【摘要】 大鼠,小鼠和仓鼠受孕后第1（d₁）,第2（d₂）和第7（d₇）天灌胃（Po）AF-113 0.56—15mg/kg 有明显的抗生育作用。其抗着床ED₅₀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IC₅₀分别为2.5±1.1×10^-5,4.3±2.6×10^-6和5.0±0.3×10^-5M更多还原

【Abstract】 AF-113,an analogue of anordrin,was proved to have antifertility effects in rats,miceand hamsters at a dose of 0.56-15 mg/kg.It had no progesterone activity on immaturerabbits as indicated by McPhail index,while the deciduoma weight in pseudopregnancy ratswas decreased significantly at antifertility dose level.The estrogenicity of AF-113 was similarto anordrin in the increase of uterine weight,but lower than anordrin in the cornification ofvaginal epithelium in overiectomized adult mice.In vivo,AF-113 showed a lower bindingrate to cytosol estrogen receptors in the uterus of rats,mice and hamsters.更多还原