@article{oai:repo.qst.go.jp:00081616, author = {Hou, Lu and Rong, Jian and Haider, Ahmed and Ogasawara, Daisuke and Varlow, Cassis and Schafroth, Michael and Mu, Linjing and Gan, Jiefeng and Xu, Hao and J. Fowler, Christopher and Ming-Rong, Zhang and Vasdev, Neil and Ametamey, Simon and F. Cravatt, Benjamin and Lu, Wang and Liang, Huan and Zhang, Ming-Rong and Lu, Wang and Liang, Huan}, issue = {1}, journal = {Journal of Medicinal Chemistry}, month = {Dec}, note = {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. Besides its physiological role, the ECS has been implicated in the development and pathophysiology of a number of central nervous system and peripheral diseases. 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, some of which have entered clinical trials. 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). Given the importance of the ECS for neuronal function, particular focus will be devoted to neuroimaging applications. State-of-the-art PET tracers for the ECS will be reviewed including their chemical design, pharmacological properties, radiolabeling strategies, 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.}, pages = {123--149}, title = {Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development}, volume = {64}, year = {2020} }