康力龙、达那唑、与自然的雄激素,与低亲和力glucocorticoid-binding网站交互雄性大鼠肝微粒体。

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费尔南德斯L, Chirino R, Boada LD,纳瓦罗D,卡布瑞拉N,德尔里奥我Diaz-Chico BN

康力龙、达那唑、与自然的雄激素,与低亲和力glucocorticoid-binding网站交互雄性大鼠肝微粒体。

内分泌学。1994年3月,134 (3):1401 - 8。doi: 10.1210 / endo.134.3.8119180。

PubMed ID

8119180 (在PubMed

]

文摘

一些17 alpha-alkylated雄激素用作合成药物,如康力龙(ST)和达那唑(DA),有具体的对肝脏的影响,不产生睾丸激素。这产生的可能性类固醇结合蛋白质,除了雄激素受体,可以调节细胞内这些代理的行为。雄性大鼠肝微粒体包含了一个均匀的[3 h]地塞米松([3 h]敏捷)绑定网站我们计价低亲和力glucocorticoid-binding网站(滞后)。因为糖皮质激素、progestagens和合成雌激素乙炔基雌二醇与[3 h]敏捷竞争绑定滞后,我们旨在研究雄激素之间可能的相互作用和滞后。调查几个雄激素是否与滞后交互的能力,我们执行竞争实验。落后没有亲和力睾酮或methyltrienolone (R1881)。然而,一些17 alpha-alkylated雄激素(DA (IC50, 116海里)>圣> > fluoxymesterone > mestaline >美雄醇> > methandrostenolone > methyltestosterone)能够与[3 h]敏捷竞争结合肝微粒体。圣和DA强有力的抑制剂[3 h]敏捷绑定到肝微粒体。他们减少了亲和力和[3 h] DEX-binding网站的数量,增加了离解率[3 h]敏捷的滞后,并引发了时间和剂量依赖性失活[3 h] DEX-binding网站。这些结果强烈表明,ST和DA施加负变构调节滞后[3 h]敏捷绑定。 The in vivo administration of ST (but not other androgens) to male rats provoked a time- and dose-dependent decrease in the LAGS level. Full recovery of the LAGS concentration required at least 8 h and was blocked by protein synthesis inhibitors. Such results suggest that ST irreversibly inactivates the [3H]DEX-binding site in vivo as it does in vitro. Taken together, these observations are indicative of an irreversible interaction between some 17 alpha-alkylated androgens and the LAGS both in vitro and in vivo and suggest that ST may be an important pharmacological tool that can be used in the elucidation of the molecular structure of the LAGS. These results also mean that the LAGS are a steroid-binding entity able to distinguish between natural androgens and 17 alpha-alkylated testosterone derivatives used as anabolic agents.

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药物靶点

药物	目标	类	生物	药理作用	行动
Fluoxymesterone	雄性激素受体	蛋白质	人类	是的	受体激动剂	细节
康力龙	糖皮质激素结合蛋白	集团	人类	未知的	粘结剂	细节