[Experimental data on estradiol 3,17-diethers (author's transl)].
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.
D000818:Animals; D004951:Esterification; D004958:Estradiol / Q000008:administration & dosage / Q000378:metabolism*; D007271:Injections, Intradermal; D007279:Injections, Subcutaneous; D008099:Liver / Q000378:metabolism*; D051381:Rats
D004958:Estradiol
Recherches expérimentales sur les 3, 17-diethers de l'estradiol.