دورية أكاديمية
5 Alpha-reductase inhibitory and anti-androgenic activities of some 4-azasteroids in the rat.
| العنوان: | 5 Alpha-reductase inhibitory and anti-androgenic activities of some 4-azasteroids in the rat. |
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| المؤلفون: | Brooks JR, Berman C, Primka RL, Reynolds GF, Rasmusson GH |
| المصدر: | Steroids [Steroids] 1986 Jan; Vol. 47 (1), pp. 1-19. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Country of Publication: United States NLM ID: 0404536 Publication Model: Print Cited Medium: Print ISSN: 0039-128X (Print) Linking ISSN: 0039128X NLM ISO Abbreviation: Steroids Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: New York Ny : Elsevier Original Publication: San Francisco. |
| مواضيع طبية MeSH: | Androgen Antagonists*, Azasteroids/*pharmacology , Oxidoreductases/*antagonists & inhibitors , Steroids, Heterocyclic/*pharmacology, Animals ; Cholestenone 5 alpha-Reductase ; Dihydrotestosterone/analogs & derivatives ; Dihydrotestosterone/antagonists & inhibitors ; Dihydrotestosterone/metabolism ; Dihydrotestosterone/pharmacology ; Drug Evaluation, Preclinical ; Male ; Orchiectomy ; Prostate/drug effects ; Prostate/metabolism ; Rats ; Structure-Activity Relationship ; Testis/physiology ; Testosterone/antagonists & inhibitors ; Testosterone/metabolism |
| مستخلص: | Inhibition of 5 alpha-reductase and anti-androgenicity were studied in rats treated with various 4-azasteroids. The known inhibitor, N,N-diethyl-4-methyl-3-oxo-4-aza-5 alpha-androstane-17 beta-carboxamide (4-MA) served as a reference compound, and analogs of this basic molecule were assayed. Enhancement of enzyme inhibitory potency was usually seen with delta 1 analogs, whereas reduction in activity was noted with substitutuents such as delta 5, a spirotetrahydrofuran ring at C-17 or 4-deaza groups. Many of the 4-azasteroids had a much greater oral anti-androgenic effect against testosterone propionate (TP) than dihydrotestosterone propionate (DHTP). This difference in activity versus the two androgens is believed to reflect the necessity for TP to undergo reduction to DHT before becoming capable of stimulating prostatic growth. Inhibition of 5 alpha-reductase by active compounds prevented the conversion, thereby producing an anti-androgenic effect. In this regard, certain delta 1 analogs of 4-MA, particularly those bearing a 17 beta-(N-tert butylcarbamoyl) group, proved very effective against TP but were relatively inactive versus DHTP. |
| المشرفين على المادة: | 0 (Androgen Antagonists) 0 (Azasteroids) 0 (Steroids, Heterocyclic) 08J2K08A3Y (Dihydrotestosterone) 3XMK78S47O (Testosterone) 73671-86-0 (17-N,N-diethylcarbamoyl-4-methyl-4-azaandrostane-3-one) 855-22-1 (dihydrotestosterone propionate) EC 1.- (Oxidoreductases) EC 1.3.1.22 (Cholestenone 5 alpha-Reductase) |
| تواريخ الأحداث: | Date Created: 19860101 Date Completed: 19870318 Latest Revision: 20190820 |
| رمز التحديث: | 20240627 |
| DOI: | 10.1016/0039-128x(86)90072-3 |
| PMID: | 3810695 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 0039-128X |
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| DOI: | 10.1016/0039-128x(86)90072-3 |