METABOLIC-FATE OF 1-HEXYLCARBAMOYL-5-FLUOROURACIL IN RATS

被引：30

作者：

KOBARI, T

TAN, K

KUMAKURA, M

WATANABE, S

SHIRAKAWA, I

KOBAYASHI, H

UJIIE, A

MIYAMA, Y

NAMEKAWA, H

YAMAMOTO, H

机构：

[1] Institute of Biological Science, Mitsui Pharmaceuticals, Inc., TGO, Mobara, Chiba

来源：

XENOBIOTICA | 1978年 / 8卷 / 09期

关键词：

D O I：

10.3109/00498257809061254

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. 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-carboxypropylcar-bamoyl)-5-fluorouracil were identified as the major urinary metabolites of 14C-HCFU. © 1978 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.

引用

页码：547 / 556

页数：10

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