Lin A L, McGill H C, Shain S A
Circ Res. 1982 May;50(5):610-6. doi: 10.1161/01.res.50.5.610.
We used the synthetic progestin R5020 (17 alpha, 21-dimethyl-19-norpregna-4,9-diene-3,20-dione) to characterize cytoplasmic progesterone receptors in baboon (Papio sp.) aorta and myocardium. The relative ability of selected steroids to inhibit binding of radiolabeled R5020 to aortic cytoplasmic progesterone receptors was radioinert R5020, 1.0; progesterone, 0.31; triamcinolone acetonide, 0.06; testosterone, 0.002; estradiol-17 beta, 0.01; and cortisol. 0.001. The relative ability of these same steroids to inhibit binding of radiolabeled R5020 to myocardial cytoplasmic progesterone receptors was, respectively, 1.0, 0.58, 0.21, 0.01, 0.01, and 0.001. Both aortic and myocardial cytoplasmic progesterone receptors migrated as macromolecules with a sedimentation coefficient of 8-9S on low ionic strength linear sucrose gradients. Cytoplasmic binding of R5020 was inactivated by incubation of 37 degrees C. Saturation analysis at 2 degrees C showed aorta and myocardium, respectively, contained 41.6 +/- 16.1 (mean +/- SD) and was 14.0 +/- 2.8 fmol R5020 binding sites/mg cytosol protein. The dissociation constant for R5020 was 2.8 +/- 1.2 nM, aorta, and 2.0 +/- 1.1 nM, myocardium. The presence of progesterone receptors in baboon cardiovascular tissues suggests that progestins may directly influence cardiovascular tissue function.
我们使用合成孕激素R5020（17α，21 - 二甲基 - 19 - 去甲孕甾 - 4,9 - 二烯 - 3,20 - 二酮）来鉴定狒狒（Papio sp.）主动脉和心肌中的细胞质孕酮受体。所选类固醇抑制放射性标记的R5020与主动脉细胞质孕酮受体结合的相对能力为：无放射性的R5020，1.0；孕酮，0.31；曲安奈德，0.06；睾酮，0.002；雌二醇 - 17β，0.01；皮质醇，0.001。这些相同类固醇抑制放射性标记的R5020与心肌细胞质孕酮受体结合的相对能力分别为1.0、0.58、0.21、0.01、0.01和0.001。在低离子强度线性蔗糖梯度上，主动脉和心肌细胞质孕酮受体均以沉降系数为8 - 9S的大分子形式迁移。R5020的细胞质结合在37℃孵育时失活。在2℃进行的饱和分析表明，主动脉和心肌分别含有41.6±16.1（平均值±标准差）和14.0±2.8 fmol R5020结合位点/毫克胞质溶胶蛋白。R5020在主动脉中的解离常数为2.8±1.2 nM，在心肌中为2.0±1.1 nM。狒狒心血管组织中存在孕酮受体表明孕激素可能直接影响心血管组织功能。
