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

Tijdschriftbijdrage - Tijdschriftartikel

Cannabinoid receptors type 2 (CB2R) represent an attractive therapeutic target for neurodegenerative diseases and cancer. Aiming at the development of a positron emission tomography (PET) radiotracer to monitor receptor density and/or occupancy during a CB2R-tailored therapy, we herein describe the radiosynthesis of 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. The first biological evaluation revealed that [18F]LU14 is a highly affine CB2R radioligand with >80% intact tracer in the brain at 30 min p.i. Its further evaluation by PET in a well-established rat model of CB2R overexpression demonstrated its ability to selectively image the CB2R in the brain and its potential as a tracer to further investigate disease-related changes in CB2R expression.
Tijdschrift: International Journal of Molecular Sciences
ISSN: 1661-6596
Issue: 15
Volume: 22
Aantal pagina's: 18
Jaar van publicatie:2021
Trefwoorden:Biochemie & -fysica en Moleculaire biologie, Multidisciplinaire scheikunde