[Epub ahead of print]
Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor.
Hortala L, Arnaud J, Roux P, Oustric D, Oury-Donat F, Avenet P, Rooney T, Alagille D, Barret O, Tamagnan G, Barth F.
Source
Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
Abstract
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 [18F]-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.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Copyright © 2013 Elsevier Ltd. All rights reserved.
KEYWORDS:
CB2, Cannabinoid, Imaging, PET, Triazine
- PMID:
- 24291040
- [PubMed – as supplied by publisher]