Ghanadian R, Smith C B, Williams G, Chisholm G D
Br J Urol. 1977;49(7):695-700. doi: 10.1111/j.1464-410x.1977.tb04555.x.
The effects of 4 antiandrogens and stilboestrol on the cytosol receptor of the rat ventral prostate have been compared. Equimolar doses of cyproterone acetate, chlormadinone acetate, SC 9022 and flutamide inhibited the binding of dihydrotestosterone to the receptor complex in vivo by 44 to 50% whereas stilboestrol had no effect. In the in vitro studies an equimolar concentration produced similar effects to those observed in vivo with the exception of flutamide which had no effect. This technique provides a method for assessing and comparing the effectiveness of antiandrogens on the androgen receptor complex of the prostate.
比较了4种抗雄激素药物和己烯雌酚对大鼠腹侧前列腺胞质受体的影响。等摩尔剂量的醋酸环丙孕酮、醋酸氯地孕酮、SC 9022和氟他胺在体内可使二氢睾酮与受体复合物的结合抑制44%至50%,而己烯雌酚则无此作用。在体外研究中,除氟他胺无作用外,等摩尔浓度产生的作用与体内观察到的相似。该技术为评估和比较抗雄激素药物对前列腺雄激素受体复合物的有效性提供了一种方法。