Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development

Hou, Lu; Rong, Jian; Haider, Ahmed; Ogasawara, Daisuke; Varlow, Cassis; Schafroth, Michael A; Mu, Linjing; Gan, Jiefeng; Xu, Hao; Fowler, Christopher J; Zhang, Ming-Rong; Vasdev, Neil; Ametamey, Simon; Cravatt, Benjamin F; Wang, Lu; Liang, Steven H

doi:10.1021/acs.jmedchem.0c01459

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Hou, L., Rong, J., Haider, A., Ogasawara, D., Varlow, C., Schafroth, M. A., Mu, L., Gan, J., Xu, H., Fowler, C. J., Zhang, M.-R., Vasdev, N., Ametamey, S., Cravatt, B. F., Wang, L., & Liang, S. H. (2021). Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development. Journal of Medicinal Chemistry, 64, 123–149. https://doi.org/10.1021/acs.jmedchem.0c01459

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)