促肾上腺皮质激素、β-内啡肽、吗啡及纳洛酮对离体肾上腺皮质醇释放的影响。

Effect of ACTH, beta-endorphin, morphine and naloxone on the release of cortisol by isolated adrenal glands.

作者信息

Bruni G, Dal Pra P, Fiaschi A I, Segre G

出版信息

Pharmacol Res Commun. 1985 Sep;17(9):847-53. doi: 10.1016/0031-6989(85)90043-8.

Abstract

The release of cortisol (determined by RIA) from isolated slices of adrenal glands of guinea pigs is stimulated by ACTH, by beta-endorphin, and by morphine in a concentration-dependent way; naloxone gives a small stimulation which is not related to its concentration. Naloxone inhibits the effect of ACTH (1.11 X 10(-11) M) in a competitive manner with an IC50 of about 3.10(-9) M. Also morphine and beta-endorphin inhibit the effect of ACTH, but not in competitive manner. Naloxone (10(-9)-10(-7) M) gives a concentration-related inhibition of the increase of cortisol release produced by morphine (10(-8) M) and by beta-endorphin (1.44 X 10(-10) M). These data suggest a similarity in the conformation of ACTH, beta-endorphin, morphine and naloxone towards the binding sites of ACTH of the guinea pig adrenal glands.

摘要

豚鼠肾上腺分离切片中皮质醇（通过放射免疫分析测定）的释放受到促肾上腺皮质激素（ACTH）、β-内啡肽和吗啡的浓度依赖性刺激；纳洛酮产生的微小刺激与其浓度无关。纳洛酮以竞争性方式抑制ACTH（1.11×10⁻¹¹ M）的作用，半数抑制浓度（IC50）约为3.10⁻⁹ M。吗啡和β-内啡肽也抑制ACTH的作用，但并非以竞争性方式。纳洛酮（10⁻⁹ - 10⁻⁷ M）对吗啡（10⁻⁸ M）和β-内啡肽（1.44×10⁻¹⁰ M）所产生的皮质醇释放增加呈现浓度相关的抑制作用。这些数据表明，ACTH、β-内啡肽、吗啡和纳洛酮在豚鼠肾上腺ACTH结合位点的构象上具有相似性。