论文部分内容阅读
大鼠,小鼠和仓鼠受孕后第1(d_1),第2(d_2)和第7(d_7)天灌胃(Po)AF-113 0.56—15mg/kg 有明显的抗生育作用。其抗着床ED_(50)大鼠和小鼠分别为1.03(0.66—1.62)和0.54(0.14—2.12)mg/kg,仓鼠为10.0(7.3—13.8)mg/kg。AF—113使幼年大鼠子宫增重的效价为EE 的1.9%;能抑制大鼠子宫内膜蜕膜瘤生长,抑制幼兔子宫内膜增生,但本身无孕激素活性;体外能与大鼠、小鼠和仓鼠子宫胞浆雌激素受体结合,其抑制~3[H]-雌二醇与雌激素受体相结合的IC_(50)分别为2.5±1.1×10~(-5),4.3±2.6×10~(-6)和5.0±0.3×10~(-5)M
Rats, mice and hamsters had significant anti-fertility effects on the 1st (d_1), 2nd (d_2) and 7th (d_7) days of intragastric administration of 0.56-15 mg / kg Po. The anti-implantation ED 50 rats and mice were 1.03 (0.66-1.62) and 0.54 (0.14-2.12) mg / kg, respectively, and the hamsters were 10.0 (7.3-13.8) mg / kg. AF-113 makes juvenile rat uterus weight gain of 1.9% of EE; can inhibit the growth of rat endometrial decidual tumors, inhibit the rabbit endometrial hyperplasia, but itself no progestogenic activity; in vitro and large The IC50 of inhibiting the binding of ~ 3 [H] -estradiol to the estrogen receptor in mice, mice and hamsters was 2.5 ± 1.1 × 10 ~ (-5) 4.3 ± 2.6 × 10 -6 and 5.0 ± 0.3 × 10 -5 M, respectively