Effects of citalopram infusion on the serotonin transporter binding of [11C] DASB in healthy controls

Effects of citalopram infusion on the serotonin transporter binding of [11C] DASB in healthy controls
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DOI:
10.1038/jcbfm.2008.41
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发表时间:
2008-08-01
影响因子:
6.3
通讯作者:
Grasby, Paul M.
Grasby, Paul M.
中科院分区:
医学1区
文献类型:
--
作者:
Hinz, Rainer;Selvaraj, Sudhakar;Grasby, Paul M.

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正电子发射断层扫描 (PET) 配体 [C-11] DASB 是目前用于人脑血清素转运蛋白 (SERT) 定量研究的最广泛使用的成像剂。这项工作的目的是评估 PET 扫描前静脉输注 10 毫克西酞普兰(一种选择性血清素再摄取抑制剂 (SSRI))对动脉血浆和选定脑区域中 [C-11] DASB 动力学的影响。在随机设计中,四名健康男性志愿者在注射安慰剂或西酞普兰后接受了两次 PET 扫描,平均注射活性为 523MBq。西酞普兰输注导致代谢物校正的动脉血浆输入函数曲线下面积显着增加。将洛根图应用于区域时间-活动曲线或通过频谱分析生成参数图来估计分布VT 的总体积。输注西酞普兰后,Logan 分析观察到小脑 VT 平均降低 19%,光谱分析平均降低 24%,这证实了之前关于小脑灰质中可置换 SERT 配体结合的发现。具有中度至高度结合的六个目标区域的 SERT 占用率为 60% 来自 BPND,69% 来自 BPP。
The positron emission tomography ( PET) ligand [C-11] DASB is currently the most widely used imaging agent for quantitative studies of the serotonin transporter ( SERT) in human brain. The aim of this work was to assess the effects of an intravenous infusion of 10mg citalopram, a selective serotonin reuptake inhibitor ( SSRI), before the PET scan on the kinetics of [C-11] DASB in arterial plasma and in selected brain regions. Four healthy male volunteers underwent two PET scans with a mean of 523MBq injected activity after either placebo or citalopram infusion in a randomised design. The citalopram infusion led to a substantial increase of the area under the curve of the metabolitecorrected arterial plasma input function. Total volumes of distribution VT were estimated applying the Logan plot to regional time - activity curves or by generating parametric maps with spectral analysis. A mean reduction of the cerebellar VT of 19% with Logan analysis and of 24% with spectral analysis was observed after citalopram infusion, which confirms previous findings of displaceable SERT ligand binding in cerebellar grey matter. The SERT occupancy for six target regions with moderate to high binding was 60% derived from BPND and 69% derived from BPP.