Novel C-6 Substituted and Unsubstituted Pregnane Derivatives as 5α-Reductase Inhibitors and Their Effect on Hamster Flank Organs Diameter Size

May 2009 in “ Steroids ”

Marisa Cabeza, Armando Zambrano, Ivonne Heuze, Erick Carrizales, Anay Palacios, Tania Segura, Norma Valencia, Eugene Bratoeff

5α-reductase inhibitors progesterone derivatives C-6 substituted pregnane derivatives antiandrogenic activity 5α-reductase enzyme hamster flank organs chlorine substituent finasteride 5-alpha-reductase inhibitors Propecia

Studysummary This study found that progesterone derivatives with chlorine or bromine substituents were effective in inhibiting 5α-reductase activity in human prostate and exhibited antiandrogenic effects in hamster flank organs.

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research Biological Activity of Novel Progesterone Derivatives Having Bulky Ester Side Chains at C-3

15 citations , April 2008 in “Steroids”

This study found that pregnane derivatives with higher lipophilicity, like compound 9d, had stronger androgen receptor binding and greater antiandrogenic effects in rats, correlating relative binding affinity with log P values.

research Novel Inhibitors of 5α-Reductase

20 citations , February 2002 in “Expert Opinion on Therapeutic Patents”

This review discusses the potential uses of 5α-reductase inhibitors for conditions ranging from benign prostatic hyperplasia to skin disorders like acne and male pattern baldness, but it reports no new clinical results.

research Evaluation of New Pregnane Derivatives as 5α-Reductase Inhibitors

23 citations , January 2001 in “Chemical & Pharmaceutical Bulletin”

This study found that several synthesized pregnane derivatives exhibited significant inhibitory effects on testosterone conversion to dihydrotestosterone and reduced related androgenic parameters in multiple pharmacological models.

research Local and Systemic Reduction by Topical Finasteride or Flutamide of Hamster Flank Organ Size and Enzyme Activity

37 citations , November 1995 in “Journal of Investigative Dermatology”

This study found that topical finasteride and flutamide both significantly reduced sebaceous gland growth and decreased prostatic weights in hamsters, indicating systemic effects despite local application.

research Pilosebaceous Physiology in Relation to Hirsutism and Acne

75 citations , May 1986 in “Clinics in endocrinology and metabolism”

This review explores how androgens and growth hormone influence the development of terminal hairs and sebaceous glands, attributing variability in hirsutism and acne to differing genetic sensitivities to androgens, but reports no new experimental data.

research Species Differences in Prostatic Steroid 5α-Reductases of Rat, Dog, and Human

193 citations , August 1985 in “Endocrinology”

This study found significant species differences in the enzyme activity and inhibitor affinities of prostatic 5α-reductases from rats, dogs, and humans, with variable potencies for different 3-oxo-4-azasteroid inhibitors across species.

research The Antiandrogenic Action of 4-Androsten-3-One-17β-Carboxylic Acid and Its Methyl Ester on Hamster Flank Organ

87 citations , April 1973 in “Endocrinology”

This study found that in hamster flank organs, 17βC inhibited enlargement caused by topical testosterone but not by DHT, suggesting potential use in androgen-related skin disorders like acne.