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Testosterone and 19-nortestosterone derivatives were evaluated in a developmental scheme designed to identify competitive progesterone antagonists having abortifacient activity. Compounds that displayed significant binding to the rabbit uterine progesterone receptor were followed in biologic tests for progestational, antiprogestational, and abortifacient activities. Of the seven compounds tested for both progestational and antiprogestational activity, only one, 5 alpha-dihydronorethindrone, behaved exclusively as an antagonist. Five other 19-nortestosterones (19-nortestosterone, 17 beta-hydroxyestra-4, 9(10)-dien-3-one, norethindrone, norethindrone acetate, and R 2323) proved to be mixed agonists/antagonists. 5 alpha-Dihydronorethindrone, norethindrone, and 19-nortestosterone terminated pregnancy during the postnidatory period in rats; in addition, the latter two compounds inhibited progesterone-supported pregnancy in spayed rats and curtailed pregnancy during the postnidatory period in hamsters. These results demonstrate that several 19-nortestosterone derivatives bind to the uterine progesterone receptor and behave either as antagonists or mixed agonists/antagonists.
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
January 1979,
Die Pharmazie,
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
May 1994,
The Journal of steroid biochemistry and molecular biology,
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
November 1957,
The Journal of endocrinology,
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
January 1974,
Problemy endokrinologii,
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
December 1996,
The Journal of clinical endocrinology and metabolism,
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
December 1982,
Journal of steroid biochemistry,
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
March 1957,
Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.),
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
June 1994,
Human reproduction (Oxford, England),
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
October 1996,
European journal of pharmacology,
J R Reel, and
R R Humphrey, and
Y H Shih, and
B L Windsor, and
R Sakowski, and
P L Creger, and
R A Edgren
February 2015,
Bioorganic & medicinal chemistry,
