Screening for antiandrogenic activity of some 4,5-cyclo-A-homo-B-nor-androstane derivatives

Five 4α, 5-cyclo-A-homo-B-nor-androstane derivatives were assayed in vivo on mice for their antiandrogenic activity and the effect was compared with that of cyproterone acetate. The inhibition of dihydrotestosterone binding to rat prostate cytosol by the compounds was correlated to the in vivo effec...

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Veröffentlicht in:	Journal of steroid biochemistry 1977-09, Vol.8 (9), p.939-941
Hauptverfasser:	Stárka, L., S̆ulcová, Jarmila, Broulik, P.D., Joska, J., Fajkoš, J., Doskočil, M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Androgen Antagonists - pharmacology Androstanes - pharmacology Animals Body Weight - drug effects Castration Cyproterone - pharmacology Drug Evaluation, Preclinical Male Mice Organ Size - drug effects Organ Specificity Structure-Activity Relationship Testosterone Congeners - pharmacology
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Zusammenfassung:	Five 4α, 5-cyclo-A-homo-B-nor-androstane derivatives were assayed in vivo on mice for their antiandrogenic activity and the effect was compared with that of cyproterone acetate. The inhibition of dihydrotestosterone binding to rat prostate cytosol by the compounds was correlated to the in vivo effect. The antiandrogenic action of 17β-acetoxy-4α, 5-cyclo-A-homo-B-nor-5α-androst-1-en-3-one was found to be comparable with that of cyproterone acetate. The compound exhibited an antirenotrophic but not a corticoid-like effect. Its teratogenicity assayed on chick embryos was similar to that of spirolactones.
ISSN:	0022-4731
DOI:	10.1016/0022-4731(77)90190-X