Multi-parameter optimization: Development of a morpholin-3-one derivative with an improved kinetic profile for imaging monoacylglycerol lipase in the brain

• Published in: European journal of medicinal chemistry Vol. 243; pp. 114750 - 114764
• Main Authors: He, Yingfang, Grether, Uwe, Taddio, Marco F., Meier, Carla, Keller, Claudia, Edelmann, Martin R., Honer, Michael, Huber, Sylwia, Wittwer, Matthias B., Heer, Dominik, Richter, Hans, Collin, Ludovic, Hug, Melanie N., Hilbert, Manuel, Postmus, Annemarieke G.J., Stevens, Anna Floor, van der Stelt, Mario, Krämer, Stefanie D., Schibli, Roger, Mu, Linjing, Gobbi, Luca C.
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 05.12.2022; Elsevier
• Subjects: Brain imaging; Chemistry, Medicinal; Life Sciences & Biomedicine; MAGL; Morpholin-3-one derivatives; PET tracer; Pharmacology & Pharmacy; Science & Technology; Structural optimization; MAGL; Brain imaging; PET tracer; Structural optimization; Morpholin-3-one derivatives; CENTRAL-NERVOUS-SYSTEM; DISCOVERY

Monoacylglycerol lipase (MAGL) is a gatekeeper in regulating endocannabinoid signaling and has gained substantial attention as a therapeutic target for neurological disorders. We recently discovered a morpholin-3-one derivative as a novel scaffold for imaging MAGL via positron emission tomography (P...