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本文报告了18-甲基乙炔雌二醇-3-甲醚的激素活性和避孕作用。 18-甲炔雌甲醚在幼年雌性小鼠能明显刺激子宫发育,说明有雌激素活性。经与炔雌醇-3-甲醚作效价比较,结果指出其雌激素活性约为炔雌醇-3-甲醚的1/50。当与雌二醇同时应用时,18-甲炔雌甲醚并不能对抗雌二醇引起的子宫发育,说明没有抗雌激素活性。 用Claubcrg方法以及用大鼠蜕膜瘤方法进行的实验说明18-甲炔雌甲醚没有孕激素活性,但有明显的抗孕激素活性。 在小鼠妊娠第1、2、3天经口给18-甲炔雌甲醚,每日1 mg/kg小鼠不能怀孕。在妊娠第6、7、8天给18-甲炔雌甲醚,小鼠只有10～20％怀孕。说明有明显的抗着床和抗早孕作用。 在小鼠妊娠第1、2两天经口给18-甲炔雌甲醚,有4/10的动物在妊娠第四天输卵管中仍可见到受精卵,而对照组在妊娠第四天输卵管中都没有卵子,可见18-甲炔雌甲醚使受精卵在输卵管中的运行变慢,这一作用也可能是18-甲炔雌甲醚抗着床作用的一个原理。 经口给小鼠18-甲炔雌甲醚2 mg/kg,连给2周,对动物体重增长和各主要脏器形态都没有明显影响。经口给狗1 mg/kg,连给两周,狗的血象、心脏和肝、肾功能没有出现异常。
This article reports the hormonal activity and contraception of 18-methylethynyl estradiol-3-methyl ether. 18-Megastromethylether significantly stimulates uterine development in young female mice, indicating estrogenic activity. By ethinyl estradiol-3-methyl ether as a titer comparison, the results indicated that the estrogen activity of ethinylestradiol-3-methyl ether about 1/50. When applied simultaneously with estradiol, 18-methylethylether did not counteract estradiol-induced uterine development, indicating no anti-estrogenic activity. Experiments with the Claubcrg method and the rat decidua method demonstrated that 18-methylestrole did not have progestin activity but had significant antiprogestin activity. Mice in the 1st, 2nd, 3rd day oral administration of 18-methylesterazine, daily 1 mg / kg mice can not be pregnant. On the 6th, 7th, and 8th days of gestation, 18-MCP was given to the mice, and only 10 to 20% of the mice were pregnant. Shows significant anti-implantation and anti-pregnancy effect. On the first and second days of pregnancy, mice were orally administered 18-methylestene methyl ether, and 4/10 animals still showed fertilized eggs in the fallopian tube during the fourth day of pregnancy. In the fourth day of pregnancy, the control group received oviducts Have no eggs, showing that 18-methylesterazine so that fertilized eggs in the fallopian tube slows down, this effect may also be a 18-methylmethylether anti-implantation effect of a principle. Oral administration of 18 mg / kg 18-methylethanol to mice for 2 weeks gave no significant effect on body weight gain and the morphology of major organs. Oral administration to dogs 1 mg / kg, even for two weeks, the dog’s blood, heart and liver, kidney function did not appear abnormal.