Molecular Pharmacology, Vol 5, 428-431, Copyright © 1969 by the American Society for Pharmacology and Experimental Therapeutics

Antagonistic Action of Anti-androgens on the Formation of a Specific Dihydrotestosterone-Receptor Protein Complex in Rat Ventral Prostate

¹ Ben May Laboratory for Cancer Research and Department of Biochemistry, University of Chicago, Chicago, Illinois 6O637

Cyproterone (1,2-methylene-6-chloro-^4,6-pregnadien-17-ol-3,20-dione) 17-acetate, a potent anti-androgen, suppressed the uptake of radioactive androgens in vivo by the ventral prostate of rats. This was accompanied by a decrease in the retention of 5-dihydrotestosterone (17-hydroxy-5-androstan-3-one) by prostate cell nuclei . Cyproterone and its 17-acetate (less than 0.5 µg/ml) also inhibited the formation of a specific dihydrotestosterone-protein complex in prostate cell nuclei when minced prostate was incubated with radioactive testosterone or dihydrotestosterone. Estradiol-17, diethylstilbestrol, and progesterone, but not hydrocortisone succinate, also suppressed the retention of dihydrotestosterone by prostatic cell nuclei in vitro, but to a much lesser extent than cyproterone.

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ACKNOWLEDGMENTS The authors wish to express their appreciation to Mrs. A. H. Lin, Mrs. D. Sagher, and Mr. J. L. Tymoczko for their skillful technical assistance.

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