Studies on the local activity of antiandrogens at the molecular and histological level

Androgen dependent skin disorders are important in clinical practice. Effective topical antiandrogens would lead to a breakthrough in their treatment. Although many attempts have been performed to develop such compounds, major successes have not been forthcoming. In the present study three existing...

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Bibliographic Details
Published in:Molecular biology reports 1986-01, Vol.11 (2), p.99-105
Main Authors: VERMORKEN, A. J. M, GOOS, C. M. A. A, SULTAN, C, VERMEESCH-MARKSLAG, A. M. G, DIJKSTRA, A. C
Format: Article
Language:English
Subjects:
Androgen Antagonists - pharmacology
Androgens - metabolism
Animals
Binding, Competitive
Biological and medical sciences
Cricetinae
Cyproterone - analogs & derivatives
Cyproterone - metabolism
Cyproterone - pharmacology
Cyproterone Acetate
Female
Hair - drug effects
Hair - metabolism
Hormones. Endocrine system
Humans
Medical sciences
Pharmacology. Drug treatments
Progesterone - metabolism
Progesterone - pharmacology
Receptors, Androgen - analysis
Testosterone - pharmacology
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Summary:Androgen dependent skin disorders are important in clinical practice. Effective topical antiandrogens would lead to a breakthrough in their treatment. Although many attempts have been performed to develop such compounds, major successes have not been forthcoming. In the present study three existing antiandrogenic molecules have been compared with regard to their effect on androgen metabolism, receptor competition and on histological parameters in the hamster flank organ test. It appears that the effect on the hamster pigmented spot can be predicted on the basis of molecular mechanism. However, the effects on histological parameters are apparently dependent on additional factors such as metabolism of the active substance before reaching the sebaceous structure or limited penetration through the skin surface. The results indicate that in the development of new antiandrogens pre-screening can be performed with the aid of metabolic and receptor studies, while the histological parameters in the hamster flank organ test provide an animal model with a good predictive value.
ISSN:0301-4851
1573-4978
DOI:10.1007/BF00364821