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[非甾体类药物作用下肝细胞细胞核中糖皮质激素受体功能的变化及糖皮质激素受体复合物的转位]

[Change in the function of glucocorticoid receptors and translocation of glucocorticoid receptor complexes in hepatocyte nuclei exposed to nonsteroidal drugs].

作者信息

Golikov P P

出版信息

Patol Fiziol Eksp Ter. 1991(6):34-6.

PMID:1818283
Abstract

Experiments were conducted on male Wistar rats weighing 180-200 g to study the effect of medical agents (Tizercin 3,5.10(-4) M, 7,0.10(-4) M, Cephazolin, streptomycin and penicillin C--10(-3) M, 10(-4) M) on the function of glucocorticoid receptors of hepatic cytosol and translocation of the glucocorticoid-receptor complexes into the nuclei of hepatocytes. Synthetic labeled ligands 3H-dexamethasone and triamcinolone 3H-acetonide were used. Their specific activity was, respectively, 20 and 22 Ci/mmol The association and dissociation constants and the number of glucocorticoid-receptor complexes after their translocation into the hepatocyte nuclei were determined by Sketcher's method. It was found that streptomycin and Tizercin inhibit while Cephazolin and penicillin C activate the function of glucocorticoid receptors. Translocation of glucocorticoid-receptor complexes into the hepatocyte nuclei does not change under the effect of these agents.

摘要

对体重180 - 200克的雄性Wistar大鼠进行实验,以研究药物(替策林3,5.10(-4)M、7,0.10(-4)M、头孢唑林、链霉素和青霉素C - 10(-3)M、10(-4)M)对肝细胞溶胶糖皮质激素受体功能以及糖皮质激素 - 受体复合物向肝细胞核内转运的影响。使用了合成标记配体3H - 地塞米松和3H - 曲安奈德。它们的比活性分别为20和22 Ci/mmol。采用Sketcher方法测定了糖皮质激素 - 受体复合物向肝细胞核内转运后的结合和解离常数以及其数量。结果发现,链霉素和替策林具有抑制作用,而头孢唑林和青霉素C具有激活糖皮质激素受体功能的作用。在这些药物的作用下,糖皮质激素 - 受体复合物向肝细胞核内的转运没有变化。

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