Michel M, Hiemke C, Ghraf R
Brain Res. 1984 May 28;301(1):149-52. doi: 10.1016/0006-8993(84)90413-x.
In a synaptosomal preparation from male rat cerebral cortex only 34% of total norepinephrine (NE) uptake could be inhibited by nanomolar concentrations of desmethylimipramine (DMI) with an apparent IC50 value of 0.37 nM. The residual uptake was efficiently inhibited by micromolar concentrations of DMI (IC50 = 4.0 microM). In synaptosomes from the hypothalamus, 74% of total NE uptake could be blocked by DMI with an IC50 of 0.1 nM whereas in synaptosomes from the striatum the IC50 for DMI inhibition was 3.8 microM. It is concluded that in synaptosomes from rat cerebral cortex only 34%, and in synaptosomes from the hypothalamus 74% of total NE are taken up by noradrenergic nerve terminals whereas the residual NE uptake occurs in dopaminergic nerve endings.
在雄性大鼠大脑皮层的突触体标本中,纳摩尔浓度的去甲丙咪嗪(DMI)仅能抑制总去甲肾上腺素(NE)摄取的34%,其表观半数抑制浓度(IC50)值为0.37 nM。残余摄取则能被微摩尔浓度的DMI有效抑制(IC50 = 4.0 μM)。在下丘脑的突触体中,DMI可阻断74%的总NE摄取,IC50为0.1 nM,而在纹状体的突触体中,DMI抑制的IC50为3.8 μM。得出的结论是,在大鼠大脑皮层的突触体中,仅34%的总NE由去甲肾上腺素能神经末梢摄取,在下丘脑的突触体中这一比例为74%,而残余的NE摄取发生在多巴胺能神经末梢。