Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain |
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| Authors: | Rodrigo Teodoro Daniel Gündel Winnie Deuther-Conrad Lea Ueberham Magali Toussaint Guy Bormans Peter Brust Rare-Petru Moldovan |
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| Affiliation: | 1.Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, Department of Neuroradiopharmaceuticals, Research Site Leipzig, 04318 Leipzig, Germany; (R.T.); (D.G.); (W.D.-C.); (L.U.); (M.T.); (P.B.);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 |
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| Abstract: | 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. |
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| Keywords: | cannabinoid receptor type 2 naphtyrid-2-one binding affinity radiochemistry fluorine-18 labelling brain positron emission tomography |
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