[H-3]-LABELED 2-NITROIMIPRAMINE - A SELECTIVE SLOWLY-DISSOCIATING PROBE OF THE IMIPRAMINE BINDING-SITE (SEROTONIN TRANSPORTER) IN PLATELETS AND BRAIN
[H-3]-LABELED 2-NITROIMIPRAMINE - A SELECTIVE SLOWLY-DISSOCIATING PROBE OF THE IMIPRAMINE BINDING-SITE (SEROTONIN TRANSPORTER) IN PLATELETS AND BRAIN
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DOI：
10.1016/0024-3205(83)90210-2
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发表时间：
1983-01-01
期刊：
影响因子：
6.1
通讯作者：
PAUL, SM
中科院分区：
文献类型：
--
作者：
REHAVI, M;TRACER, H;PAUL, SM
[3H]丙咪嗪（一种抗抑郁药）的高亲和力结合位点与5 -羟色胺的突触前和血小板摄取位点之间存在密切的功能和结构关系。丙咪嗪的几种硝基衍生物，对丙咪嗪结合位点有非常高的亲和力，在0-4度孵育时解离很慢。C合成。描述了[3H]2-硝基丙咪嗪与人血小板和大鼠脑膜结合的特点。本文描述了这种配体在研究丙咪嗪结合位点（血清素转运体）方面的相对效用，因为这种类似物比[3H]丙咪嗪具有更高的亲和力和特异性活性。[3H]2-硝基丙咪嗪由于其极慢的解离速率，应该成为随后表征和纯化血清素摄取或运输部位的有价值的工具。
There is a close functional and structural relationship between the high affinity binding site for [3H]imipramine [an antidepressant] and the presynaptic and platelet uptake site(s) for serotonin. Several nitro derivatives of imipramine which have a very high affinity for the imipramine binding site and which dissociate very slowly when incubations are performed at 0-4.degree. C were synthesized. The characteristics of [3H]2-nitroimipramine binding to human platelet and rat brain membranes are described. The relative utility of this ligand for studying the impramine binding site (serotonin transporter) is described since this analog has both a higher affinity and specific activity than [3H]imipramine. [3H]2-Nitroimipramine by virtue of its extremely slow dissociation rate should be a valuable tool in subsequent characterization and purification of the serotonin uptake or transport site.