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Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development
- Source :
- J Med Chem
- Publication Year :
- 2021
-
Abstract
- The endocannabinoid system (ECS) is involved in a wide range of biological functions and is comprised of cannabinoid receptors and enzymes responsible for endocannabinoid synthesis and degradation. Over the past two decades, significant advances towards developing drugs and positron emission tomography (PET) tracers targeting different components of the ECS have been made. Herein, we summarized the recent development of PET tracers for imaging cannabinoid receptors 1 (CB1R) and 2 (CB2R) as well as the key enzymes monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), particularly focusing on PET neuroimaging applications. State-of-the-art PET tracers for the ECS will be reviewed including their chemical design, pharmacological properties, radiolabeling, as well as preclinical and human PET imaging. In addition, this review addresses the current challenges for ECS PET biomarker development and highlights the important role of PET ligands to study disease pathophysiology as well as to facilitate drug discovery.
- Subjects :
- Cannabinoid receptor
01 natural sciences
Article
Amidohydrolases
03 medical and health sciences
Neuroimaging
Fatty acid amide hydrolase
Drug Discovery
medicine
Animals
Humans
Enzyme Inhibitors
Receptors, Cannabinoid
030304 developmental biology
0303 health sciences
medicine.diagnostic_test
Drug discovery
Chemistry
Brain
Endocannabinoid system
3. Good health
0104 chemical sciences
Biomarker (cell)
Monoacylglycerol lipase
010404 medicinal & biomolecular chemistry
Positron emission tomography
Positron-Emission Tomography
Molecular Medicine
Neuroscience
Biomarkers
Endocannabinoids
Subjects
Details
- ISSN :
- 15204804
- Volume :
- 64
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- Journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....6a63466d63b88dc40732259bab5024cc