Estrogenic and Antiestrogenic Effects of Clomiphene, MER-25 and CN-55,945-27 on the Rat Uterus and Vagina

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Abstract
The estrogenic effects of compounds which also possess antiestrogenic activity, MER-25, clomiphene and CN-55,945-27, were compared with those of 17 [beta]-estradiol in ovariectomized rats. Increases in uterine glycogen, glucose, % water, and vaginal glycogen were noted with single doses of all the compounds. The maximal glycogen response to the inhibitors was about 1/2 of that induced by estradiol at the doses employed. The 3 antagonists also markedly inhibited the 6-hr. increase in glycogen, glucose and % water due to estradiol when they were given in multiple doses prior to estradiol treatment. MER-25, clomiphene, and CN-55,945-27 are competitive inhibitors of estrogen at a common site of action.