制癌剤1-(2-Tetrahydrofuryl)-5-fluorouracil(FT一207), の生体内運命(第3報)直腸内投与による吸収, 体内分布, 排泄および代謝

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In order to investigate the fate of 1-(2-tetrahydrofuryl)-5-fluorouracil (FT-207) in comparison with that of 5-fluorouracil tritiated FT-207 (^3H-FT-207) and 5-fluovouracil (^3H-5-fluorouracil)were administered from the rectum in normal and AH-130 tumor-bearing rats, and rapid absorption of ^3H-FT-207 or ^3H-5-fluorouracil, was observed. Blood level of radioactivity after rectal administration of ^3H-FT-207 was higher and more continuous than that of ^3H-5-fluorouracil. Although the radioactivity after rectal administration of ^3H-FT-207 and ^3H-5-fluovouracil was widely distributed in the various tissues of the animal with or without tumor, the highest concentration of the radioactivity was observed in the kidneys, and higher in tumor. The radioactivity in lymphatic gland reached a maximum level within 2-4 hr after the rectal administration of ^3H-FT-207 and declined very slowly. The urinary excretion of radioactivity within 24 hr was about 30% of the administered dose of ^3H-FT-207. More than 85% of the excreted radioactivity accounted for FT-207 and its metabolite, α-fluoro-β-alanine. Other metabolites such as 5-fluorouracil, α-fluoro-β-ureidopropionic acid and tritiated water were detected in small amounts in rat urine. The radioactivity in blood and tumor, 4 hr after rectal administration of ^3H-FT-207,was found to represent FT-207. However, the radioactivity in liver was due to the presence of α-fluoro-β-alanine. About 90% radioactivity in lymphatic gland within 2-6 hr after rectal administration of ^3H-FT-207 was detected as FT-207.
社団法人日本薬学会の論文
1975-06-25

制癌剤1-(2-Tetrahydrofuryl)-5-fluorouracil(FT一207), の生体内運命(第3報)直腸内投与による吸収, 体内分布, 排泄および代謝

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