SAR127303 / Sanofi - LARVOL DELTA

Neuroprotective effects of minocycline and KML29, a potent inhibitor of monoacylglycerol lipase, in an experimental stroke model: a small-animal positron emission tomography study. (PubMed, Theranostics) - "PET studies of the brains of the ischemic rats were performed at several experimental time points (pre-occlusion, days 2, 4, and 7 after the MCAO surgery) using [C]SAR127303 for MAGL and [F]FEBMP for 18 kDa translocator protein (TSPO, a hall-mark of neuroinflammation). In MCAO rats, minocycline treatment showed a neuroprotective effect in the sensorimotor cortex suffering from severe hypoxic injury, whereas KML29 treatment saved neurons in the striatum, including bundles of myelinated axons. PET imaging allowed visualization of the different neuroprotective effects of minocycline and KML29, and indicated that combination pharmacotherapy using these drugs may be an effective therapy in acute ischemia."

Journal • Cardiovascular • Immunology • Inflammation • Metabolic Disorders

Demonstration of high affinity, reversible JNJ-42226314 binding by monoacylglycerol lipase in brain homogenates and via autoradiography using [3H]SAR-127303 (Neuroscience 2019) - "Jump dilution with a tracer solution further shows the reversibility of JNJ-42226314 and its Koff. In vitro autoradiography experiments using native rodent, simian and human brain samples further show the brain distribution of MGLL."