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

oleh: Rodrigo Teodoro, Daniel Gündel, Winnie Deuther-Conrad, Lea Ueberham, Magali Toussaint, Guy Bormans, Peter Brust, Rareş-Petru Moldovan

Format: Article
Diterbitkan: MDPI AG 2021-07-01

Deskripsi

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 <i>cis</i>-[<sup>18</sup>F]1-(4-fluorobutyl-<i>N</i>-((1s,4s)-4-methylcyclohexyl)-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide ([<sup>18</sup>F]<b>LU14</b>) starting from the corresponding mesylate precursor. The first biological evaluation revealed that [<sup>18</sup>F]<b>LU14</b> 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.