Michel M C, Rother A, Hiemke C, Ghraf R
Institut für Physiologische Chemie, Universitätsklinikum Essen, Federal Republic of Germany.
Biochem Pharmacol. 1987 Oct 1;36(19):3175-80. doi: 10.1016/0006-2952(87)90629-0.
High-affinity uptake of dopamine and serotonin into a synaptosomal preparation from rat cerebral cortex was inhibited by a number of estrogen agonists and antagonists in vitro in a stereoselective and competitive manner. The most potent estrogenic inhibitors in the dopaminergic and serotonergic system were ethinylestradiol (KI = 558 nM) and 2-hydroxyethinylestradiol (KI = 226 nM), respectively. Structure-activity relationships are discussed and compared with the effects of estrogens on noradrenaline uptake. However, as all physiologically occurring estrogens inhibited amine uptake only in the micromolar concentration range it seems unlikely that this direct interaction of estrogen with the amine carrier is responsible for the changes in dopamine and serotonin uptake observed during the estrous cycle or after in vivo administration of estrogens and/or progesterone.
在体外，多种雌激素激动剂和拮抗剂以立体选择性和竞争性方式抑制大鼠大脑皮质突触体制剂对多巴胺和5-羟色胺的高亲和力摄取。多巴胺能和5-羟色胺能系统中最有效的雌激素抑制剂分别是乙炔雌二醇（KI = 558 nM）和2-羟基乙炔雌二醇（KI = 226 nM）。讨论了构效关系，并与雌激素对去甲肾上腺素摄取的影响进行了比较。然而，由于所有生理上存在的雌激素仅在微摩尔浓度范围内抑制胺摄取，雌激素与胺载体的这种直接相互作用似乎不太可能是发情周期期间或体内给予雌激素和/或孕酮后观察到的多巴胺和5-羟色胺摄取变化的原因。
