摘要
本文观察了乙炔雌二醇(EE)、双炔失碳醇(AF-45)和双炔失碳酯(AF-53)的相对子宫增重效价、与子宫胞浆雌二醇受体(ERc)的相互作用特性和抗生育效应由此分析三者的雌激素活性和抗生育效应的关系。结果指示,三者在竞争[^3H]-E2结合大鼠子宫胞浆ERc的能力和相对子宫增重效价相平行,若以EE的子宫胞浆ERc的相对结合亲和力(RBA)和相对子宫增重效价的比值为1,则AF-45的比值接近于1。
This report is on relative Estrongenicity potency,relative binding affinity(RBA)for uterinecytosol Estradiol receport and relative antiftertility potency by an Ethynyl estradiol(EE).Anorstoroide(AF-45),Anordin(AF-53)in rats and to detrnonstrate the relationship between their hormornalactivities and antifertillty effects.The RBA of the three compounds for uterine cytosol estradiol receporsparalleled the relative potenc of uterine weight.As the ratio of RBA and relative potency of uterineweight for EE was equal to 1,the ratio AF-45 was close to 1 and the ratio for AF-53<1.It hasbeen dechled through petalled comparison that if value of EE antifertillty effect and estrgenieityrelative potency was equal to 1,the ratio value of AF-45 or AF-53 is 22.64 or 15.7 when theywere used for the antionplantation;as the terminating early pregnancy,the value of AF-45 or AF-53is 5.7 or 4.5.Similary,if the rarions of antifertility effect and RBA was equal to 1,the value ofAF-45 was 19.1 or 3.84 when they were used for the antionplantation or the termining earlyprenaney.It was clear that the antifertitility effect of AF-45 or AF-53 was not parallels with relativeostogenicity potency.The estigenicity potency was not the only factor,which set off the antigertilityeffect of AF-45 and AF-53,there existed differentiation to a certain extent,it was suggested that theRBA of AF-45,and AF-53 for urerine cytosol estradiol recetors in was been markedly different,which might be associated with the substilution of diproprionte on 2 and 17 possitiom of AF-53.
出处
《生殖与避孕》
CAS
CSCD
北大核心
1993年第5期336-341,共6页
Reproduction and Contraception
关键词
双炔失碳甾体
雌激素活性
药理学
EE,AF-45,AF-53,Uteine-REc,RVA,Relative estogenicity potency,AF-realtive potency