Routledge C, Marsden C A
J Neurochem. 1987 Sep;49(3):821-7. doi: 10.1111/j.1471-4159.1987.tb00967.x.
The uptake of [3H]adrenaline and [3H]noradrenaline into rat hypothalamic slices was compared for determination of whether adrenaline uptake was independent of uptake into noradrenergic neurones. Kinetic analysis revealed a similar high-affinity uptake process for both adrenaline and noradrenaline, with Km and Vmax values within similar ranges. These uptakes were inhibited by desipramine and maprotiline in a dose-dependent manner, but the selective dopamine and 5-hydroxytryptamine uptake inhibitors benztropine and fluoxetine, respectively, were without effect. Competition for uptake sites by unlabelled adrenaline with [3H]adrenaline and [3H]-noradrenaline and by unlabelled noradrenaline with [3H]-adrenaline and [3H]noradrenaline was very similar. Lesioning of the major adrenaline-containing cell group (C1 cell group) decreased the hypothalamic adrenaline concentration but had no effect on hypothalamic [3H]adrenaline or [3H]noradrenaline uptake. The results suggest that exogenous adrenaline is largely taken up by high-affinity sites on noradrenergic nerve terminals.
比较了[3H]肾上腺素和[3H]去甲肾上腺素对大鼠下丘脑切片的摄取情况,以确定肾上腺素的摄取是否独立于去甲肾上腺素能神经元的摄取。动力学分析显示,肾上腺素和去甲肾上腺素的摄取过程具有相似的高亲和力,Km和Vmax值在相似范围内。这些摄取被地昔帕明和马普替林以剂量依赖性方式抑制,但选择性多巴胺和5-羟色胺摄取抑制剂苯海索和氟西汀分别无作用。未标记的肾上腺素与[3H]肾上腺素和[3H]去甲肾上腺素以及未标记的去甲肾上腺素与[3H]肾上腺素和[3H]去甲肾上腺素对摄取位点的竞争非常相似。主要含肾上腺素细胞群(C1细胞群)的损伤降低了下丘脑肾上腺素浓度,但对下丘脑[3H]肾上腺素或[3H]去甲肾上腺素的摄取没有影响。结果表明,外源性肾上腺素主要被去甲肾上腺素能神经末梢上的高亲和力位点摄取。