound of a new benzodioxane derivative, 8-[(1, 4-benzodioxane-2-yl) methyl]-3-oxo-1-thia-4, 8-diazaspiro (4, 5) decane maleate (Y-3506), was administered to rats orally, intraperitonealy, intravenously or intramuscularly. About 50% and 40% of the administered radioactivity (
3H) were excreted in the urine and feces, respectively, by any route within 3 days. Following oral administration, 57% of the dose was also excreted in the bile during 24 hours. The highest concentration of
3H in most organs was found from 0.5 to 1 hour after oral administration, and the levels of
3H in the liver, adrenals, kidney, and serum were high, but those in the adipose tissue and brain were relatively low. Concentration of
3H in the adipose tissue was high in the case of intravenous administration. Protein binding of
3H in the serum was 15%. About 70% or more of
3H in the tissues other than the liver was attributable to S-oxide of Y-3506, one of the metabolites of Y-3506, and less than 20% to the unchanged Y-3506, 30 min after oral administration. On the other hand about 50% of
3H was found to exist as the unchanged compound in the blood and liver, 15 min after intravenous administration. Y-3506-S-oxide was identified as the major metabolite in 24-hour urine. Urinary excretion of the unchanged compound in the case of intravenous administration was more than that in the case of oral administration.
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