1-己基氨基甲酰基-5-氟尿嘧啶在大鼠体内的代谢命运
Metabolic fate of 1-hexylcarbamoyl-5-fluorouracil in rats.
作者信息
Kobari T, Tan K, Kumakura M, Watanabe S, Shirakawa I, Kobayashi H, Ujiie A, Miyama Y, Namekawa H, Yamamoto H
出版信息
Xenobiotica. 1978 Sep;8(9):547-56. doi: 10.3109/00498257809061254.
PMID:695698
Abstract
- The metabolic fate of a new antitumour agent, 1-hexylcarbamoyl-5-fluoro [6-14C]uracil (14C-HCFU) in rats after oral administration was compared with that of 5-fluoro[6-14C]uracil (14C-FU). 2. Tissue radioactivity reached a max. 1 to 3 h after administration of 14C-HCFU and 0.5 h after 14C-FU. 3. Both drugs were excreted rapidly, mostly in urine. Expired 14CO2 from 14C-HCFU was significantly less than that from 14C-FU. 4. Unchanged FU was not detected in plasma 3 h after administration of 14C-FU, whereas FU was detected in plasma 5 h after 14C-HCFU. The pyrimidine ring of 14C-HCFU might be degradated more slowly than that of 14C-FU. 5. 1-(5-Carboxypentylcarbamoyl)-5-fluorouracil and 1-(3-carboxypropylcarbamoyl)-5-fluorouracil were identified as the major urinary metabolites of 14C-HCFU.
摘要
- 将新型抗肿瘤药物1-己基氨基甲酰基-5-氟[6-¹⁴C]尿嘧啶（¹⁴C-HCFU）与5-氟[6-¹⁴C]尿嘧啶（¹⁴C-FU）口服给药后在大鼠体内的代谢命运进行了比较。2. ¹⁴C-HCFU给药后1至3小时以及¹⁴C-FU给药后0.5小时，组织放射性达到最大值。3. 两种药物均迅速排泄，大部分经尿液排出。¹⁴C-HCFU呼出的¹⁴CO₂明显少于¹⁴C-FU。4. ¹⁴C-FU给药后3小时血浆中未检测到未变化的FU，而¹⁴C-HCFU给药后5小时血浆中检测到了FU。¹⁴C-HCFU的嘧啶环降解可能比¹⁴C-FU更慢。5. 1-(5-羧基戊基氨基甲酰基)-5-氟尿嘧啶和1-(3-羧基丙基氨基甲酰基)-5-氟尿嘧啶被鉴定为¹⁴C-HCFU的主要尿液代谢产物。
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