Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 62, Issue 18, Pages 8532-8543Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b00847
Keywords
-
Categories
Ask authors/readers for more resources
Monoacylglycerol lipase (MAGL), a serine hydrolase extensively expressed throughout the brain, serves as a key gatekeeper regulating the tone of endocannabinoid signaling. Preclinically, inhibition of MAGL is known to provide therapeutic benefits for a number of neurological disorders. The availability of a MAGL-specific positron emission tomography (PET) ligand would considerably facilitate the development and clinical characterization of MAGL inhibitors via noninvasive and quantitative PET imaging. Herein, we report the identification of the potent and selective irreversible MAGL inhibitor 7 (PF-06809247) as a suitable radioligand lead, which upon radiolabeling was found to exhibit a high level of MAGL specificity; this enabled cross-species measurement of MAGL brain expression (B-max), assessment of in vivo binding in the rat, and nonhuman primate PET imaging.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available