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16,17-吡唑雌酮(16,17-PES)是一个以雌酮为母体而合成的雌酮衍生物。前曾报道,它的雌激素样活性仅为雌酮的1/3或1/15,但却具有与雌酮相同的降血脂作用。本研究用大鼠重复了雌激素活性的测定,获得与过去相似的结果。同时证明,它们的雌激素活性与子宫雌激素受体浓度之间存在着平行关系,即经雌酮和16,17-PES处理的动物,无论按每个子宫所含受体数目或每mg蛋白所含受体浓度,前者均显著高于后者。但体外试验表明,二者取代~3H-雌二醇与雌激素受体结合的竞争曲线几乎完全重叠,说明二者对受体的亲和力是相等的。大鼠注射同一剂量的雌酮和16,17-PES后,它们在子宫内的分布量分别为69.0和38.4μg/g,这一结果可用来解释二者雌激素活性的差异,也可解释子宫受体数目的差异。油水分布系数的测定未能说明雌酮和16,17-PES在子宫分布量的不同。
16,17-Pyrazole Estrone (16,17-PES) is an estrone derivative synthesized from estrone as the parent. It has previously been reported that its estrogenic activity is only one-third or one-fifth that of estrone but that it has the same lipid-lowering effect as estrone. The present study repeated the estrogen activity assay in rats to obtain similar results as in the past. At the same time, it has been demonstrated that there is a parallel relationship between their estrogenic activity and uterine estrogen receptor concentration, ie estrone and 16,17-PES treated animals, irrespective of the number of receptors per uterus or per mg of protein Contained receptor concentrations, the former were significantly higher than the latter. However, in vitro experiments showed that the competition between the two substituted ~ 3H-estradiol and estrogen receptor almost completely overlapped, indicating that their affinity for the receptor is equal. After injections of the same dose of estrone and 16,17-PES in rats, their distribution in the womb were 69.0 and 38.4 μg / g, respectively. This result can be used to explain the differences in estrogen activity between the two groups, as well as in the uterus Differences in the number of receptors. The determination of oil-water distribution coefficient failed to account for the difference in the amount of estrone and 16,17-PES in the uterus.