Bioassay法による制癌剤 N<SUB>1</SUB>-(2-Tetrahydrofuryl)-5-fluorouracil (FT-207) の体内分布, 排泄, 代謝

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  • DISTRIBUTION, EXCRETION AND METABOLISM OF N<SUB>1</SUB>-(2-TETRAHYDROFURYL)-5-FLUOROURACIL (FT-207) BY A BIOASSAY METHOD
  • Bioassayホウ ニ ヨル セイガンザイ N1- 2-Tetrahydrofuryl 5 fluorouracil FT-207 ノ タイナイ ブンプ , ハイセツ , タイシャ

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N1-(2-Tetrahydrofuryl)-5-fluorouracil (FT-207), a new antimetabolic anticancer agent synthesized in USSR, was studied on antimicrobial activity in vitro and distribution, excretion and metabolism in vivo.<BR>The results obtained were as follows.<BR>1) Antimicrobial activity<BR>FT-207 showed fairly active against Micrococcus flavus ATCC 10240, Sarcina lutea PCI 1001, Staphylococcus epidermidis and Staphylococcus aureus 209 P, but in general the activity was inferior to that of 5-FU.<BR>2) Distribution<BR>By the intravenous administration of FT-207, 400mg/kg, in normal and AH-130 bearing rats, the concentration of FT-207 in serum and tissues maintained measurably until 16-24 hours.<BR>On the other hand, the active substances (5-FU, etc.) from FT-207 detected at 1-4 hours and peaked at 4-16 hours in tissues.<BR>3) Urinary excretion<BR>FT-207 and its active substances were excreted in urine for a long time, and the recoveries of FT-207 for 48 hours in rats, mice and rabbits were 12-18%.<BR>4) Metabolism<BR>In normal and AH-130 bearing rats, the main active substance from FT-207 administrated intravenously was 5-FU.

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