Gestrinone 是一种合成类固醇，偶尔用于治疗子宫内膜异位症。子宫内膜异位症是一种常见疾病，其特征是子宫外存在子宫内膜组织，约占绝经前妇女的10％。它主要作用于下丘脑-垂体系统，以抑制促黄体激素（LH）和促卵泡激素（FSH）的释放，从而减少雌激素的合成。它也与人子宫内膜组织中的雄激素（AR），孕酮（PR）和雌激素（ER）受体结合，但不与类固醇激素结合球蛋白或与皮质激素结合的球蛋白结合。孕酮与AR和PR结合的EC | 50 |值分别约为20和30 nM。这些值反映出对这些受体的亲和力比睾丸激素和孕酮 用途： Gestrinone (R2323) 是用于治疗子宫内膜异位症的合成类固醇激素。抑制平滑肌瘤的IC50值为43.67 μM。 Gestrinone is a synthetic steroid occasionally used to treat endometriosis. The common disease endometriosis is characterized by the presence of endometrial tissue outside the uterus which affects approximately 10% of premenopausal women. It acts centrally on the hypothalamic-pituitary system to suppress release of lutenizing hormone (LH) and follicle-stimulating hormone (FSH), thus reducing estrogen synthesis. It also binds to androgen (AR), progesterone (PR), and estrogen (ER) receptors in the human endometrial tissue but not to steroid hormone binding globulin or corticord-binding globulin. Gestrinone binds to AR and PR with EC|50|values of approximately 20 and 30 nM, respectively. These values reflect approximately 5-6 fold lower affinity than testosterone and progesterone, the natural AR and PR ligands, for these receptors.