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2α, 3α-Epithio-5α-androstan-17β-ol (10275-S) has been known to possess a potent and long-acting anti-estrogenic activity in rodents. In this experiment, 1.25mg 10275-S injected once subcutaneously into the ovariectomized and estradiol-treated mice caused a complete block of vaginal cornification for 24.3 days in spite of the successive treatment with estrogen. Pre-treatment with 10275-S in ovariectomized mice either 4 or 24 hr before tritiated estradiol injection caused significant inhibition of accumulation of radioactivity in the uterus. Pre-incubation of uterine cytosol from immature rat with 10275-S competitively suppressed the formation of estradiol-macromolecule complex maximally around the 8S region, and 50% suppression was obtained at 4.4×10-7M, about 70-fold over the estradiol. Under the same conditions, 10-5M progesterone or testosterone gave no effect on estradiol binding at the 8S region. The relation of these in vitro results to the in vivo activities of this steroid was discussed.

Epithioandrostanol (10275-S), an Estrogen Antagonist