Merriam G R, Pfeiffer D G, Loriaux D L, Lipsett M B
J Steroid Biochem. 1983 Jul;19(1B):619-25. doi: 10.1016/0022-4731(83)90227-3.
The catechol estrogens, the 2- or 4-hydroxylated metabolites of estrone and estradiol, have pharmacologic properties of both estrogens and catecholamines and are formed from estrogens in peripheral tissues and in the brain. This has led to speculation that they may mediate some of the feedback effects of estrogens upon gonadotropins and prolactin (PRL). Studies testing these hypotheses are still few and have not been conclusive. There have been reports that the catechol estrogen 2-hydroxyestrone (2-OHE1) might act as a partial estrogen antagonist, stimulating gonadotropin secretion; and that it might have dopamine-like effects, suppressing the secretion of PRL. In studies testing the chronic and acute effects of catechol estrogens on LH, FSH, and PRL in men and women, we found that they behaved as estrogens, suppressing gonadotropins when given in doses high enough to compensate for their rapid clearance and degradation. We found no evidence that they suppress PRL secretion. The weight of available evidence suggests that these effects are mediated by estrogen receptor interactions; and that the formation of catechol estrogens is not an obligatory step in the feedback effects of estrogens, although it may have a modulatory role. Plasma levels of catechol estrogens are too low for them to exert circulating neuroendocrine effects.
儿茶酚雌激素是雌酮和雌二醇的2-或4-羟基化代谢产物，具有雌激素和儿茶酚胺的药理特性，在外周组织和大脑中由雌激素形成。这引发了一种推测，即它们可能介导雌激素对促性腺激素和催乳素（PRL）的一些反馈作用。检验这些假设的研究仍然很少，而且尚无定论。有报道称，儿茶酚雌激素2-羟基雌酮（2-OHE1）可能作为部分雌激素拮抗剂，刺激促性腺激素分泌；并且它可能具有类似多巴胺的作用，抑制PRL分泌。在检验儿茶酚雌激素对男性和女性LH、FSH和PRL的慢性和急性影响的研究中，我们发现它们表现为雌激素，当给予足够高的剂量以补偿其快速清除和降解时，会抑制促性腺激素。我们没有发现它们抑制PRL分泌的证据。现有证据表明，这些作用是由雌激素受体相互作用介导的；并且儿茶酚雌激素的形成不是雌激素反馈作用的必要步骤，尽管它可能具有调节作用。儿茶酚雌激素的血浆水平过低，无法发挥循环神经内分泌作用。
