REGIONAL DISTRIBUTION OF SEROTONERGIC PRESYNAPTIC AND POSTSYNAPTIC MARKERS IN HUMAN-BRAIN
REGIONAL DISTRIBUTION OF SEROTONERGIC PRESYNAPTIC AND POSTSYNAPTIC MARKERS IN HUMAN-BRAIN
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DOI：
10.1111/j.1600-0447.1989.tb07175.x
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发表时间：
1989-01-01
影响因子：
6.7
通讯作者：
MALOTEAUX, JM
中科院分区：
文献类型：
--
作者：
LARUELLE, M;MALOTEAUX, JM
突触前标志物帕罗西汀是一种新型抗抑郁药，是一种选择性血清素 (5-HT) 摄取阻滞剂。[3Hl-帕罗西汀结合位点已在人血小板 (1) 和大鼠皮质 (2) 中描述，并且与 5-HT 摄取位点密切相关。 13Hl-帕罗西汀是比 [3Hl-丙咪嗪 (3) 更具选择性的 5-HT 摄取位点标记配体。在大鼠大脑中，用 5, 7-二羟基色胺 (5, 7-DHT) 选择性破坏 5-HT 神经末梢导致 5-HT 水平降低 94%，13H1-帕罗西汀结合降低 90% (2)，但 [3H1-丙咪嗪结合仅降低 42% (4)。因此，我们研究了[3H1-帕罗西汀在人脑中的结合特征，以确定其作为特异性5-HT突触前标记物的用途。 突触后标记物 至少有两类不同的5-HT结合位点：5-HT1和5-HT2 (5)。 5-HTI 结合位点由 L3H1-5-HT 标记，但其生理作用仍不清楚。最近的药理学研究区分了 5-HTI 结合位点的三个不同亚群：（5-HTIA、5-HTIB 和 5-HTlc）(6)。 S-HT 结合位点是一个异质组，可能位于突触前和突触后 (7)。例如，与 5-HTIA 位点相关的[3H1-8-羟基-2-NYN-二丙氨基四氢萘 (13H1-8-OHDPAT) 结合位点不受海马中 5, 7-DHT 损伤的影响，但受到纹状体中此类损伤的影响显着减少 (8)。另一方面，由[3H1-ketanserin 标记的5-HT2 结合位点涉及特定的药理作用(9)。它们可能主要位于突触后膜上，因为它们
Presynaptic markers Paroxetine is a new antidepressant which is a selective serotonin (5-HT) uptake blocker.[3Hl-paroxetine binding sites have been described in human platelets (1) and rat cortex (2), and are closely related to the 5-HT uptake sites. 13Hl-paroxetine is a more selective ligand for labelling of 5-HT uptake sites than [3Hl-imipramine (3). In rat brain, selective destruction of 5-HT nerve terminals with 5, 7-dihydroxytryptamine (5, 7-DHT) leads to a 94% reduction in 5-HT levels and a 90% reduction in 13H1-paroxetine binding (2), but to only a 42% reduction in [3Hl-imipramine binding (4). Therefore, we investigated the binding characteristics of [3Hl-paroxetine in human brain to determine its use as a specific 5-HT presynaptic marker.Postsynaptic markers There are at least two distinct classes of 5-HT binding sites: 5-HT1 and 5-HT2 (5). 5-HTI binding sites are labelled by L3H1-5-HT but their physiological role remains unclear. Recent pharmacological studies have differentiated three distinct subpopulations of 5-HTI binding sites:(5-HTIA, 5-HTIB, and 5-HTlc)(6). S-HT, binding sites are a heterogeneous group that are probably located both pre-and postsynaptically (7). For example,[3H1-8-hydroxy-2-NYN-dipropylamino-tetralin (13Hl-8-OHDPAT) binding sites that are related to 5-HTIA sites are unaffected by 5, 7-DHT lesions in the hippocampus, but are markedly decreased by such lesions in the striatum (8). On the other hand, 5-HT2 binding sites, which are labelled by [3Hl-ketanserin are implicated in specific pharmacological actions (9). They are probably localized mainly on postsynaptic membranes since they are