REGIONAL AND SUBCELLULAR-LOCALIZATION IN HUMAN-BRAIN OF [H-3] PAROXETINE BINDING, A MARKER OF SEROTONIN UPTAKE SITES
REGIONAL AND SUBCELLULAR-LOCALIZATION IN HUMAN-BRAIN OF [H-3] PAROXETINE BINDING, A MARKER OF SEROTONIN UPTAKE SITES
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DOI：
10.1016/0006-3223(88)90198-9
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发表时间：
1988-07-01
影响因子：
10.6
通讯作者：
MALOTEAUX, JM
中科院分区：
文献类型：
--
作者：
LARUELLE, M;VANISBERG, MA;MALOTEAUX, JM
研究了选择性5-羟色胺（5-HT）摄取阻滞剂[3H]帕罗西汀在人脑中的结合特性。Kd值为0.23 +-。0.07 nM， Bmax值为190 +-。壳核蛋白39 fmol/mg。各种抗抑郁药物抑制人脑[3H]帕罗西汀特异性结合的能力与其抑制大鼠脑[3H]5-HT摄取的能力密切相关。[3H]帕罗西汀特异性结合位点在黑质、下丘脑和海马中浓度最高。基底节区和丘脑的数值较低。特异性结合在大脑和小脑皮层非常低。[3H]帕罗西汀结合位点的区域分布与[3H]酮色胺结合S2 5 -羟色胺受体的区域分布不同。通过差速离心获得的[3H]帕罗西汀特异性结合位点的亚细胞分布显示，突触体富集于额叶皮层和纹状体，而微粒体部分富集于纹状体。结果表明[3H]帕罗西汀是标记人脑5-羟色胺摄取分子复合物的首选配体。
The characteristics of the binding of [3H]paroxetine, a selective serotonin (5-HT) uptake blocker, were investigated in human brain. The Kd value was 0.23 .+-. 0.07 nM, and the Bmax value was 190 .+-. 39 fmol/mg protein in the putamen. The capacity of various antidepressive drugs to inhibit [3H]paroxetine-specific binding in human brain was well correlated with their capacity to inhibit [3H]5-HT uptake in rat brain. The highest concentrations of [3H]paroxetine-specific binding sites were found in the substantia nigra, hypothalamus, and hippocampus. Lower values were obtained in the basal ganglia and the thalamus. The specific binding was very low in cerebral and cerebellar cortices. The regional distribution of [3H]paroxetine binding sites differs from that of [3H]ketanserin binding to S2 serotonin receptors. The subcellular distribution of the [3H]paroxetine-specific binding sites obtained by differential centrifugation revealed a synaptosomal enrichment in the frontal cortex and striatum, whereas an enrichment in the microsomal fraction was found in striatum. The results show that [3H]paroxetine is a ligand of choice to label the 5-HT uptake molecular complex in human brain.