Okatani Y
Nihon Sanka Fujinka Gakkai Zasshi. 1986 Feb;38(2):151-60.
Administration of 100 micrograms 2-hydroxyestrone (2-OHE1) on the morning of proestrus to 4 day cycling rats resulted in suppression of the preovulatory LH surge. The greatest response was observed when the injection of 2-OHE1 coincided with plasma estradiol levels that were close to but not at their maximal proestrus levels. Injection of 100 micrograms 2-hydroxyestradiol-17 beta (2-OHE2-17 beta) effectively inhibited the LH surge when given at 0800 or 0900h, but not when injected at 1000 or 1200h. Non estrogenic 2-hydroxyestradiol-17 alpha was effective in suppressing the LH surge when given at 0900 or 1000h. Neither 2-OHE1 nor 2-OHE2-17 beta interfered with LH secretion in response to LH-RH administration, indicating that the inhibitory action of the catecholestrogen is exercised at the hypothalamic level. However, 2-OHE1 given five times following the implantation of an estradiol capsule in ovariectomized rats had no effect on the LH surge elicited on the second day. These data indicate that catecholestrogen interferes with the brief neuronal triggering phase necessary for LH-RH release, but not the sensitization phase of positive feedback of estrogen on phasic LH secretion. The evidence also indicates that the action does not involve conventional competition for the estradiol receptor.
在动情前期早晨给4日龄的周期大鼠注射100微克2-羟基雌酮(2-OHE1)会抑制排卵前促黄体生成素(LH)峰。当2-OHE1注射时间与血浆雌二醇水平接近但未达到动情前期最高水平时,观察到最大反应。当在0800或0900时给予100微克2-羟基雌二醇-17β(2-OHE2-17β)时可有效抑制LH峰,但在1000或1200时注射则无效。非雌激素性的2-羟基雌二醇-17α在0900或1000时给予时可有效抑制LH峰。2-OHE1和2-OHE2-17β均不干扰对促性腺激素释放激素(LH-RH)给药的LH分泌反应,表明儿茶酚雌激素的抑制作用在下丘脑水平发挥。然而,在去卵巢大鼠植入雌二醇胶囊后给予5次2-OHE1对第二天引发的LH峰没有影响。这些数据表明,儿茶酚雌激素干扰LH-RH释放所需的短暂神经元触发阶段,但不干扰雌激素对阶段性LH分泌的正反馈致敏阶段。证据还表明,该作用不涉及对雌二醇受体的传统竞争。