Reference

Kinetics of the transcutaneous penetration and binding of estradiol 3-propyl 17-methyl ether in different rat tissues

Kinetics of the transcutaneous penetration and binding of estradiol 3-propyl 17-methyl ether in different rat tissues. Tresca, Jean Pierre; Ponsard, Genevieve; Jayle, Max Fernand (Lab. Biochim., Fac. Med., Paris, Fr.). Can. J. Biochem., 55(10), 1096-102 (French) 1977. CODEN: CJBIAE. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) The transcutaneous penetration of estradiol 3-Pr ether, 17-Me ether (I) [39219-28-8] occurred by a diffusion phenomenon and did not seem to be modulated by a cutaneous receptor. After transcutaneous administration of I and estradiol [50-28-2], a comparison of the kinetics of uptake in the uterus and of uterotrophic effects, as well as an anal. of radioactivity taken up by a partition method between petroleum ether and NaOH, indicates that a cleavage of both ether groups of I occurred leading to estradiol. This deetherification may take place in the liver after a period of quiescence. I was taken up by the aorta and adipose tissue. The etherification of the alc. functions of estradiol allows an adequate protection of the hormone against hepatic catabolism. This may explain, along with the release of metabolites taken up by the adipose tissue, why I was bound to a greater extent thanestradiol by various tissues.

Study of an estrogen diether oxide (promestriene D

Study of an estrogen diether oxide (promestriene D.C.I.) on experimental seborrhea. Thevenot, R.; Paris, J.; Bonnet, P.; Hazard, M. C.; Krebs, B.; Milano, G. (Serv. Rech., Lab. Theramex, Monaco). Therapie, 31(6), 771-84 (French) 1976. CODEN: THERAP. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) Seborrhea stimulated in the rat by testosterone administration was inhibited by promestriene (I) [39219-28-8] in a dose dependent manner. 17.beta.-Estradiol [50-28-2] had a similar effect. Both estrogens also inhibited sebaceous activity in hamster flank organ and 5-.alpha.-reductase [9081-34-9] activity in rat prostate and skin. Since I has weak estrogenic activity but is equal to estradiol in antiseborrheic activity, there is no correlation between this activity and estrogenic activity.