Houssay A B, Epper C E, Varela V, Curbelo H M
Acta Physiol Lat Am. 1978;28(1):11-8.
Several synthetic analogues of cortisol and progesterone were compared to cortisol in their effect of inhibiting the hair growth waves in castrated male C3H/Ep mice. This inhibitory effect was enhanced by fluorination at C-9 alpha and by methylation at C-16 alpha; it decreased by hydroxylation at C-17 alpha and C-21, by removal of hydroxyl group at C-11 and by the addition to bromine to C-12 alpha; it was not modified by oxidation of the hydroxyl group at C-11 or by the delta 1-4 substitution. There was a correlation between the glucocorticoid and hair inhibiting potencies in the cortisol analogues, but some progesterone analogues with very low glucocorticoid activity have marked hair inhibitory effects. No relation was found with the mineralocorticoid effects.
将几种皮质醇和孕酮的合成类似物与皮质醇对去势雄性C3H/Ep小鼠毛发生长波的抑制作用进行了比较。在C-9α位进行氟化和在C-16α位进行甲基化可增强这种抑制作用;在C-17α和C-21位进行羟基化、去除C-11位的羟基以及在C-12α位添加溴会使其降低;C-11位羟基的氧化或δ1-4取代对其无影响。皮质醇类似物的糖皮质激素活性与毛发抑制效力之间存在相关性,但一些糖皮质激素活性非常低的孕酮类似物具有显著的毛发抑制作用。未发现与盐皮质激素作用有相关性。