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Prostatic effects of a nonsteroidal antiandrogen
Investigative Urology
|January 1, 1975
Summary
The nonsteroidal antiandrogen SCH 13521 interferes with steroid localization in the prostate, suggesting a competitive mechanism. Its interaction with estrogens indicates a complex action beyond simple androgen competition.
Area of Science:
- Endocrinology
- Pharmacology
- Urology
Background:
- Nonsteroidal antiandrogens are crucial in managing prostate conditions.
- Understanding the precise mechanisms of antiandrogen action is vital for therapeutic development.
Purpose of the Study:
- To investigate the antiprostatic effects and mechanisms of SCH 13521.
- To determine the influence of SCH 13521 on steroid deposition in prostate tissue.
Main Methods:
- Administered radiolabeled testosterone, dihydrotestosterone, and estriol (E-3) to rats and dogs.
- Assessed the localization of radioactivity in prostate and other tissues.
- Compared in vivo results with in vitro binding data.
Main Results:
- SCH 13521 interfered with the localization of steroids in the prostate, indicating competitive inhibition.
- A metabolite of SCH 13521 may play a role in its in vivo effects.
- SCH 13521 competed with both androgens and estrogens (E-3) in the prostate.
- Prostatic secretion volume decreased significantly, while 5-alpha-reductase and arginase activities were minimally affected.
Conclusions:
- SCH 13521's antiprostatic effects involve competition with androgens at the cellular level.
- Competition with estrogens suggests a more complex mechanism of action for SCH 13521 compared to other antiandrogens.