| Literature DB >> 33379862 |
Lu Hou1, Jian Rong2, Ahmed Haider2, Daisuke Ogasawara3, Cassis Varlow4, Michael A Schafroth3, Linjing Mu5, Jiefeng Gan1, Hao Xu1, Christopher J Fowler6, Ming-Rong Zhang7, Neil Vasdev2,4, Simon Ametamey5, Benjamin F Cravatt3, Lu Wang1,2, Steven H Liang2.
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.Entities:
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Year: 2020 PMID： 33379862 PMCID： PMC7877880 DOI： 10.1021/acs.jmedchem.0c01459
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446