Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain.
Rodrigo TeodoroDaniel GündelWinnie Deuther-ConradLea UeberhamMagali ToussaintGuy BormansPeter BrustRareş-Petru MoldovanPublished in: International journal of molecular sciences (2021)
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.
Keyphrases
- pet imaging
- positron emission tomography
- computed tomography
- resting state
- white matter
- pet ct
- poor prognosis
- cerebral ischemia
- binding protein
- functional connectivity
- cell proliferation
- papillary thyroid
- squamous cell carcinoma
- single cell
- mesenchymal stem cells
- stem cells
- deep learning
- smoking cessation
- subarachnoid hemorrhage
- young adults