妊娠期间常用的一些药物缺乏雌激素活性。

W D Isenhower, R R Newbold, R C Cefalo, K S Korach, J A McLachlan
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引用次数: 0

摘要

孕妇用雌激素化合物如己烯雌酚(DES)治疗与其雄性和雌性后代的生殖道异常有关。由于这些数据表明,发育中的胎儿对雌激素物质的致瘤性和致畸形作用非常敏感,因此了解妊娠期间常用的一些药物的雌激素活性是很重要的。基于与其他已知雌激素化合物的结构相似性和孕妇使用频率,对苯巴比妥、糖精和对乙酰氨基酚的雌激素活性进行了分析;以DES为阳性对照。通过竞争性受体结合试验,这些化合物与可溶性子宫受体制剂没有明显的结合,而DES则表现出很强的结合相互作用。使用未成熟雌性小鼠进行体内促子宫生物测定分析表明,在使用的剂量范围内(5微克/千克-50微克/千克),只有DES具有雌激素活性,而其他化合物均为阴性。因此,在试验条件下,苯巴比妥、糖精和对乙酰氨基酚不显示雌激素活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Absence of estrogenic activity in some drugs commonly used during pregnancy.

Treatment of pregnant women with estrogenic compounds such as diethylstilbestrol (DES) has been associated with genital tract abnormalities in their male and female offspring. Since these data suggest the developing fetus is highly susceptible to the tumorigenic and dysmorphogenic effects of estrogenic substances, knowledge of the estrogenic activity of some drugs commonly used during pregnancy is important. Based on structural similarities to other known estrogenic compounds and to the frequency of use among pregnant women, phenobarbital, saccharin and acetaminophen were assayed for estrogenic activity; DES was used as a positive control. Using a competitive receptor binding assay, these compounds did not show appreciable binding to a soluble uterine receptor preparation while DES showed strong binding interactions. Analysis of the compounds in an in vivo uterotropic bioassay using immature female mice showed that, over the dose range used (5 micrograms/kg-50 micrograms/kg), only DES had any estrogenic activity while the other compounds were negative. Therefore, phenobarbital, saccharin and acetaminophen did not display estrogenic activity under the conditions of test.

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