Reprint of 鈥?span style='font-style: italic'>In vitro and in vivo evaluation of a 3尾-androsterone derivative as inhibitor of 17尾-hydroxysteroid dehydrogenase type 3鈥?
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- 作者：Jenny Roy ; Michelle-Audrey Fournier ; René ; Maltais ; Lucie Carolle Kenmogne ; Donald Poirier ; donald.poirier@crchul.ulaval.ca" class="auth_mail" title="E-mail the corresponding author
- 关键词：AR ; androgen receptor ; A-diol ; 5伪-androstane-3伪 ; 17尾-diol ; A-dione ; 5伪-androstane-3 ; 17-dione ; 5-diol ; 5-androstene-3尾 ; 17尾-diol ; 4-dione ; 4-androstene-3 ; 17-dione ; ADT ; androsterone ; AUC ; area under curve ; CTX ; castrated ; CTL ; control ; DHEA ; dehydroepiandrosterone ; DHT ; dihydrotestosterone ; DMSO ; dimethyl sulfoxide ; E2 ; estradiol ; E1 ; estrone ; EDTA ; ethylenediaminetetraacetic acid ; GC ; gas chromatography ; IC50 ; half maximal inhibitory concentration ; P450c17 ; 17尾-hydroxylase/17 ; 20-lyase ; 17尾-HSD3 or
- 刊名：Journal of Steroid Biochemistry and Molecular Biology
- 出版年：2015
- 出版时间：September 2015
- 年：2015
- 卷：153
- 期：Complete
- 页码：170-178
- 全文大小：1321 K
文摘
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17尾-HSD3 is involved in the formation of androgenic hormone testosterone (T).
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10">RM-532-105 is an androsterone derivative inhibiting 17尾-HSD3.
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15">RM-532-105 inhibits the formation of T in homogenized and whole HEK-293 cells overexpressing 17尾-HSD3.
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RM-532-105 (10 mg/kg, s.c.) reached a plasma concentration of 250 ng/mL at 7 h in rat.