Journal
MOLECULAR IMAGING AND BIOLOGY
Volume 21, Issue 1, Pages 113-121Publisher
SPRINGER
DOI: 10.1007/s11307-018-1198-7
Keywords
TSPO; PET; Molecular imaging; Glioma; VUIIS1018A; DPA-714; Cancer imaging
Funding
- National Institutes of Health [K25 CA127349, P50 CA128323, S10 RR17858, U24 CA126588, 1R01 CA163806]
- National Natural Science Foundation of China [81601536]
- Kleberg Foundation
- Lustgarten Foundation
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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.
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