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Article

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

1
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, Department of Neuroradiopharmaceuticals, Research Site Leipzig, 04318 Leipzig, Germany
2
Radiopharmaceutical Research, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, BE-3000 Leuven, Belgium
3
The Lübeck Institute of Experimental Dermatology, University Medical Center Schleswig-Holstein, 23562 Lübeck, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: Rosaria Meccariello
Int. J. Mol. Sci. 2021, 22(15), 8051; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22158051
Received: 25 June 2021 / Revised: 20 July 2021 / Accepted: 23 July 2021 / Published: 28 July 2021
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. View Full-Text
Keywords: cannabinoid receptor type 2; naphtyrid-2-one; binding affinity; radiochemistry; fluorine-18 labelling; brain; positron emission tomography cannabinoid receptor type 2; naphtyrid-2-one; binding affinity; radiochemistry; fluorine-18 labelling; brain; positron emission tomography
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MDPI and ACS Style

Teodoro, R.; Gündel, D.; Deuther-Conrad, W.; Ueberham, L.; Toussaint, M.; Bormans, G.; Brust, P.; Moldovan, R.-P. Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain. Int. J. Mol. Sci. 2021, 22, 8051. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22158051

AMA Style

Teodoro R, Gündel D, Deuther-Conrad W, Ueberham L, Toussaint M, Bormans G, Brust P, Moldovan R-P. Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain. International Journal of Molecular Sciences. 2021; 22(15):8051. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22158051

Chicago/Turabian Style

Teodoro, Rodrigo, Daniel Gündel, Winnie Deuther-Conrad, Lea Ueberham, Magali Toussaint, Guy Bormans, Peter Brust, and Rareş-Petru Moldovan. 2021. "Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain" International Journal of Molecular Sciences 22, no. 15: 8051. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22158051

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