Abstract |
Intramuscular administration of a new steroidal anti- androgen, TSAA-291 (16 beta-ethyl-17 beta-hydroxy-4-oestren-3-one), in doses of 0.05, 0.5 and 5 mg/kg body weight reduced the in vivo uptake of [3H] testosterone by the ventral prostate of castrated rats of 78, 59 and 37% of the control level, respectively. Analysis on subcellular fractions of the prostate by gel-filtration and sucrose density-gradient centrifugation followed by thin layer chromatographic identification of testosterone metabolites revealed that 5 alpha-dihydrotestosterone (5 alpha-DHT) which was found to be largely bound to macromolecules in the cytosol and nucleus was the predominant metabolite even in the presence of the anti- androgen, and radioactivities corresponding to the 5 alpha-DHT- macromolecular complexes were decreased by the anti- androgen. TSAA-291 also inhibited the in vitro formation of the 5 alpha-DHT- macromolecular complexes in both cytosol and nucleus from minced prostates incubated with [3H] testosterone. The importance of the findings is discussed in connection with the mode of anti-androgenic action of TSAA-291 in terms of the interaction with the androgen receptor.
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Authors | K Sudo, K Yoshida, Y Kimura, R Nakayama |
Journal | Acta endocrinologica. Supplementum
(Acta Endocrinol Suppl (Copenh))
Vol. 229
Pg. 67-81
( 1979)
ISSN: 0300-9750 [Print] Denmark |
PMID | 294108
(Publication Type: Journal Article)
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Chemical References |
- Androgen Antagonists
- Macromolecular Substances
- Receptors, Androgen
- Receptors, Steroid
- Dihydrotestosterone
- Testosterone
- Nandrolone
- Cyproterone
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Topics |
- Androgen Antagonists
(administration & dosage, pharmacology)
- Animals
- Castration
- Cell Nucleus
(metabolism)
- Centrifugation, Density Gradient
- Chromatography, Gel
- Cyproterone
(pharmacology)
- Cytosol
(metabolism)
- Dihydrotestosterone
(metabolism)
- Injections, Intramuscular
- Macromolecular Substances
- Male
- Nandrolone
(analogs & derivatives, pharmacology)
- Prostate
(metabolism)
- Rats
- Receptors, Androgen
(biosynthesis)
- Receptors, Steroid
(biosynthesis)
- Testosterone
(metabolism)
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