Development of High Brain-Penetrant and Reversible Monoacylglycerol Lipase PET Tracers for Neuroimaging
| Autor: | Yingfang He, Matthias Schild, Uwe Grether, Jörg Benz, Lea Leibrock, Dominik Heer, Andreas Topp, Ludovic Collin, Bernd Kuhn, Matthias Wittwer, Claudia Keller, Luca C. Gobbi, Roger Schibli, Linjing Mu |
|---|---|
| Rok vydání: | 2022 |
| Předmět: |
Molecular Conformation
Brain Neuroimaging Crystallography X-Ray Monoacylglycerol Lipases Rats Mice Structure-Activity Relationship Drug Stability Positron-Emission Tomography Drug Discovery Molecular Medicine Animals Tissue Distribution Carbon Radioisotopes Enzyme Inhibitors Radiopharmaceuticals Rats Wistar |
| Zdroj: | Journal of medicinal chemistry. 65(3) |
| ISSN: | 1520-4804 |
| Popis: | Monoacylglycerol lipase (MAGL) is one of the key enzymes in the endocannabinoid system. Inhibition of MAGL has been proposed as an attractive approach for the treatment of various diseases. In this study, we designed and successfully synthesized two series of piperazinyl pyrrolidin-2-one derivatives as novel reversible MAGL inhibitors. ( |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|