新型18f标记的基于恶二唑的β-淀粉样蛋白正电子发射断层示踪剂的合成和评价。

IF 2.5 3区医学 Q2 BIOLOGY

Radiation research Pub Date : 2025-03-24 DOI:10.1667/RADE-25-00035.1

Zhongyuan Qi, Wantong Guo, Mengchao Cui, Jie Lu

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引用次数: 0

摘要

本研究详细介绍了用于阿尔茨海默病（AD）中β-淀粉样蛋白（Aβ）可视化的新型恶二唑基化合物的合成、结构-活性评价和分析。这些衍生物在体外表现出与Aβ聚集体的结合亲和力。[18F]标记的化合物[18F]4-（5-（4-氟苯基）-1,3,4-恶二唑-2-基）- n， n -二甲基苯胺（化合物[18F] 3）和[18F]4-（5-（4-氟苯基）-1,3,4-恶二唑-2-基）- n -甲基苯胺（化合物[18F]4）有效地标记了阿尔茨海默病患者和APP/PS1小鼠脑组织中的Aβ斑块。在健康小鼠的动态正电子发射断层扫描（PET）研究中，这些化合物显示出良好的脑吸收和清除。化合物[18F] 3和[18F] 4的额外结构改变可能导致更有效的PET示踪剂的发展，以精确显示Aβ斑块。

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Synthesis and Evaluation of Novel 18F-labeled Oxadiazole-based Positron Emission Tomography Tracers for β-Amyloid.

This research details the synthesis, structure-activity evaluation, and analysis of novel oxadiazole-based compounds for visualizing β-amyloid (Aβ) in Alzheimer's disease (AD). The derivatives exhibited binding affinities to Aβ aggregates in vitro. The [18F]-labeled compounds, [18F]4-(5-(4-Fluorophenyl)-1,3,4-oxadiazol-2-yl)-N, N-dimethylaniline (compound [18F] 3) and [18F] 4-(5-(4-Fluorophenyl)-1,3,4-oxadiazol-2-yl)-N-methylaniline (compound [18F]4), effectively labeled Aβ plaques in brain sections from Alzheimer's disease patients and APP/PS1 mice. In dynamic positron emission tomography (PET) studies on healthy mice, these compounds demonstrated favorable brain uptake followed by clearance. Additional structural alterations to compounds [18F] 3 and [18F] 4 may lead to the development of more efficient PET tracers for precise visualization of Aβ plaques.

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来源期刊

Radiation research 医学-核医学

CiteScore

5.10

自引率

8.80%

发文量

179

审稿时长

1 months

期刊介绍： Radiation Research publishes original articles dealing with radiation effects and related subjects in the areas of physics, chemistry, biology and medicine, including epidemiology and translational research. The term radiation is used in its broadest sense and includes specifically ionizing radiation and ultraviolet, visible and infrared light as well as microwaves, ultrasound and heat. Effects may be physical, chemical or biological. Related subjects include (but are not limited to) dosimetry methods and instrumentation, isotope techniques and studies with chemical agents contributing to the understanding of radiation effects.