Knuppen R, Ball P, Emons G
J Steroid Biochem. 1986 Jan;24(1):193-8. doi: 10.1016/0022-4731(86)90050-6.
Estrogens substituted in the ortho-position of the phenolic hydroxy-group with an additional hydroxy- or methoxy-group are quantitatively important estrogen metabolites; first isolated and identified from the urine of man and rodents have been demonstrated in blood and different organs, e.g. the pituitary and hypothalamus. The physiological importance of the preeminent representatives of this group, the 2- and 4-hydroxyestrogens, the so-called catecholestrogens, is still equivocal. For example, numerous in vivo investigations in rodents have demonstrated that gonadotrophin secretion is influenced by these catecholestrogens. However, depending on the position of the A-ring substituent, major potency differences have been observed. The significant discrepancies between the quantitative and qualitative effects of catecholestrogens in in vitro and in vivo experiments have been presented and explained on the basis of different receptor affinities and the pharmacokinetics of catecholestrogens. An array of A-ring-substituted steroid model substances has been tested with respect to the effects of 2- and/or 4-substitution on stimulation or blockade of the estrogenic potency.
在酚羟基的邻位被额外的羟基或甲氧基取代的雌激素是重要的雌激素代谢产物；首次从人和啮齿动物尿液中分离并鉴定出来，已在血液和不同器官（如垂体和下丘脑）中得到证实。该类主要代表物2-和4-羟基雌激素，即所谓的儿茶酚雌激素的生理重要性仍不明确。例如，在啮齿动物中进行的大量体内研究表明，这些儿茶酚雌激素会影响促性腺激素的分泌。然而，根据A环取代基的位置，已观察到显著的效价差异。基于不同的受体亲和力和儿茶酚雌激素的药代动力学，已阐述并解释了儿茶酚雌激素在体外和体内实验中定量和定性效应之间的显著差异。一系列A环取代的甾体模型物质已就2-和/或4-取代对雌激素效价的刺激或阻断作用进行了测试。
