孕三烯酮与兔子宫雌激素与孕激素受体的亲和力测定  

Affinity of gestrinone to estrogen and progestin receptors of uterine cytosol in rabbits

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作  者:桂耀庭[1,2] 吴昌杰[1,2] 吴熙瑞 

机构地区:[1]深圳市红十字会医院中西医结合研究所 [2]同济医科大学生殖医学中心

出  处:《中国药理学与毒理学杂志》1997年第1期77-78,共2页Chinese Journal of Pharmacology and Toxicology

摘  要:孕三烯酮与兔子宫雌激素与孕激素受体的亲和力测定桂耀庭吴昌杰1吴熙瑞1(深圳市红十字会医院中西医结合研究所,深圳518029;1同济医科大学生殖医学中心,武汉430030)孕三烯酮(gestrinone,R2323)是一种19—去甲基睾丸酮衍生物.80...Radioligand receptor binding assay(RRBA)was used to determine the characteristics of gestrinone binding to estrogen and progestin receptors of the uterine cytosol in rabbits.The results showed that the binding og progesterone and estradiol to uterine cytosols was in a concentration-dependent saturation manner,the dissociation constants (K d) were 0.86 and 0.18nmol·L -1 by the Scatchard analysis. If the affinities of progesterone and estradiol binding to progestin and estrogen receptors were taken to by 100%,the relative binding affinities of gestrinone were 54.87%,0.74%,respectively. The results indicated that gestrinone showed a considerably high affinity with progestin receptor,but had only a very poor affinity with estrogen receptor.

关 键 词:孕三烯酮 雌激素 孕激素 子宫 亲和力 

分 类 号:R977.12[医药卫生—药品]

 

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