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Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain.


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.

SUBMITTER: Teodoro R 

PROVIDER: S-EPMC8347709 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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

Teodoro Rodrigo R   Gündel Daniel D   Deuther-Conrad Winnie W   Ueberham Lea L   Toussaint Magali M   Bormans Guy G   Brust Peter P   Moldovan Rareş-Petru RP  

International journal of molecular sciences 20210728 15


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 co  ...[more]

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