Steinmeyer A, Neef G, Kirsch G, Schwarz K, Rach P, Haberey M, Thieroff-Ekerdt R
Research Laboratories of Schering AG, Berlin, Germany.
Steroids. 1992 Sep;57(9):447-52. doi: 10.1016/0039-128x(92)90099-u.
8(14)a-Homocalcitriol was synthesized and tested for its biologic activities. It exhibited a vitamin D agonist activity profile. The compound was bound to the pig intestinal receptor with an affinity slightly less than calcitriol, showed the same potency in inducing HL 60 cell differentiation and inhibition of keratinocyte proliferation as calcitriol, and was found to be approximately 10-fold less potent in inducing hypercalcemia and hypercalciuria after a single injection in normal rats.
合成了8(14)a-高骨化三醇并对其生物活性进行了测试。它呈现出维生素D激动剂的活性特征。该化合物与猪肠道受体结合，亲和力略低于骨化三醇，在诱导HL-60细胞分化和抑制角质形成细胞增殖方面与骨化三醇具有相同的效力，并且在正常大鼠单次注射后诱导高钙血症和高钙尿症的效力约低10倍。
