PHARMACOLOGY OF 2 NEW VERY SELECTIVE ANTIPROGESTAGENS - ORG-31710 AND ORG-31806
PHARMACOLOGY OF 2 NEW VERY SELECTIVE ANTIPROGESTAGENS - ORG-31710 AND ORG-31806
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DOI：
10.1093/humrep/9.suppl_1.47
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发表时间：
1994-06-01
影响因子：
6.1
通讯作者：
SCHOONEN, WGEJ
中科院分区：
文献类型：
--
作者：
KLOOSTERBOER, HJ;DECKERS, GH;SCHOONEN, WGEJ
组织31710和组织31806是新的抗孕药。在不同的动物模型上测试了这些化合物与各种类固醇受体的结合亲和力和生物活性，并与RU38486和ZK 98299的结果进行了比较。这两个有机化合物都是强的抗孕激素，几乎没有抗糖皮质激素的活性，除了一些弱的雄激素和抗雄激素活性外，没有其他激素活性。这两个化合物在抗孕激素活性方面比RU38486和ZK 98299更有效，而且更具选择性。有机化合物能有效地抑制7，12-二甲基苯并(A)菲(DMBA)大鼠模型肿瘤的发展。ORG 31710和ORG 31806可用于治疗乳腺肿瘤和改善生育控制。
Org 31710 and Org 31806 are new antiprogestagens. These compounds were tested for their binding affinity to various steroid receptors and for their bio-activity in various animal models and the results were compared with those of RU38486 and ZK 98299. Both Org compounds are strong antiprogestagens with little antiglucocortocoid activity and are devoid of other hormonal activities except for some weak androgenic and anti-androgenic activity. The two compounds are more potent than RU38486 and ZK 98299 with respect to their anti-progestational activity and are more selective. The Org compounds are effective in inhibiting the development of tumours in the 7,12-dimethylbenz(a)anthracene (DMBA) rat model. Org 31710 and Org 31806 may be applied for both the treatment of breast tumours and the improvement of fertility control.