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应用放射配体结合法,比较了21-氨基类固醇U72099E在胞液、完整胸腺细胞及突触质膜中对标记糖皮质激素与其受体结合的竞争能力。结果显示,U72099E的竞争能力在胞液为零,在完整细胞较低,而在突触质膜非常高,提示质膜上存在U72099E的结合部位(很可能是糖皮质激素的膜受体)。U72099E在突触质膜的抑制常数Ki(32.16±1.65 μmol/L)与其模拟糖皮质激素对抗脑损伤的作用所需浓度相近,提示糖皮质激素膜受体可能介导U72099E的有益作用。
Radioligand binding assay was used to compare the competitive ability of 21-aminosteroid U72099E on the binding of labeled glucocorticoids to their receptors in cytosol, intact thymocytes and synaptic membranes. The results showed that the competitive ability of U72099E was zero in the cytosol, lower in intact cells and very high in the synaptic plasma membrane, suggesting the presence of a U72099E binding site on the plasma membrane, most likely a glucocorticoid membrane receptor. The inhibitory constant Ki of Synaptic plasma membrane (32.16 ± 1.65 μmol / L) was similar to that of U72099E in simulating the effect of glucocorticoid on brain damage, suggesting that glucocorticoid membrane receptor might mediate the beneficial effect of U72099E.