Luzzani F, Barone D, Galliani G, Glässer A
Eur J Pharmacol. 1983 Jan 28;87(1):61-6. doi: 10.1016/0014-2999(83)90050-x.
The interaction of glucocorticoids with thymic cytosol receptors in the adrenalectomized rat was studied by a method based on their capacity to deplete cytosol receptors when administered in vivo. Three h after a single oral administration of reference steroids at various dose levels, thymus cytosol aliquots were incubated with a saturating concentration of [3H]dexamethasone (30 nM) for 24 h at 0-2 degrees C with and without 2000 nM unlabeled dexamethasone. Bound radioactivity was determined by dextran-coated charcoal adsorption. The depletion of cytosol receptors was dose-dependent for each glucocorticoid, with the following ED50 (mg/kg): fluocinolone acetonide 0.032, dexamethasone 0.09, triamcinolone acetonide 0.12, betamethasone 0.24, deflazacort 0.55, triamcinolone 1.6, prednisolone 4.0, hydrocortisone 17.0. A striking correlation (r 0.991) between ex vivo receptor binding and thymolytic effect was observed. When data from in vitro competition studies were compared with those obtained in ex vivo experiments, the latter were correlated more tightly with the biological response.
通过一种基于糖皮质激素在体内给药时耗尽胞质溶胶受体能力的方法，研究了肾上腺切除大鼠中糖皮质激素与胸腺胞质溶胶受体的相互作用。在以不同剂量水平单次口服给予参比甾体激素三小时后，将胸腺胞质溶胶等份在有和没有2000 nM未标记地塞米松的情况下，与饱和浓度的[3H]地塞米松（30 nM）在0-2℃下孵育24小时。通过葡聚糖包被的活性炭吸附法测定结合的放射性。每种糖皮质激素的胞质溶胶受体耗尽呈剂量依赖性，其半数有效剂量（ED50，mg/kg）如下：醋酸氟轻松0.032、地塞米松0.09、曲安奈德0.12、倍他米松0.24、地夫可特0.55、曲安西龙1.6、泼尼松龙4.0、氢化可的松17.0。观察到离体受体结合与胸腺溶解作用之间存在显著相关性（r = 0.991）。当将体外竞争研究的数据与离体实验获得的数据进行比较时，后者与生物学反应的相关性更强。
