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.
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 rat...
| Publicado en: | Molecular Imaging & Biology Vol. 16; no. 6; pp. 813 - 821 |
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| Autores principales: | , , , , |
| Formato: | research Journal Article |
| Publicado: |
Springer Nature
Dec2014
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=109764622&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 109764622 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 15361632 KJU jtl: Molecular Imaging & Biology issn: 15361632 maglogo: N pubinfo: dt: Dec2014 vid: 16 iid: 6 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 109764622 109764622 NLM24845529 2012799695 10.1007/s11307-014-0743-2 NLM24845529 PMC4372299 109764622 ppf: 813 ppct: 8 formats: fmt: @attributes: type: P tig: atl: 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. aug: au: Tang, Dewei Nickels, Michael L Tantawy, M Noor Buck, Jason R Manning, H Charles sug: subj: Brain Neoplasms Metabolism Carrier Proteins Metabolism Fluorine Radioisotopes Diagnostic Use Glioma Metabolism Heterocyclic Compounds Diagnostic Use Receptors, Cell Surface Metabolism Tomography, Emission-Computed Methods Animal Studies Brain Neoplasms Pathology Brain Neoplasms Radiography Fluorine Radioisotopes Pharmacokinetics Glioma Pathology Glioma Radiography Heterocyclic Compounds Pharmacokinetics Ligands Mice Rats ab: 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. pubtype: Academic Journal doctype: research Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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