Di Carlo F, Conti G, Reboani C
J Endocrinol. 1978 Apr;77(1):49-55. doi: 10.1677/joe.0.0770049.
The inhibitory effect of some gestagens and calusterone on the binding of oestradiol-17beta to its specific uterine receptors has been investigated in intact rats. Progesterone, medrogestone, clogestone, medroxyprogesterone acetate and calusterone reduce the specific oestradiol-receptor interaction in vitro; this effect is dose-dependent and does not differ significantly from one drug to the other. A more relevant decrease in the amount of oestradiol-17beta bound to specific receptors has been observed with calusterone. Progesterone, clogestone, medrogestone, medroxyprogesterone acetate and calusterone given orally induce a marked decrease (between 30 and 70% depending on the dose) in the binding capacity of oestradiol-17beta to specific uterine receptors in vivo. Results from a Scatchard plot analysis suggest that the interference with the binding of oestradiol-17beta caused by both progestogens and calusterone is due to a non-competitive interaction.
在完整大鼠中研究了某些孕激素和卡鲁睾酮对雌二醇-17β与其子宫特异性受体结合的抑制作用。孕酮、甲羟孕酮、氯地孕酮、醋酸甲羟孕酮和卡鲁睾酮在体外可降低雌二醇受体的特异性相互作用；这种作用呈剂量依赖性，且不同药物之间无显著差异。卡鲁睾酮使与特异性受体结合的雌二醇-17β量有更明显的减少。口服给予孕酮、氯地孕酮、甲羟孕酮、醋酸甲羟孕酮和卡鲁睾酮可使体内雌二醇-17β与子宫特异性受体的结合能力显著降低（根据剂量不同，降低幅度在30%至70%之间）。Scatchard图分析结果表明，孕激素和卡鲁睾酮对雌二醇-17β结合的干扰是由于非竞争性相互作用。
