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Metabolic Studies with 5-Fluorocytosine-6-14C in Mouse, Rat, Rabbit, Dog and Man

 

作者: Annemarie Polak,   E. Eschenhof,   M. Fernex,   H.J. Scholer,  

 

期刊: Chemotherapy  (Karger Available online 1976)
卷期: Volume 22, issue 3-4  

页码: 137-153

 

ISSN:0009-3157

 

年代: 1976

 

DOI:10.1159/000221923

 

出版商: S. Karger AG

 

关键词: 5-Fluorocytosine-6-14C;Metabolism;Mouse;Rat;Rabbit;Dog;Man

 

数据来源: Karger

 

摘要:

Metabolism of 5-fluorocytosine-6-14C (5-FC) was studied in mice, rats, rabbits and dogs after oral and subcutaneous, single and repeated administration. In the urines of all species, intact 5-FC accounted for more than 90% of the total radioactivity at any time of the various treatment schedules. The average proportion of the urinary metabolites was around 5% in dogs, 3% in rabbits, 2.5% in rats and 2% in mice of the total radioactivity. At repeated dosage, there was an increase of metabolites in mice but a decrease in rats treated subcutaneously. Neither increase nor decrease was observed in rabbits (treated orally) and dogs. Two metabolites were identified, α-fluoro-β-ureido-propionic acid (FUPA) and α-fluoro-β-alanine, the latter occurring mainly after oral treatment. These compounds represent probably that part of 5-FC which was deaminated to 5-fluorouracil (5-FU) or directly to 5-fluorodihydroura

 

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