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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hortala L,Arnaud J,Roux P,Oustric D,Boulu L,Oury-Donat F,Avenet P,Rooney T,Alagille D,Barret O,Tamagnan G,Barth F

doi

10.1016/j.bmcl.2013.11.023

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

283-7

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01302-4

journal_volume

24

pub_type

杂志文章

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