摘要
ZK98.734(11β-[4-(N,N-二甲胺基)-苯基]-17β-羟基-17a-(3-羟丙烯-1)-△^(4,9)-雌甾二烯-3-酮)是一种强的抗孕酮剂。本实验用雌激素刺激去卵巢大鼠作为动物模型,观察ZK98.734对垂体胞液中孕激素受体的效应。实验结果表明,在离体情况下ZK98.734能取代~3H-R 5020与大鼠垂体胞液孕激素受体的结合,作用是竞争性的,ZK98.734与垂体胞液孕激素受体的复合物的解离常数为1.99×10^(-9)M;ZK98.734的相对亲和力与R 5020相似。以同样的动物模型进行体内实验,肌肉注射ZK 98.734(1mg/kg)后1小时,测得垂体和子宫内膜的游离孕激素受体结合位点大大下降。ZK98.734的抗生育作用可能与这二个靶组织中孕激素受体的阻断有关。
ZK 98.734 (11β-(4-dimethyl-aminophenyl)-17 β-hydroxy-17α-(3-hydroxy-propyl-enyl)-4, 9(10)-estradien-3-one) is a potent antiprogestin. Estrogen-primed ovariectomizedadult female SD rats were used as the experimental model to determine the binding ofZK 98.734 to the pituitary cytosol progesterone receptors. ZK 98.734 displaced the binding of ~3H-R 5020. Competition studies indicated that therelative binding affinity of ZK 98.734 was as high as that of the potent agonist R 5020. While rats received intramuscular injection of ZK 98.734 (1mg/kg) the free proges-terone binding sites remaining in pituitary and endometrium decreased sharply. Therefore,the antifertility action of ZK 98.734 could be a result of blocking the progesterone recep-tors in both target tissues.
出处
《生殖与避孕》
CAS
CSCD
北大核心
1990年第3期43-47,共5页
Reproduction and Contraception
关键词
ZK98.734
孕激素受体
抗孕酮剂
ZK 98. 734
Cytosol progesterone receptor in pituitary or endometrium
Binding sites
Relative binding affinity
