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奥沙西泮剂量的饲料处理后B6C3F1小鼠肝脏药物代谢酶的活性

Activity of hepatic drug metabolizing enzymes following oxazepam-dosed feed treatment in B6C3F1 mice.

作者信息

Griffin R J, Burka L T, Cunningham M L

机构信息

Chemistry Branch, National Institute of Environmental Health Sciences MD C3-02, Research Triangle Park, NC 27709, USA.

出版信息

Toxicol Lett. 1995 Apr;76(3):251-6. doi: 10.1016/0378-4274(95)80010-b.

DOI:10.1016/0378-4274(95)80010-b
PMID:7762012
Abstract

Oxazepam has been determined to be a potent hepatocarcinogen in mice. Evidence in the literature indicates that oxazepam is capable of inducing drug metabolizing enzymes in rodents and an association between enzyme induction and carcinogenesis has been proposed for other compounds such as phenobarbital. We examined the pattern of enzyme induction that occurs under bioassay conditions in male B6C3F1 mice. The results indicate that oxazepam is capable of inducing multiple drug metabolizing enzymes under bioassay conditions. Closer examination of the most induced samples suggests that oxazepam is a phenobarbital-type enzyme inducer.

摘要

已确定奥沙西泮在小鼠中是一种强效肝癌致癌物。文献中的证据表明,奥沙西泮能够在啮齿动物中诱导药物代谢酶,并且已有人提出酶诱导与其他化合物(如苯巴比妥)的致癌作用之间存在关联。我们研究了在生物测定条件下雄性B6C3F1小鼠体内发生的酶诱导模式。结果表明,在生物测定条件下,奥沙西泮能够诱导多种药物代谢酶。对诱导程度最高的样本进行更仔细的检查表明,奥沙西泮是一种苯巴比妥型酶诱导剂。

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