一些与乙胺氧三苯乙醇（MER 25）相关的三苯乙烷和三苯乙烯的雌激素、抗雌激素及生育作用
Oestrogenic, anti-oestrogenic and fertility effects of some triphenylethanes and triphenylethylenes related to ethamoxytriphetol (MER 25).
作者信息
Clark E R, Jordan V C
出版信息
Br J Pharmacol. 1976 Aug;57(4):487-93. doi: 10.1111/j.1476-5381.1976.tb10375.x.
Five triphenylethylenes, a triphenylethane and a triphenylethanol, carrying methyl substituents ortho to one or both of the ring oxygen functions, have been examined for oestrogenic, and antioestrogenic activity in mice, and three of the compounds, alpha-[4-(beta-diethylaminoethoxy)-3, 5-xylyl]-alpha-phenyl-beta-4-methoxyphenyl-ethanol (IV), alpha'-[4-(beta-diethylaminoethoxy)-3, 5-xylyl]-4-methoxy-bibenzyl (V) and alpha'-[4-(beta-diethylaminoethoxy)-3, 5-xylyl]-4-methoxy-stilbene (VI), were tested for their effects on fertility in mice. 2 Orthomethylation reduces oestrogenic and/or anti-oestrogenic activity compared with the reported activities of non-methylated analogues. 3 The anti-oestrogenic ethamoxytriphetol (MER 25) reduced fertility in mice whereas its inactive dimethylated analogue (IV) was ineffective. The weakly active anti-oestrogens, V and VI, did not affect fertility in mice.
对五种三苯乙烯、一种三苯乙烷和一种三苯乙醇进行了研究，这些化合物在与环氧化合物的一个或两个相邻位置带有甲基取代基，检测了它们在小鼠体内的雌激素活性和抗雌激素活性。对其中三种化合物，即α-[4-(β-二乙氨基乙氧基)-3,5-二甲苯基]-α-苯基-β-4-甲氧基苯基乙醇（IV）、α'-[4-(β-二乙氨基乙氧基)-3,5-二甲苯基]-4-甲氧基联苄（V）和α'-[4-(β-二乙氨基乙氧基)-3,5-二甲苯基]-4-甲氧基芪（VI），测试了它们对小鼠生育能力的影响。2与未甲基化类似物的报道活性相比，邻甲基化降低了雌激素活性和/或抗雌激素活性。3抗雌激素药物乙氧三苯氧胺（MER 25）降低了小鼠的生育能力，而其无活性的二甲基化类似物（IV）则无效。活性较弱的抗雌激素药物V和VI对小鼠的生育能力没有影响。
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