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Estradiol ethers reveal a biological activity in female rats which decreases according to the length of the side chain at position 3. Further, percutaneous injections have an activity which is 6 to 30 times greater that subcutaneous ones. This suggests that de-etherification could occur, leading to estradiol. After percutaneous administration of tritiated promestriene (3-propyl ether, 17-methyl ether estradiol) and estradiol, a comparison of the uptake on the uterus and of uterotrophic effects as well as an analysis of radioactivity taken up indicates that a cleavage of both ether groups of promestriene occurs leading to estradiol. This de-etherification takes place in the liver, as demonstrated by perfused liver experiments. With promestriene, antagonist activity is shown on the seborrheic androgen-stimulated rat and on 5-alpha-reductase activity in vitro and in vivo.
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