Compound 4f / Takeda - LARVOL DELTA

Compound 4f, a novel brain-penetrant reversible monoacylglycerol inhibitor, ameliorates neuroinflammation, neuronal cell loss, and cognitive impairment in mice with kainic acid-induced neurodegeneration. (PubMed, PLoS One) - "Gene expression profiles and pathway analyses revealed that compound 4f reversed the KA-induced changes in the expression of genes related to inflammation and neurotransmission. These results indicate that the selective and reversible MAGL inhibitor, compound 4f, can be used as a potential therapeutic agent for the treatment of neurodegenerative diseases."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Inflammation

Compound 4f, a novel brain-penetrant reversible monoacylglycerol inhibitor, ameliorates neuroinflammation, neuronal cell loss and cognitive impairment in mice with kainic acid-induced neurodegeneration (Neuroscience 2022) - "The cannabinoid receptor 1 antagonist AM251 and cannabinoid receptor 2 antagonist AM630 partly blocked the neuroprotective effects of compound 4f in the hippocampus of KA-injected mice, suggesting that CB1R and CB2R signaling contributes to neuroprotective effects of compound 4f. Taken together, these results indicate that MAGL inhibitor compound 4f has potential therapeutic effects in neurodegenerative diseases accompanying neuroinflammation."

Preclinical • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • IL1B • IL6 • TNFA