4.5 Article

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

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 1, 页码 283-287

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.11.023

关键词

Cannabinoid; CB2; PET; Imaging; Triazine

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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 [F-18]-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 0.7-0.9 g/mL, followed by a moderate washout over time. (C) 2013 Elsevier Ltd. All rights reserved.

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