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氟尿嘧啶在比格犬和恒河猴体内的代谢。

The metabolism of ftorafur in the beagle dog and rhesus monkey.

作者信息

Freudenthal R I, Emmerling D C

出版信息

Xenobiotica. 1977 Dec;7(12):757-64. doi: 10.3109/00498257709038705.

Abstract
  1. Ftorafur, a fluorinated pyrimidine nucleoside antimetabolite, is metabolized by the beagle dog and rhesus monkey to 5-fluorouracil, which is subsequently biotransformed to the corresponding nucleosides, to alpha-fluoro-beta-ureidopropionic acid, to urea and to CO2. 2. In the dog, urea was the primary urinary metabolite while in the monkey, alpha-fluoro-beta-ureidopropionic acid predominated. 3. The dog and monkey excrete about 35 percent of the recovered dose as CO2. 4. The possibility that ftorafur is a relatively inactive transport form of 5-fluorouracil is discussed.
摘要
  1. 氟尿嘧啶,一种氟化嘧啶核苷抗代谢物,在比格犬和恒河猴体内代谢为5-氟尿嘧啶,随后5-氟尿嘧啶再生物转化为相应的核苷、α-氟-β-脲基丙酸、尿素和二氧化碳。2. 在犬体内,尿素是主要的尿液代谢物,而在猴体内,α-氟-β-脲基丙酸占主导。3. 犬和猴将约35%回收剂量以二氧化碳形式排出。4. 文中讨论了氟尿嘧啶是5-氟尿嘧啶相对无活性转运形式的可能性。

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