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[吡唑啉酮类制剂对特定III型糖皮质激素受体的激活作用]

[The activation of specific type-III glucocorticoid receptors by pyrazolone series preparations].

作者信息

Golikov P P, Nikolaeva N Iu, Kladiev A A

出版信息

Patol Fiziol Eksp Ter. 1989 Jul-Aug(4):19-22.

PMID:2594422
Abstract

Experiments were conducted on intact and adrenalectomized male Wistar rats (weighing 180-200 g) with labelled corticosterone of high specific activity to study the effect of analgin and aminopyrine on the level of type-III glucocorticoid receptors in the liver. Analgin and aminopyrine in doses of 10(-2) and 10(-3) increase the specific binding of labelled corticosterone by type-III glucocorticoid receptors of the hepatic cytosol and by blood plasma transcortin in modelled experiments. The effect of the agents depends on the dose. Intravenous administration of 140 mg/100 g of analgin to intact rats and intraperitoneal injection of an equal dose of analgin to adrenalectomized rats also increases the specific binding of labelled corticosterone by type-III glucocorticoid receptors of the hepatic cytosol. The importance of the revealed effect of agents of the pyrazolone series in stress regulation is discussed.

摘要

对完整的和肾上腺切除的雄性Wistar大鼠(体重180 - 200克)进行实验,使用高比活度的标记皮质酮,以研究安乃近和氨基比林对肝脏中III型糖皮质激素受体水平的影响。在模拟实验中,剂量为10(-2)和10(-3)的安乃近和氨基比林增加了肝细胞质中III型糖皮质激素受体以及血浆皮质转运蛋白对标记皮质酮的特异性结合。药物的作用取决于剂量。对完整大鼠静脉注射140毫克/100克安乃近,对肾上腺切除大鼠腹腔注射等量安乃近,也增加了肝细胞质中III型糖皮质激素受体对标记皮质酮的特异性结合。讨论了吡唑啉酮系列药物所揭示的作用在应激调节中的重要性。

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