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Molecules, Vol. 23, Pages 1375: [18F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model

Molecules, Vol. 23, Pages 1375: [18F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model

Molecules doi: 10.3390/molecules23061375

Authors: Nicolas Vignal Salvatore Cisternino Nathalie Rizzo-Padoin Carine San Fortune Hontonnou Thibaut Gelé Xavier Declèves Laure Sarda-Mantel Benoît Hosten

[18F]FEPPA is a specific ligand for the translocator protein of 18 kDa (TSPO) used as a positron emission tomography (PET) biomarker for glial activation and neuroinflammation. [18F]FEPPA radiosynthesis was optimized to assess in a mouse model the cerebral inflammation induced by an intraperitoneal injection of Salmonella enterica serovar Typhimurium lipopolysaccharides (LPS; 5 mg/kg) 24 h before PET imaging. [18F]FEPPA was synthesized by nucleophilic substitution (90 °C, 10 min) with tosylated precursor, followed by improved semi-preparative HPLC purification (retention time 14 min). [18F]FEPPA radiosynthesis were carried out in 55 min (from EOB). The non-decay corrected radiochemical yield were 34 ± 2% (n = 17), and the radiochemical purity greater than 99%, with a molar activity of 198 ± 125 GBq/µmol at the end of synthesis. Western blot analysis demonstrated a 2.2-fold increase in TSPO brain expression in the LPS treated mice compared to controls. This was consistent with the significant increase of [18F]FEPPA brain total volume of distribution (VT) estimated with pharmacokinetic modelling. In conclusion, [18F]FEPPA radiosynthesis was implemented with high yields. The new purification/formulation with only class 3 solvents is more suitable for in vivo studies.

Authors:   Vignal, Nicolas ; Cisternino, Salvatore ; Rizzo-Padoin, Nathalie ; San, Carine ; Hontonnou, Fortune ; Gelé, Thibaut ; Declèves, Xavier ; Sarda-Mantel, Laure ; Hosten, Benoît
Journal:   Molecules
Volume:   23
edition:   6
Year:   2018
Pages:   1375
DOI:   10.3390/molecules23061375
Publication date:   07-Jun-2018
Facts, background information, dossiers
  • Radiosynthesis
  • brain
  • molecules
  • Nucleophilic Substitution
  • neuroinflammation
  • inflammation
  • imaging
  • biomarker
More about Molecular Diversity Preservation International
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