Koch B, Lutz-Bucher B, Briaud B, Mialhe C
Neuroendocrinology. 1979;28(3):169-77. doi: 10.1159/000122859.
This study reports on the kinetics of glucocorticoid-induced inhibition of ACTH release, together with steroid binding to specific pituitary receptors. It was shown that corticosterone (CORT) inhibited ACTH output provoked by either corticotropin-releasing factor (CRF) extracts or dbcAMP, in a manner which was both dose- and time-dependent. A close correlation appeared to exist between the degree of ACTH blockade and the percentage of filled steroid-binding sites. However, exposure of hypophyses to CORT for a critical period of time was a prerequisite for such a relationship to develop. Furthermore, it was found that dexamethasone (DEX) was more potent than CORT in inhibiting ACTH secretion and, in addition, bound to a greater extent to nuclei of pituitary cells. These data suggest the existence of a close correlation between occupancy of pituitary glucocorticoid receptors and modulation of ACTH secretion.
本研究报告了糖皮质激素诱导促肾上腺皮质激素(ACTH)释放抑制的动力学,以及类固醇与垂体特异性受体的结合情况。结果表明,皮质酮(CORT)以剂量和时间依赖性方式抑制促肾上腺皮质激素释放因子(CRF)提取物或二丁酰环磷腺苷(dbcAMP)引发的ACTH分泌。ACTH阻断程度与类固醇结合位点的填充百分比之间似乎存在密切相关性。然而,垂体在关键时间段暴露于CORT是这种关系形成的先决条件。此外,还发现地塞米松(DEX)在抑制ACTH分泌方面比CORT更有效,并且在更大程度上与垂体细胞的细胞核结合。这些数据表明垂体糖皮质激素受体的占据与ACTH分泌的调节之间存在密切相关性。