Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor

Cannabinoid CB2 PET tracers are considered as a promising alternative to PBR/TSPO tracers for the in-vivo imaging of neuroinflammation. We describe here the synthesis and characterization of compound 3, a new potent and brain penetrating CB2 ligand based on an original triazine template. The PET tra...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-01, Vol.24 (1), p.283-287
Main Authors: Hortala, Laurent, Arnaud, Joëlle, Roux, Pascale, Oustric, Didier, Boulu, Laurent, Oury-Donat, Florence, Avenet, Patrick, Rooney, Thomas, Alagille, David, Barret, Olivier, Tamagnan, Gilles, Barth, Francis
Format: Article
Language:English
Subjects:
Animals
Brain
Brain - metabolism
Fluorine Radioisotopes - chemistry
Fluorine Radioisotopes - metabolism
Fluorine Radioisotopes - pharmacokinetics
Humans
Ligands
Macaca mulatta
Molecular Structure
Papio
Positron-Emission Tomography
Receptor, Cannabinoid, CB2 - metabolism
Triazines - chemical synthesis
Triazines - metabolism
Triazines - pharmacokinetics
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Summary:Cannabinoid CB2 PET tracers are considered as a promising alternative to PBR/TSPO tracers for the in-vivo imaging of neuroinflammation. We describe here the synthesis and characterization of compound 3, a new potent and brain penetrating CB2 ligand based on an original triazine template. The PET tracer [(18)F]-dideutero-3 was prepared in a three steps radiosynthesis, and demonstrated significant uptake in rhesus macaque and baboon brain with a maximum SUV of about 0.7-0.9g/mL, followed by a moderate washout over time.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.11.023