Gaillard R C, Poffet D, Riondel A M, Saurat J H
J Clin Endocrinol Metab. 1985 Dec;61(6):1009-11. doi: 10.1210/jcem-61-6-1009.
RU 486 [17 beta-hydroxy-11 beta-(4-dimethylaminophenyl)17 alpha-(prop-1-ynyl)estra-4,9-dien-3-one] is a synthetic steroid receptor antagonist. To evaluate the peripheral antiglucocorticoid action of this compound, we investigated its ability to antagonize cutaneous steroid-induced vasoconstriction. This phenomenon, produced by three different topical steroids in six normal men, was consistently and significantly attenuated or abolished by oral administration of 6 mg/kg RU 486. This demonstration of a peripheral action of RU 486 is important in relation to the potential therapeutic use of this well tolerated drug in states of hypercortisolism. It also indicates that the cutaneous vasoconstrictor effects of topical steroids are mediated by occupancy of glucocorticoid receptors.
RU 486 [17β - 羟基 - 11β -（4 - 二甲基氨基苯基）- 17α -（丙 - 1 - 炔基）雌甾 - 4,9 - 二烯 - 3 - 酮]是一种合成类固醇受体拮抗剂。为评估该化合物的外周抗糖皮质激素作用，我们研究了其拮抗皮肤类固醇诱导的血管收缩的能力。在六名正常男性中，由三种不同的局部类固醇引起的这种现象，通过口服6毫克/千克的RU 486可持续且显著地减弱或消除。RU 486外周作用的这一证明对于这种耐受性良好的药物在皮质醇增多症状态下的潜在治疗用途具有重要意义。这也表明局部类固醇的皮肤血管收缩作用是由糖皮质激素受体的占据介导的。
