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| Autor: | Rodrigo, Teodoro, Daniel, Gündel, Winnie, Deuther-Conrad, Lea, Ueberham, Magali, Toussaint, Guy, Bormans, Peter, Brust, Rareş-Petru, Moldovan |
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| Rok vydání: | 2021 |
| Předmět: |
Fluorine Radioisotopes
positron emission tomography brain Brain cannabinoid receptor type 2 naphtyrid-2-one fluorine-18 labelling Article Rats Rats Sprague-Dawley Receptor Cannabinoid CB2 Mice Positron-Emission Tomography binding affinity Animals Humans Female Naphthyridines Radiopharmaceuticals radiochemistry Cells Cultured Protein Binding |
| Zdroj: | International Journal of Molecular Sciences |
| ISSN: | 1422-0067 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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