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Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain

Teodoro, R.; Gündel, D.; Ueberham, L.; Toussaint, M.; Bormans, G.; Brust, P.; Deuther-Conrad, W.; Moldovan, R.-P.

Cannabinoid receptors represent an attractive therapeutic target for neurodegenerative diseases and cancer. Aiming at a positron emission tomography (PET) radiotracer to monitor neuronal changes of receptor density and/or occupancy during the CB2R-tailored therapy, we developed here cis-[18F]1-(4-fluorobutyl-N-((1s,4s)-4-methylcyclohexyl)-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide ([18F]LU14) starting from the corresponding mesylate precursor. First biological evalua-tion revealed that [18F]LU14 is a highly affine CB2R radioligand with optimal metabolic stability (>80% intact tracer in brain at 30 min p.i.). Its further evaluation in a well-established rat model of CB2R overexpression by PET demonstrated its ability to selectively image the CB2R in the brain and its potential as tracer to further investigate diseased related CB2R alterations.

Keywords: Cannabinoid receptor type 2; naphtyrid-2-one; binding affinity; radiochemistry; fluorine-18 labeling; brain; positron emission tomography (PET)

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Publ.-Id: 32557