publication . Article . 2015

Efficient tritiation of the TSPO (18 kDa) selective ligand DPA-714

Damont, Annelaure; Garcia-Argote, Sébastien; Buisson, David-Alexandre; Rousseau, Bernard; Dollé, Frédéric;
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  • Published: 23 Jan 2015 Journal: Journal of Labelled Compounds and Radiopharmaceuticals, volume 58, pages 1-6 (issn: 0362-4803, Copyright policy)
  • Publisher: Wiley
Abstract
DPA-714 (N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide) is a recently discovered fluorinated ligand of the translocator protein 18 kDa (TSPO). Labelled with the short-lived positron emitter fluorine-18, this structure is today the radioligand of reference for in vivo imaging of microglia activation and neuroinflammatory processes with positron emission tomography. In the present work, an isotopically tritium-labelled version was developed ([3H]DPA-714), in order to access high resolution in vitro and ex vivo microscopic autoradiography studies, repeated and long-lasting receptor binding studies and in vivo pharma...
Subjects
free text keywords: isotopic labelling, TSPO 18 kDa, PBR, tritiodebromination, hydrogen-for-tritium exchange, Ligand, Chemistry, Radioligand, Biochemistry, Pyrimidine, chemistry.chemical_compound, Acetamide, Ligand (biochemistry), DPA-714, Translocator protein, biology.protein, biology, Tritium
Related Organizations
Funded by
EC| INMIND
Project
INMIND
Imaging of Neuroinflammation in Neurodegenerative Diseases
  • Funder: European Commission (EC)
  • Project Code: 278850
  • Funding stream: FP7 | SP1 | HEALTH
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publication . Article . 2015

Efficient tritiation of the TSPO (18 kDa) selective ligand DPA-714

Damont, Annelaure; Garcia-Argote, Sébastien; Buisson, David-Alexandre; Rousseau, Bernard; Dollé, Frédéric;