两种新型高选择性抗孕激素Org 31710和Org 31806的药理学

Pharmacology of two new very selective antiprogestagens: Org 31710 and Org 31806.

作者信息

Kloosterboer H J, Deckers G H, Schoonen W G

机构信息

Organon Scientific Development Group, Department of Endocrinology, Oss, The Netherlands.

出版信息

Hum Reprod. 1994 Jun;9 Suppl 1:47-52. doi: 10.1093/humrep/9.suppl_1.47.

DOI:10.1093/humrep/9.suppl_1.47

PMID:7962469

Abstract

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.

摘要

Org 31710和Org 31806是新型抗孕激素。对这些化合物进行了测试，以检测它们与各种甾体受体的结合亲和力以及在各种动物模型中的生物活性，并将结果与RU38486和ZK 98299的结果进行比较。两种Org化合物都是强效抗孕激素，几乎没有抗糖皮质激素活性，除了一些微弱的雄激素和抗雄激素活性外，没有其他激素活性。这两种化合物在抗孕激素活性方面比RU38486和ZK 98299更强，且更具选择性。Org化合物在7,12-二甲基苯并(a)蒽（DMBA）大鼠模型中可有效抑制肿瘤发展。Org 31710和Org 31806可用于治疗乳腺肿瘤和改善生育控制。