Hinz Rainer, Selvaraj Sudhakar, Murthy N Venkatesha, Bhagwagar Zubin, Taylor Matthew, Cowen Philip J, Grasby Paul M
Wolfson Molecular Imaging Centre, University of Manchester, Manchester, UK.
J Cereb Blood Flow Metab. 2008 Aug;28(8):1478-90. doi: 10.1038/jcbfm.2008.41. Epub 2008 May 14.
The positron emission tomography (PET) ligand [(11)C]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 10 mg citalopram, a selective serotonin reuptake inhibitor (SSRI), before the PET scan on the kinetics of [(11)C]DASB in arterial plasma and in selected brain regions. Four healthy male volunteers underwent two PET scans with a mean of 523 MBq 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 metabolite-corrected arterial plasma input function. Total volumes of distribution V(T) 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 V(T) 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 BP(ND) and 69% derived from BP(P).
正电子发射断层扫描（PET）配体[(11)C]DASB是目前用于人脑5-羟色胺转运体（SERT）定量研究的应用最为广泛的显像剂。本研究旨在评估PET扫描前静脉注射10 mg西酞普兰（一种选择性5-羟色胺再摄取抑制剂（SSRI））对[(11)C]DASB在动脉血浆及选定脑区动力学的影响。4名健康男性志愿者按随机设计在接受安慰剂或西酞普兰输注后进行了两次PET扫描，平均注入活度为523 MBq。西酞普兰输注导致代谢物校正动脉血浆输入函数曲线下面积大幅增加。应用Logan图对区域时间-活度曲线进行分析，或通过频谱分析生成参数图来估算分布总体积V(T)。西酞普兰输注后，经Logan分析小脑V(T)平均降低19%，经频谱分析降低24%，这证实了先前关于小脑灰质中可置换SERT配体结合的研究结果。6个具有中度至高结合的靶区的SERT占有率，由BP(ND)得出为60%，由BP(P)得出为69%。
