DANAZOL BINDING AND TRANSLOCATION OF STEROID-RECEPTORS
DANAZOL BINDING AND TRANSLOCATION OF STEROID-RECEPTORS
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DOI：
10.1016/0002-9378(80)90665-1
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发表时间：
1980-01-01
影响因子：
9.8
通讯作者：
PAUERSTEIN, CJ
中科院分区：
文献类型：
--
作者：
CHAMNESS, GC;ASCH, RH;PAUERSTEIN, CJ
达那唑是乙炔睾酮的异恶唑衍生物，可抑制促性腺激素水平并作为弱雄激素发挥作用，竞争性研究表明，达那唑可结合大鼠雄激素受体（Ki [抑制常数] 10-8 M）和孕酮受体（Ki 10-7 M），但不结合雌激素受体。大鼠体内有效的抗促性腺激素剂量仅将雄激素受体转运至靶细胞核;核受体水平保持升高超过6 h。当大鼠子宫与达那唑在体外孵育时，发生相同的易位，表明达那唑的作用是直接的，可能不需要药物的代谢转化。
Danazol, an isoxazol derivative of ethinyl testosterone which suppresses gonadotropin levels and acts as a weak androgen, is shown by competition studies to bind rat androgen receptor (Ki [inhibition constant] 10-8 M) and progestin receptor (Ki 10-7 M) but not estrogen receptor. Effective antigonadotropin doses to the rat in vivo translocate only androgen receptor to target cell nuclei; nuclear receptor levels remain elevated more than 6 h. The same translocation occurs when rat uteri are incubated with danazol in vitro, showing that the action of danazol is direct and probably does not require metabolic conversion of the drug.