Development of the High-Affinity Carborane-Based Cannabinoid Receptor Type 2 PET Ligand [¹⁸F]LUZ5-d₈.

ABSTRACT: The development of cannabinoid receptor type 2 (CB₂R) radioligands for positron emission tomography (PET) imaging was intensively explored. To overcome the low metabolic stability and simultaneously increase the binding affinity of known CB₂R radioligands, a carborane moiety was used as a bioisostere. Here we report the synthesis and characterization of carborane-based 1,8-naphthyridinones and thiazoles as novel CB₂R ligands. All tested compounds showed low nanomolar CB₂R affinity, with (Z)-N-[3-(4-fluorobutyl)-4,5-dimethylthiazole-2(3H)-ylidene]-(1,7-dicarba-closo-dodecaboranyl)-carboxamide (LUZ5) exhibiting the highest affinity (0.8 nM). Compound [¹⁸F]LUZ5-d_8<

SUBMITTER: Ueberham L 

PROVIDER: S-EPMC10782483 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature