代谢
Sprague-Dawley Crl:CD/BR 大鼠,无论雌雄,分别口服给予10或1000毫克/千克的[(14)C] ... /bifenazate/(... 放射化学纯度:>98%,比活性:34.4 mCi/mmol,芳香环上标记,... /bifenazate/(未标记... 纯度:99.6%)通过口服灌胃。... 分析在粪便中回收的放射性标记部分揭示了母体化合物的多种修饰。肼氧化,脱甲基,环羟基化,分解成联苯和对肼羧酸部分以及与葡萄糖醛酸或硫酸的共轭。对于10毫克/千克组,从粪便中提取的识别部分构成了给予剂量的39%(AD)。主要化合物是... /bifenazate/ 葡萄糖苷酸(占AD的6.3-8.9%),... /bifenazate/(占AD的4.8-7.2%)和... 联苯,4-羟基(占AD的5.5-7.1%)。相比之下,对于1000毫克/千克组,在粪便中回收的母体化合物构成了AD的48-61%。... /Bifenazate/ 葡萄糖苷酸构成了AD的4.7-5.6%。尿液中回收的主要部分是... p, p-联苯酚或... /p, p'-联苯酚/和... /联苯,4-羟基/的硫酸盐的共轭物。这些化合物的总量构成了10毫克/千克组的给予剂量的19-21%,以及1000毫克/千克组的给予剂量的6-7%。胆汁中识别的主要代谢物是... /联苯,4-羟基/(在10毫克/千克组中占AD的17-20%,在1000毫克/千克组中占AD的2.1-2.5%),... 联苯,4-羟基,4-甲氧基(在10毫克/千克组中占AD的17-19%,在1000毫克/千克组中占AD的2.8%)和... /bifenazate/ 葡萄糖苷酸(在10毫克/千克组中占AD的9-12%,在1000毫克/千克组中占AD的9-13%)。
Sprague-Dawley Crl:CD/BR rats of both sexes were dosed with either 10 or 1,000 mg/kg of [(14)C] ... /bifenazate/ ( ... radiochemical purity: >98%, specific activity: 34.4 mCi/mmol, label on the aromatic ring, ... /bifenazate/ (unlabeled ... purity: 99.6%) by oral gavage. ... Analysis of the radiolabeled moieties recovered in the feces revealed a number of modifications of the parent cmpd. Hydrazine oxidation, demethylation, ring hydroxylation, separation into biphenyl and hydrazinecarboxylic acid moieties and conjugation with glucuronic acid or sulfate. For the 10 mg/kg group, identified moieties extracted from the feces constituted 39% of the administered dose (AD). The predominant compounds were ... /bifenazate/ glucuronide (6.3-8.9% of AD), ... /bifenazate/ (4.8-7.2% of AD) and ... biphenyl, 4-hydroxy (5.5-7.1% of AD). In contrast, for the 1,000 mg/kg group, the parent cmpd which was recovered in the feces constituted 48-61% of the AD. ... /Bifenazate/ glucuronide constituted 4.7-5.6% of the AD. The primary moieties recovered in the urine were conjugates of ... p, p-biphenol or sulfates of ... /p, p'-biphenol/ and ... /biohenyl, 4-hydroxy/. The total of these cmpds constituted 19-21% of the administered dose for the 10 mg/kg group and 6-7% of the administered dose for the 1,000 mg/kg group. Major metabolites identified in the bile were ... /biphenyl, 4-hydroxy/ (17-20% of AD in the 10 mg/kg group and 2.1-2.5% of the AD in the 1,000 mg/kg group), ... biphenyl, 4-hydroxy, 4-methoxy (17-19% of the AD in the 10 mg/kg and 2.8% of the AD in the 1,000 mg/kg group) and ... /bifenazate/ glucuronide (9-12% of the AD in the 10 mg/kg and 9-13% of the AD in the 1,000 mg/kg group).
来源:Hazardous Substances Data Bank (HSDB)