title: Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor.
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 [(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.
authors.affiliation: Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
authors.forename: Laurent
authors.initials: L
authors.lastname: Hortala
authors.affiliation: Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
authors.forename: Joëlle
authors.initials: J
authors.lastname: Arnaud
authors.affiliation: Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
authors.forename: Pascale
authors.initials: P
authors.lastname: Roux
authors.affiliation: Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
authors.forename: Didier
authors.initials: D
authors.lastname: Oustric
authors.affiliation: Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
authors.forename: Laurent
authors.initials: L
authors.lastname: Boulu
authors.affiliation: Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France.
authors.forename: Florence
authors.initials: F
authors.lastname: Oury-Donat
authors.affiliation: Exploratory Unit, Sanofi R&D, 1 Avenue Pierre Brossolette, 91385 Chilly-Mazarin, France.
authors.forename: Patrick
authors.initials: P
authors.lastname: Avenet
authors.affiliation: Aging TSU, Sanofi R&D, 1 Avenue Pierre Brossolette, 91385 Chilly-Mazarin, France.
authors.forename: Thomas
authors.initials: T
authors.lastname: Rooney
authors.affiliation: Molecular NeuroImaging, 60 Temple St, New Haven, CT 06510, USA.
authors.forename: David
authors.initials: D
authors.lastname: Alagille
authors.affiliation: Molecular NeuroImaging, 60 Temple St, New Haven, CT 06510, USA.
authors.forename: Olivier
authors.initials: O
authors.lastname: Barret
authors.affiliation: Molecular NeuroImaging, 60 Temple St, New Haven, CT 06510, USA.
authors.forename: Gilles
authors.initials: G
authors.lastname: Tamagnan
authors.affiliation: Exploratory Unit, Sanofi R&D, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France. Electronic address: francis.barth@sanofi.com.
authors.forename: Francis
authors.initials: F
authors.lastname: Barth
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D005462:Fluorine Radioisotopes / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics; D006801:Humans; D008024:Ligands; D008253:Macaca mulatta; D015394:Molecular Structure; D010215:Papio; D049268:Positron-Emission Tomography; D043885:Receptor, Cannabinoid, CB2 / Q000378:metabolism*; D014227:Triazines / Q000138:chemical synthesis / Q000378:metabolism* / Q000493:pharmacokinetics
chemical_list: D005462:Fluorine Radioisotopes; D008024:Ligands; D043885:Receptor, Cannabinoid, CB2; D014227:Triazines
keywords: CB2; Cannabinoid; Imaging; PET; Triazine