Köster G, Breuer H, Schneider H T
Acta Endocrinol (Copenh). 1982 Jan;99(1):1-8. doi: 10.1530/acta.0.0990001.
The effects of oestradiol-17 beta, 2-hydroxyoestradiol-17 beta and 2-methoxyoestradiol-17 beta on the metabolism of [3H]noradrenaline were studied in various brain regions of ovariectomized in rats in vivo. Under the experimental conditions chosen, oestradiol-17 beta had no effect on the metabolic pattern of noradrenaline. After pre-treatment of ovariectomized rats with 2-hydroxyoestradiol-17 beta, the formation of methylate metabolites of noradrenaline (normetanephrine and 3-methoxy-4-hydroxyphenylglycol sulphate) was reduced, whereas that of non-methylated products (3,4-dihydroxymandelic acid and 3,4-dihydroxyphenylglycol sulphate) was increased. The inhibition of methylation was most pronounced in posterior hypothalamus and less significant in anterior hypothalamus and thalamus. Pre-treatment with 2-methoxyoestradiol-17 beta yielded inconsistent results. From the findings described here it may be concluded that 2-hydroxyoestradiol-17 beta, as previously shown in vitro, also affects the metabolism of noradrenaline in vivo by directly interacting with the catechol-O-methyltransferase. It is suggested that this metabolic effect may be responsible - at least to some extent - for the inhibitory effect of 2-hydroxyoestradiol-17 beta on LH secretion.
在体内对去卵巢大鼠的不同脑区研究了17β-雌二醇、2-羟基-17β-雌二醇和2-甲氧基-17β-雌二醇对[3H]去甲肾上腺素代谢的影响。在所选择的实验条件下，17β-雌二醇对去甲肾上腺素的代谢模式没有影响。用2-羟基-17β-雌二醇对去卵巢大鼠进行预处理后，去甲肾上腺素的甲基化代谢产物（去甲变肾上腺素和3-甲氧基-4-羟基苯乙二醇硫酸盐）的生成减少，而非甲基化产物（3,4-二羟基扁桃酸和3,4-二羟基苯乙二醇硫酸盐）的生成增加。甲基化的抑制在下丘脑后部最为明显，而在下丘脑前部和丘脑则不太显著。用2-甲氧基-17β-雌二醇进行预处理产生了不一致的结果。从这里描述的研究结果可以得出结论，如先前在体外所显示的，2-羟基-17β-雌二醇在体内也通过与儿茶酚-O-甲基转移酶直接相互作用来影响去甲肾上腺素的代谢。有人提出，这种代谢作用可能至少在一定程度上是2-羟基-17β-雌二醇对促黄体生成素分泌产生抑制作用的原因。
