Norepinephrine neuronal uptake binding sites in rat brain membranes labeled with [3H]desipramine.
Norepinephrine neuronal uptake binding sites in rat brain membranes labeled with [3H]desipramine.
复制标题
大鼠脑膜中去甲肾上腺素神经元摄取结合位点用[3H]地昔帕明标记。
DOI：
10.1073/pnas.78.8.5250
复制
发表时间：
1981
影响因子：
11.1
通讯作者：
Snyder,SH
中科院分区：
文献类型：
--
作者：
Lee,CM;Snyder,SH
去甲肾上腺素神经元中的神经元摄取识别位点已用抗抑郁药[3H]地昔帕明标记。 [3H]地昔帕明与大鼠大脑皮层膜结合的高亲和力成分被 6-羟基多巴胺损伤选择性地消除，从而破坏中枢儿茶酚胺神经元。高亲和力的[3H]地昔帕明结合对地昔帕明具有纳摩尔亲和力常数，并被三环类抗抑郁药抑制，其效力与其抑制神经元摄取去甲肾上腺素的能力相关。 [3H]地昔帕明与摄取位点的结合受到钠的显着刺激，而钾、锂和胆碱的效果则要差得多。在简单的结合研究中监测去甲肾上腺素神经元摄取“受体”的能力应该允许对药物对去甲肾上腺素识别位点和易位机制的影响进行差异分析。钠对[3H]地昔帕明结合的调节可能有助于阐明钠如何影响神经递质的摄取。
Neuronal uptake recognition sites in norepinephrine neurons have been labeled with the antidepressant [3H]desipramine. A high-affinity component of [3H]desipramine binding to rat cerebral cortex membranes is abolished selectively by 6-hydroxydopamine lesions, which destroy central catecholamine neurons. The high-affinity [3H]desipramine binding has a nanomolar affinity constant for desipramine and is inhibited by tricyclic antidepressants with potencies that correlate with their ability to inhibit the neuronal uptake of norepinephrine. [3H]Desipramine binding to the uptake sites is markedly stimulated by sodium, with potassium, lithium, and choline being much less effective. The ability to monitor norepinephrine neuronal uptake "receptors" in simple binding studies should permit a differential analysis of drug influences on the norepinephrine recognition site and the translocation mechanism. The regulation of [3H]desipramine binding by sodium may help clarify how sodium influences neurotransmitter uptake.