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采用体外放射配体受体结合法测定3-酮-地索高诺酮(KDG)与兔子宫胞浆雌激素受体(EcR)、孕激素受体(PcR)和大鼠腹侧前列腺胞浆雄激素受体(AcR)结合的亲和力,并以左旋18-甲基炔诺酮(LNG)作对照,从受体水平探讨KDG对当体激素受体的选择性。结果表明:KDG对PcR有很高的亲和力,是LNG的1.5倍;对AcR的亲和力很低,仅为LNG的0.74倍;对EcR几乎没有亲和力,受体亲和力选择系数也明显高于LNG。由此可见,在LNG甾核结构中C11位引入次甲基合成的KDG,其受体亲和力选择性更专一。
In vitro radioligand-receptor binding assay was used to determine the relationship between KDG and the uterine cytosolic estrogen receptor (EcR), progesterone receptor (PcR) and rat ventral prostate cytoplasm Androgen receptor (AcR) binding affinity, and the use of levonorgestrel (LNG) as a control, from the receptor level to explore the KDG when the hormone receptor selectivity. The results showed that: KDG has a high affinity for PcR, which is 1.5 times that of LNG; its affinity for AcR is very low, only 0.74 times that of LNG; almost no affinity for EcR and a significantly high selectivity for receptor affinity In LNG. Thus, introduction of methine-synthesized KDG at the C11 position in the LNG steroid nuclear structure is more specific for its receptor affinity selectivity.