High-affinity binding of [H-3]paroxetine to caudate nucleus and microvessels from porcine brain

被引:7
作者
Brust, P
Bergmann, R
Johannsen, B
机构
[1] Research Center Rossendorf, Inst. Bioinorganic R., 01314 Dresden
关键词
blood-brain barrier; caudate nucleus; citalopram; clomipramine; desipramine; fluoxetine; imipramine; paroxetine binding; pig; serotonin transport;
D O I
10.1097/00001756-199605310-00016
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
SEROTONIN (5-HT) is an important signal molecule not only for neurones but also for a variety of other cell types. Targeting the brain endothelium, the constitutive element of the blood-brain barrier (BBB), it elicits permeability changes. Using the selective 5-HT uptake inhibitor [H-3]paroxetine we demonstrated the presence of a 5-HT transporter-like protein at the BBB. The binding capacities (B-max) at the BBB (382 fmol mg(-1)) and on caudate nucleus membranes (392 fmol mg(-1)) were similar. However, the binding affinities differed by a factor of 5 (membranes: K-d = 0.10 nM, BBB: 0.47 nM). The affinities of various specific uptake inhibitors were also 2- to 13-fold lower in the microvessel preparation. It is suggested that the 5-HT transporter(s) in the brain and microvessels are different or differently regulated proteins.
引用
收藏
页码:1405 / 1408
页数:4
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