Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor |
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| Institution: | 1. Division of Molecular Imaging, Institute of Biomedical Research and Innovation, Kobe, Japan;2. Department of Nuclear Medicine, Saitama Medical University International Medical Center, Hidaka, Japan;3. Department of Radiological Technology, Okayama Rosai Hospital, Okayama, Japan;4. Department of Psychiatry, Kobe University Graduate School of Medicine, Kobe, Japan;5. Division of Bio-Function Dynamics Imaging, Center for Life Science Technologies RIKEN, Kobe, Japan;6. Division of Pharmaceutical Chemistry, Center Showa Pharmaceutical University, Machida, Japan;1. Research Imaging Centre, Centre for Addiction and Mental Health, Toronto, ON, Canada M5T 1R8;2. Institute of Medical Science, University of Toronto, Toronto, ON, Canada M5S 1A8;3. Department of Psychiatry, University of Toronto, Toronto, ON, Canada M5T 1R8;4. Department of Radiology, Harvard Medical School and Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, Boston, MA 02114, USA |
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| 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 0.7–0.9 g/mL, followed by a moderate washout over time. |
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| Keywords: | Cannabinoid CB2 PET Imaging Triazine |
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