Golikov P P, Udovichenko V I, Kalinin V N, Kozhevnikova L M, Nikolaeva N Iu, Marchenko V V, Moiseev S K
Patol Fiziol Eksp Ter. 1996 Jan-Mar(1):9-13.
The effects of opiate receptor agonists and antagonists on the function of glucocorticoid receptors in the hepatic cytosol were examined in male Wistar rats weighing 180-240 g. With the Scatchard analysis, in vitro experiments by using labelled ligands revealed that the pure opiate agonist morphine in the wide range of concentrations (0,01-10,0 mM) failed to affect the function Type II glucocorticoid receptors, though inhibited the function of Type III glucocorticoid receptors in the dose-dependent manner. Buprenorphine and diprenorphine depressed the function of Types II and III glucocorticoid receptors. Buterphanol, an opiate receptor antagonist-agonist, like naltrexone, an opiate receptor antagonist, decreased the function of Type III glucocorticoid receptors, but modulated that of Type II glucocorticoid receptors by lowering the association constant of the ligand-Type II glucocorticoid receptor complex, but by enhancing the density of Type II glucocorticoid receptors. In vivo studies established that butorphanol dose-dependently increased the density of Type II glucocorticoid receptors in the hepatic cytosol and elevating blood pressure in rat traumatic shock. Whether glucocorticoid receptors involve in the mechanism of the antishock effect of morphine derivatives is discussed in the paper.
在体重为180 - 240克的雄性Wistar大鼠中,研究了阿片受体激动剂和拮抗剂对肝细胞溶质中糖皮质激素受体功能的影响。通过Scatchard分析,使用标记配体的体外实验表明,在广泛浓度范围(0.01 - 10.0 mM)内,纯阿片激动剂吗啡未能影响II型糖皮质激素受体的功能,但以剂量依赖方式抑制了III型糖皮质激素受体的功能。丁丙诺啡和二丙诺啡抑制了II型和III型糖皮质激素受体的功能。阿片受体拮抗剂 - 激动剂布托啡诺与阿片受体拮抗剂纳曲酮一样,降低了III型糖皮质激素受体的功能,但通过降低配体 - II型糖皮质激素受体复合物的结合常数,但增加II型糖皮质激素受体的密度,调节了II型糖皮质激素受体的功能。体内研究表明,布托啡诺在大鼠创伤性休克中剂量依赖性地增加了肝细胞溶质中II型糖皮质激素受体的密度并升高了血压。本文讨论了糖皮质激素受体是否参与吗啡衍生物抗休克作用的机制。