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首页> 外文期刊>Biochemistry >HETEROGENEITY OF ANTIDEPRESSANT BINDING SITES ON THE RECOMBINANT RAT SEROTONIN TRANSPORTER SERT1
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HETEROGENEITY OF ANTIDEPRESSANT BINDING SITES ON THE RECOMBINANT RAT SEROTONIN TRANSPORTER SERT1

机译：重组大鼠血清素转运蛋白SERT1上抗氧化剂结合位点的异质性

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摘要

Antidepressant drugs block the uptake of serotonin into serotonergic nerve terminals and blood platelets. Here, binding of the tricyclic antidepressant [H-3]imipramine to the recombinant rat serotonin transporter SERT1 expressed in human embryonic kidney cells was found to be nonhomogeneous. Scatchard analysis and competition experiments revealed the existence of two distinct antidepressant binding sites. At site 1, [H-3]imipramine binding was strictly sodium-dependent with an apparent K-D of similar to 10 nM. In contrast, [H-3]imipramine binding to site 2 occurred also in the absence of sodium and exhibited a lower affinity. Binding of the nontricyclic antidepressant [3H]citalopram was observed only at site 2. The natural substrate of this carrier, serotonin, competitively inhibited antidepressant binding at both sites; however, its affinity to site 2 was similar to 5-fold lower. These data provide a molecular explanation for the distinct pharmacological actions of different antidepressants.
机译：抗抑郁药会阻止5-羟色胺摄取到5-羟色胺能神经末梢和血小板中。在这里，发现三环抗抑郁药[H-3]丙咪嗪与在人胚胎肾细胞中表达的重组大鼠血清素转运蛋白SERT1的结合是不均匀的。斯卡查德分析和竞争实验表明存在两个不同的抗抑郁药结合位点。在位点1，[H-3]丙咪嗪的结合严格地依赖于钠，其表观K-D约为10 nM。相反，在没有钠的情况下也发生[H-3]丙咪嗪与位点2的结合，并且显示出较低的亲和力。仅在第2位观察到非三环抗抑郁药[3H]西酞普兰的结合。5-羟色胺这种载体的天然底物在两个位点均竞争性抑制了抗抑郁药的结合。但是，它对位点2的亲和力低了5倍。这些数据为不同抗抑郁药的独特药理作用提供了分子解释。

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