H. Manning
Faculty Member
Last active: 3/22/2018

Preclinical imaging evaluation of novel TSPO-PET ligand 2-(5,7-Diethyl-2-(4-(2-[(18)F]fluoroethoxy)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide ([ (18)F]VUIIS1008) in glioma.

Tang D, Nickels ML, Tantawy MN, Buck JR, Manning HC
Mol Imaging Biol. 2014 16 (6): 813-20

PMID: 24845529 · PMCID: PMC4372299 · DOI:10.1007/s11307-014-0743-2

PURPOSE - Translocator protein (TSPO) concentrations are elevated in glioma, suggesting a role for TSPO positron emission tomography (PET) imaging in this setting. In preclinical PET studies, we evaluated a novel, high-affinity TSPO PET ligand, [(18)F]VUIIS1008, in healthy mice and glioma-bearing rats.

PROCEDURES - Dynamic PET data were acquired simultaneously with [(18)F]VUIIS1008 injection, with binding reversibility and specificity evaluated in vivo by non-radioactive ligand displacement or blocking. Compartmental analysis of PET data was performed using metabolite-corrected arterial input functions. Imaging was validated with histology and immunohistochemistry.

RESULTS - [(18)F]VUIIS1008 exhibited rapid uptake in TSPO-rich organs. PET ligand uptake was displaceable with non-radioactive VUIIS1008 or PBR06 in mice. Tumor accumulation of [(18)F]VUIIS1008 was blocked by pretreatment with VUIIS1008 in rats. [(18)F]VUIIS1008 exhibited improved tumor-to-background ratio and higher binding potential in tumors compared to a structurally similar pyrazolopyrimidine TSPO ligand, [(18)F]DPA-714.

CONCLUSIONS - The PET ligand [(18)F]VUIIS1008 exhibits promising characteristics as a tracer for imaging glioma. Further translational studies appear warranted.

MeSH Terms (15)

Animals Brain Neoplasms Carrier Proteins Fluorine Radioisotopes Glioma Ligands Mice Mice, Inbred C57BL Positron-Emission Tomography Pyrazoles Pyrimidines Rats Rats, Wistar Receptors, GABA Receptors, GABA-A

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