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大鼠体内肝毒性抗保幼激素早熟素II的代谢命运

Metabolic fate of the hepatotoxic anti-juvenile hormone precocene II in the rat.

作者信息

Grossman S J, Hsia M T

出版信息

Toxicology. 1982;25(4):293-8. doi: 10.1016/0300-483x(82)90107-x.

DOI:10.1016/0300-483x(82)90107-x
PMID:7157406
Abstract

The metabolic fate of precocene II (6,7-dimethoxy-2,2-dimethyl-2H-benzo[b]pyran), a potent anti-juvenile hormone, was examined in male Sprague-Dawley rats. When a single intraperitoneal dose of [3H]precocene II was administered, approximately 34% of the administered dose was excreted within the first 24 h. Examination of the various urinary metabolites indicated that precocene II is metabolized to a stereoisomeric cis/trans mixture of the 3,4-dihydroxy-3,4-dihydroprecocene II. In addition, a mercapturic acid derivative of precocene II was tentatively identified. Thus, it is postulated that a highly reactive 3,4-epoxide intermediate is generated in vivo by the rat during oxidative metabolism.

摘要

在雄性斯普拉格-道利大鼠中研究了早熟素II(6,7-二甲氧基-2,2-二甲基-2H-苯并[b]吡喃)(一种有效的抗保幼激素)的代谢命运。当腹腔注射单剂量的[3H]早熟素II时,给药剂量的约34%在最初24小时内排出。对各种尿液代谢物的检测表明,早熟素II代谢为3,4-二羟基-3,4-二氢早熟素II的立体异构顺式/反式混合物。此外,还初步鉴定出早熟素II的一种巯基尿酸衍生物。因此,推测大鼠在氧化代谢过程中在体内产生了高反应性的3,4-环氧化物中间体。

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