Luzzani F, Glässer A
Eur J Pharmacol. 1981 Dec 17;76(4):427-30. doi: 10.1016/0014-2999(81)90115-1.
Deflazacort, a new steroidal anti-inflammatory agent, has remarkable glucocorticoid activity in both animals and humans. Its biologically active form, 21-desacetyl deflazacort, displaces [3H]dexamethasone from its cytosol receptor sites in rat kidney, thymus and liver in vitro. Although less active than prednisolone in its binding to glucocorticoid receptors, deflazacort 'stabilizes' the resulting steroid-receptor complex more effectively than the former in the kidney and thymus but not in the liver. This property might explain the greater activity of deflazacort than of prednisolone in the rat.
地夫可特是一种新型甾体抗炎药，在动物和人类中均具有显著的糖皮质激素活性。其生物活性形式21-去乙酰地夫可特，在体外可将大鼠肾脏、胸腺和肝脏细胞质中的[3H]地塞米松从其受体位点上置换下来。尽管地夫可特与糖皮质激素受体结合的活性低于泼尼松龙，但其在肾脏和胸腺中比泼尼松龙更有效地“稳定”所形成的类固醇-受体复合物，而在肝脏中则不然。这一特性可能解释了地夫可特在大鼠中比泼尼松龙具有更强活性的原因。
