Sirett D A, Grant J K
J Steroid Biochem. 1982 Apr;16(4):553-5. doi: 10.1016/0022-4731(82)90078-4.
Saturable, high affinity binding of [3H]-promegestone has been observed in sheep liver cytosol. In two tissues specimens the Kd values were 5.9 and 6.3 nmol/l, and the concentrations of binding sites were 84.5 and 66.2 pmol/g wet tissue respectively. The synthetic steroids methyltrienolone and ORG 2058 were capable of some degree of competition. Progesterone was a weak competitor; cortisol, dexamethasone and testosterone were ineffective. Bound promegestone in liver cytosol was taken up by liver nuclei, but not by sheep uterine nuclei. These promegestone-binding sites are neither progesterone or glucocorticoid receptors.
在绵羊肝脏胞质溶胶中观察到了[3H]-孕美孕酮的可饱和、高亲和力结合。在两个组织样本中,解离常数(Kd)值分别为5.9和6.3纳摩尔/升,结合位点浓度分别为84.5和66.2皮摩尔/克湿组织。合成类固醇甲基三烯醇酮和ORG 2058具有一定程度的竞争能力。孕酮是一种较弱的竞争者;皮质醇、地塞米松和睾酮则无作用。肝脏胞质溶胶中结合的孕美孕酮被肝细胞核摄取,但不被绵羊子宫细胞核摄取。这些孕美孕酮结合位点既不是孕酮受体也不是糖皮质激素受体。