Effect of Estrone and Progestational Steroids on Human Chorionic Gonadotrophin (HCG)-Induced Ovarian Augmentation in Parabiotic Rats

Sager, Dorothea B.; Schuetz, Allen W.; Meyer, Roland K.

doi:10.1210/endo-78-3-445

Cited by 2 publications

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This family, which was found to express unexpected antiandrogenic properties, was screened and the 17α-propionate ester of cortexolone (CB-03-01, CAS 19608-29-8) was selected for its optimum topical antiandrogenic profile. CB-03-01 was assayed in the following tests: local antiandrogenic activity in hamster's flank organ [6,8], systemic antiandrogenic, antianabolic and glucocorticoid activity in the immature male castrated rat [9], effect on gonadotropins hypersecretion in the parabiotic rat [10], and effect on plasma corticosterone in rat. Preliminary information about the potential systemic toxicity of CB-03-01 in rat has been also collected.…”

Section: Introductionmentioning

confidence: 99%

Biological Profile of Cortexolone 17a-Propionate (CB-03-01), a New Topical and Peripherally Selective Androgen Antagonist

Celasco¹,

Moro²,

Bozzella³

et al. 2011

Arzneimittelforschung

View full text Add to dashboard Cite

The aim of this study was to investigate the antiandrogenic activity of a new monoester of cortexolone, cortexolone 17alpha-propionate (CAS 19608-29-8, CB-03-01). Although the compound displayed a strong local antiandrogenic activity in hamster's flank organ test, it did not exhibit antiandrogenic activity in rats after subcutaneous injection, nor did it affect gonadotropins hypersecretion when injected to parabiotic rats. As topical antiandrogen, the steroid resulted about 4 times more active than progesterone (CAS 57-83-0) and, when compared to known antiandrogen standards, it was about 3 times more potent than flutamide (CAS 13311-84-7), about 2 times more effective than finasteride (CAS 98319-26-7) and approximately as active as cyproterone acetate (CAS 427-51-0). Its pharmacological activity seemed to be primarily related to its ability to antagonistically compete at androgen receptor level; nevertheless its primary pharmacological target needs to be further investigated. Its topical activity, along with the apparent absence of systemic effects, anticipates this compound to have the potential of representing a novel and safe therapeutic approach for androgen-dependent skin disorders.

show abstract

Section: Introductionmentioning

confidence: 99%