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Orally active synthetic estrogens and progestins were studied in tests to prevent pregnancy in rats. Groups of 10 female rats were given the test compound 17alpha-(3-furyl)-estra-135(10)7-tetraene-317-diol 3-acetate (AU-11483) every day for 35 days during cohabitation with males. Other rats were given combinations of other estrogens and progestins. Results show that none of the estrogens alone (10 mcg/rat) and none of the progestins alone (100 mcg/rat) were completely effective in preventing pregnancy when given over a period of 35 days. The contraceptive effect of ethynylestradiol and AY-11483 were potentiated by three progestins: chlormadinone acetate 6-chloro-3beta17alpha-dihydroxypregn-46-dien-20-one diacetate (AY-11440) and medrogestone. AY-11483 given alone or together with AY-11440 was more potent in preventing ovulation and implantation than ethynylestradiol alone or in combination with other compounds. Chlormadinone acetate or AY-11440 alone were completely inactive in all the assays. Results show that in the rat implantation seems more vulnerable to estrogens than does ovulation. This study indicates that AY-11483 is orally active in preventing pregnancy in rats by interfering with both ovulation and implantation.

ORALLY ACTIVE OESTROGENS AND PROGESTINS IN PREVENTION OF PREGNANCY IN RATS