Tamaya T, Fujimoto J, Watanabe Y, Arahori K, Okada H
Acta Obstet Gynecol Scand. 1986;65(5):439-41. doi: 10.3109/00016348609157380.
To understand the mechanism of biological action of gestrinone (R2323), which has a therapeutic effect against endometriosis, the binding of gestrinone to numerous classes of intracellular steroid binding proteins was studied in the human uterine endometrium. Gestrinone bound to endometrial receptors for estrogen, progesterone and androgen, but seemed not to bind to endometrial intracellular corticosteroid-binding globulin and sex hormone-binding globulin. Gestrinone occupies all specific binding sites of steroids in the steroid target cells despite the presence of endogenous steroids. It is speculated that the binding behavior of gestrinone may be related to its therapeutic effect on endometriosis. Gestrinone's more avid affinity for estrogen receptor may be the reason for the ability to use a lower clinical dose of gestrinone.
为了解具有治疗子宫内膜异位症作用的孕三烯酮（R2323）的生物学作用机制，对人子宫内膜中孕三烯酮与多种细胞内类固醇结合蛋白的结合情况进行了研究。孕三烯酮可与雌激素、孕激素和雄激素的子宫内膜受体结合，但似乎不与子宫内膜细胞内的皮质类固醇结合球蛋白和性激素结合球蛋白结合。尽管存在内源性类固醇，孕三烯酮仍占据类固醇靶细胞中类固醇的所有特异性结合位点。推测孕三烯酮的结合行为可能与其对子宫内膜异位症的治疗作用有关。孕三烯酮对雌激素受体具有更高的亲和力，这可能是其能够使用较低临床剂量的原因。
