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用人绒毛膜促性腺激素(hCG)升高幼大鼠卵巢cAMP含量及增加幼大鼠储精囊重量的方法,试验了乙二醇二甲磺酸酯及其8种衍生物的抗hCG作用。结果表明:乙二醇二甲磺酸酯、甲磺酸氯乙酯及甲磺酸溴乙酯都有明显抗hCG作用;甘油三甲磺酸酯、丙二醇-1,2-二甲磺酸酯则无此作用;甲磺酸乙酯及甲磺酸-β-苯乙酯有抗hCG的储精囊增重作用,但对卵巢cAMP浓度无明显影响;甲磺酸正丙酯及甲磺酸异戊酯在储精囊增重试验中,表现了抗hCG作用。根据以上实验资料,初步分析了乙二醇二甲磺酸酯类抗hCG作用部位及构效关系。
The effect of human chorionic gonadotropin (hCG) on the ovarian cAMP content in young rats and the increase of seminal vesicle weight in young rats was tested on the anti-hCG effect of ethylene glycol dimethanesulfonate and its eight derivatives. The results showed that both ethylene glycol dimethanesulfonate, chloroethyl methanesulfonate and bromoethyl methanesulfonate have obvious anti-hCG effect; while glycerol trimethanesulfonate and propylene glycol-1,2-dimethanesulfonate No effect; ethyl methanesulfonate and β-phenethyl methanesulfonate anti-hCG seminal vesicle weight gain effect, but no significant effect on cAMP concentration in ovaries; n-propyl methanesulfonate and isoprene mesylate Ester in the seminal vesicle weight gain test showed an anti-hCG effect. Based on the above experimental data, preliminary analysis of ethylene glycol dimethanesulfonate anti-hCG site and structure-activity relationship.