| Literature DB >> 35771668 |
Daniel Gündel1, Winnie Deuther-Conrad1, Lea Ueberham1, Sarandeep Kaur1, Elina Otikova1, Rodrigo Teodoro1, Magali Toussaint1, Thu Hang Lai1,2, Oliver Clauß1, Matthias Scheunemann1, Guy Bormans3, Michael Bachmann1, Klaus Kopka1,4, Peter Brust1,5, Rareş-Petru Moldovan1.
Abstract
The cannabinoid receptor type 2 (CB2R) is an attractive target for the diagnosis and therapy of neurodegenerative diseases and cancer. In this study, we aimed at the development of a novel 18F-labeled radioligand starting from the structure of the known naphthyrid-2-one CB2R ligands. Compound 28 (LU13) was identified with the highest binding affinity and selectivity versus CB1R (CB2RKi = 0.6 nM; CB1RKi/CB2RKi > 1000) and was selected for radiolabeling with fluorine-18 and biological characterization. The new radioligand [18F]LU13 showed high CB2R affinity in vitro as well as high metabolic stability in vivo. PET imaging with [18F]LU13 in a rat model of vector-based/-related hCB2R overexpression in the striatum revealed a high signal-to-background ratio. Thus, [18F]LU13 is a novel and highly promising PET radioligand for the imaging of upregulated CB2R expression under pathological conditions in the brain.Entities:
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Year: 2022 PMID： 35771668 DOI： 10.1021/acs.jmedchem.2c00256
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 8.039