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Preclinical Evaluation of a Novel TSPO PET Ligand 2-(7-Butyl-2-(4-(2-[F-18]Fluoroethoxy)phenyl)-5-Methylpyrazolo[1,5-a]Pyr imidin-3-yl)-N,N-Diethylacetamide (F-18-VUIIS1018A) to Image Glioma 期刊论文

编号：

343e8237-5102-44e7-9fb4-bfba5e5bb3df
作者：

Tang, Dewei#^[1,2]Li, Jun^[3,4,5];Nickels, Michael L.^[3,4,5];Huang, Gang(黄钢)^[1,2]Cohen, Allison S.^[3,4];Manning, H. Charles*^{[3,4,5,6,7,8,9]}
语种：

英文
期刊：

MOLECULAR IMAGING AND BIOLOGY ISSN：1536-1632 2019 年 21 卷 1 期 (113 - 121) ; FEB
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关键词：

TSPO PET Molecular imaging Glioma VUIIS1018A DPA-714 Cancer imaging
摘要：

PurposeThere is an urgent need for the development of novel positron emission tomography (PET) tracers for glioma imaging. In this study, we developed a novel PET probe ([F-18]VUIIS1018A) by targeting translocator protein (TSPO), an imaging biomarker for glioma. The purpose of this preclinical study was to evaluate this novel TSPO probe for glioma imaging.ProceduresIn this study, we synthesized [F-19]VUIIS1018A and the precursor for radiosynthesis of [F-18]VUIIS1018A. TSPO binding affinity was confirmed using a radioligand competitive binding assay in C6 glioma cell lysate. Further, dynamic imaging studies were performed in rats using a microPET system. These studies include displacement and blocking studies for ligand reversibility and specificity evaluation, and compartment modeling of PET data for pharmacokinetic parameter measurement using metabolite-corrected arterial input functions and PMOD.ResultsCompared to previously reported TSPO tracers including [F-18]VUIIS1008 and [F-18]DPA-714, the novel tracer [F-18]VUIIS1018A demonstrated higher binding affinity and BPND. Pretreatment with the cold analog [F-19]VUIIS1018A could partially block tumor accumulation of this novel tracer. Further, compartment modeling of this novel tracer also exhibited a greater tumor-to-background ratio, a higher tumor binding potential and a lower brain binding potential when compared with other TSPO probes, such as [F-18]DPA-714 and [F-18]VUIIS1008.ConclusionsThese studies illustrate that [F-18]VUIIS1018A can serve as a promising TSPO PET tracer for glioma imaging and potentially imaging of other solid tumors.
推荐引用方式
GB/T 7714：

Tang Dewei,Li Jun,Nickels Michael L., et al. Preclinical Evaluation of a Novel TSPO PET Ligand 2-(7-Butyl-2-(4-(2-[F-18]Fluoroethoxy)phenyl)-5-Methylpyrazolo[1,5-a]Pyr imidin-3-yl)-N,N-Diethylacetamide (F-18-VUIIS1018A) to Image Glioma [J].MOLECULAR IMAGING AND BIOLOGY,2019,21(1):113-121.
APA：

Tang Dewei,Li Jun,Nickels Michael L.,Huang Gang,&Manning H. Charles.(2019).Preclinical Evaluation of a Novel TSPO PET Ligand 2-(7-Butyl-2-(4-(2-[F-18]Fluoroethoxy)phenyl)-5-Methylpyrazolo[1,5-a]Pyr imidin-3-yl)-N,N-Diethylacetamide (F-18-VUIIS1018A) to Image Glioma .MOLECULAR IMAGING AND BIOLOGY,21(1):113-121.
MLA：

Tang Dewei, et al. "Preclinical Evaluation of a Novel TSPO PET Ligand 2-(7-Butyl-2-(4-(2-[F-18]Fluoroethoxy)phenyl)-5-Methylpyrazolo[1,5-a]Pyr imidin-3-yl)-N,N-Diethylacetamide (F-18-VUIIS1018A) to Image Glioma" .MOLECULAR IMAGING AND BIOLOGY 21,1(2019):113-121.
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