Gjerde H, Gadeholt G, Olsen H, Mørland J, Norman N
Acta Pharmacol Toxicol (Copenh). 1985 Jul;57(1):36-9. doi: 10.1111/j.1600-0773.1985.tb00006.x.
11-Deoxycortisol (cortexolone) has previously been used as a glucocorticoid antagonist in vitro and in adrenalectomized rats. Antiglucocorticoid properties of 11-deoxycortisol in intact rats were examined by studying the effect of 11-deoxycortisol on the induction of hepatic tryptophan oxygenase (TO) by corticosterone. No antiglucocorticoid effect was observed. When 11-deoxycortisol was injected into rats, the TO activity increased. This was probably mainly caused by an elevation of the serum corticosterone level. The induction of TO by 11-deoxycortisol was inhibited by metyrapone. However, 11-deoxycortisol (100 mg/kg) was still not a glucocorticoid antagonist even in presence of metyrapone.
11-脱氧皮质醇(皮质素原)此前已在体外和肾上腺切除的大鼠中用作糖皮质激素拮抗剂。通过研究11-脱氧皮质醇对皮质酮诱导肝色氨酸加氧酶(TO)的影响,检测了其在完整大鼠中的抗糖皮质激素特性。未观察到抗糖皮质激素作用。当向大鼠注射11-脱氧皮质醇时,TO活性增加。这可能主要是由血清皮质酮水平升高引起的。美替拉酮可抑制11-脱氧皮质醇对TO的诱导作用。然而,即使存在美替拉酮,11-脱氧皮质醇(100 mg/kg)仍不是糖皮质激素拮抗剂。