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Article

[18F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model

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Assistance Publique—Hôpitaux de Paris, Hôpital Saint-Louis, Unité Claude Kellershohn, 75010 Paris, France
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Inserm UMR-S 1144, Faculté de Pharmacie de Paris, Université Paris Descartes, 75006 Paris, France
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Assistance Publique—Hôpitaux de Paris, Hôpital Universitaire Necker—Enfants Malades, 75015 Paris, France
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Institut Universitaire d’Hématologie, Université Paris Diderot, 75013 Paris, France
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Assistance Publique—Hôpitaux de Paris, Hôpital Cochin, 75014 Paris, France
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Assistance Publique—Hôpitaux de Paris, Hôpital Lariboisière, Médecine Nucléaire, 75010 Paris, France
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Inserm UMR-S 942, Université Paris Diderot, 75013 Paris, France
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(6), 1375; https://doi.org/10.3390/molecules23061375
Received: 24 April 2018 / Revised: 25 May 2018 / Accepted: 4 June 2018 / Published: 7 June 2018
(This article belongs to the Special Issue Current Aspects of Radiopharmaceutical Chemistry)
[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. View Full-Text
Keywords: [18F]FEPPA; TSPO; brain inflammation; small-animal PET imaging; radiolabeling; radiotracer metabolism [18F]FEPPA; TSPO; brain inflammation; small-animal PET imaging; radiolabeling; radiotracer metabolism
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MDPI and ACS Style

Vignal, N.; Cisternino, S.; Rizzo-Padoin, N.; San, C.; Hontonnou, F.; Gelé, T.; Declèves, X.; Sarda-Mantel, L.; Hosten, B. [18F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model. Molecules 2018, 23, 1375. https://doi.org/10.3390/molecules23061375

AMA Style

Vignal N, Cisternino S, Rizzo-Padoin N, San C, Hontonnou F, Gelé T, Declèves X, Sarda-Mantel L, Hosten B. [18F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model. Molecules. 2018; 23(6):1375. https://doi.org/10.3390/molecules23061375

Chicago/Turabian Style

Vignal, Nicolas, Salvatore Cisternino, Nathalie Rizzo-Padoin, Carine San, Fortune Hontonnou, Thibaut Gelé, Xavier Declèves, Laure Sarda-Mantel, and Benoît Hosten. 2018. "[18F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model" Molecules 23, no. 6: 1375. https://doi.org/10.3390/molecules23061375

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