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2-(3-三氟甲基苯基)四氢-1,4-恶嗪(CERM 1841)在大鼠和犬体内的代谢产物。

Metabolites of 2-(3-trifluoromethylphenyl)tetrahydro-1,4-oxazine (CERM) 1841) in rats and dogs.

作者信息

Kucharczyk N, Yang J T, Valia K H, Stiefel F J, Sofia R D

出版信息

Xenobiotica. 1979 Nov;9(11):703-11. doi: 10.3109/00498257909042338.

DOI:10.3109/00498257909042338
PMID:532219
Abstract
  1. In rats and dogs dosed with 14C-labelled 2-(3-trifluoromethylphenyl)tetrahydro-1,4-oxazine hydrochloride, the 14C was excreted in the urine. The 14C eliminated in the faeces of dog was significantly higher than for rat. 2. Conjugated metabolites, mostly glucuronides, accounted for the greater part of the urinary radioactivity in both species. 3. Biotransformation products were predominantly acids in both species, followed by significant amounts of basic metabolites, with very little neutral substances. 4. The major urinary metabolite in rats was 3-trifluoromethylbenzoic acid and 3-trifluoromethylhipuric acid. In the dog it was 3-trifluoromethylmandelic acid in addition to the benzoic acid and its conjugate. The basic products identified in the urine of both species were unchanged drug and 1-amino-2-hydroxy-2-(3-trifluoromethylphenyl)ethane, with the first predominating.
摘要
  1. 给大鼠和狗服用14C标记的盐酸2-(3-三氟甲基苯基)四氢-1,4-恶嗪后,14C经尿液排出。狗粪便中排出的14C显著高于大鼠。2. 结合代谢物,主要是葡糖醛酸苷,占两种动物尿液放射性的大部分。3. 两种动物的生物转化产物主要是酸性物质,其次是大量碱性代谢物,中性物质极少。4. 大鼠尿液中的主要代谢物是3-三氟甲基苯甲酸和3-三氟甲基马尿酸。狗尿液中的主要代谢物除苯甲酸及其结合物外,还有3-三氟甲基扁桃酸。在两种动物尿液中鉴定出的碱性产物是未变化的药物和1-氨基-2-羟基-2-(3-三氟甲基苯基)乙烷,前者占主导。

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