17 alpha-Propylmesterolone (SH 434): an antiandrogenic sebosuppressive substance not influencing circulating testosterone concentrations. Experimental studies in Syrian hamsters

• Published in: Naunyn-Schmiedeberg's archives of pharmacology 1984-12, Vol.328 (2), p.214-218
• Main Authors: Luderschmidt, C, Eiermann, W, Jawny, J, Bidlingmaier, F, Ring, J
• Format: Article
• Language: English
• Subjects: Androgen Antagonists - pharmacology; Animals; Cricetinae; Dihydrotestosterone - analogs & derivatives; Ear - anatomy & histology; Male; Mesocricetus; Mesterolone - analogs & derivatives; Mesterolone - pharmacology; Organ Size - drug effects; Receptors, Steroid - metabolism; Sebaceous Glands - anatomy & histology; Sebaceous Glands - drug effects; Sebum - metabolism; Testis - drug effects; Testosterone - blood
• ISSN: 0028-1298
• DOI: 10.1007/BF00512076

17 alpha-Propylmesterolone is a new synthetic 5 alpha-reduced steroid with a propyl group in C-17 position and a methyl group in the A ring. The antiandrogenic action of 17 alpha-propylmesterolone on the sebaceous glands, testes weights and plasma testosterone concentrations were examined in the animal model of the Syrian hamster. The substance was given systemically (3, 5 or 10 mg/kg) and topically (3 or 5 mg/kg). 17 alpha-propylmesterolone reduced both sebaceous gland size and sebogenesis significantly in a dose-dependent manner. The topical administration was more effective than the systemic treatment. There was no influence of 17 alpha-propylmesterolone on testosterone concentration in plasma or testes weights although a diminished capacity or absence of free cytoplasmatic androgen receptor sites was detected in the sebaceous glands of the systematically or topically treated Syrian hamster. 17 alpha-Propylmesterolone exerts a potent topical sebosuppressive effect in the animal model. These findings should give rise to human studies and clinical trials.