Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development
Year: 2020
Type: article
Abstract: The endocannabinoid system (ECS) is involved in a wide range of biological functions and comprises cannabinoid receptors and enzymes responsible for endocannabinoid synthesis and degradation. Over the past 2 decades, significant advances toward 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.
Source: Journal of Medicinal Chemistry
Institutions: Jinan University, First Affiliated Hospital of Jinan University, Harvard University, Massachusetts General Hospital, Scripps Research Institute, Centre for Addiction and Mental Health, University of Toronto, ETH Zurich, Institute of Pharmaceutical Sciences, Umeå University, National Institutes for Quantum Science and Technology, National Institute of Radiological Sciences
Language: English
Subfield: Pharmacology
Field: Medicine
Domain: Health Sciences
Open Access status: green
Funders: Canada Foundation for Innovation, Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung, Canada Research Chairs, National Natural Science Foundation of China, Ministry of Education of the People's Republic of China, Azrieli Foundation, Basic and Applied Basic Research Foundation of Guangdong Province, National Institute on Aging, National Institute on Drug Abuse
Awards: G11191501, G120164892, G1491884472, G2214356056, G3593534703, G3687771071, In Vivo Inhibition and Functional Characterization of the Calcium-dependent Acyltransferase PLA2G4E, G3977483212, Translation of tau-selective PET radiopharmaceuticals in Alzheimers patients, New PET tracers for neuroimaging of FAAH in endocannabinoid signaling, G576783429, G6946693079, G7331048563, G7777734671, Neuro-PET Radiotracer Discovery for Imaging Glycogen Synthase Kinase-3, G8740365566
OpenAlex ID: W3115672273