potent, reversible MAGL serine hydrolase inh.
orally efficacious in inflamm. pain model
from optimization of prior ligand
Bioorg. Med. Chem. Lett., May 7, 2020
Janssen R&D, Spring House, PA
“Compound 6g”
1 min read
“Compound 6g” is a potent, selective, and reversible inhibitor of monoacylglycerol lipase (MAGL), which degrades the cannabinoid receptor (CB) agonist 2-arachidononylglycerol (2-AG) to arachadonic acid (AA). Inhibition of MAGL therefore indirectly agonizes CB receptors and reduces inflammatory AA levels, which may be beneficial for a range of disorders. In contrast to most prior MAGL inhibitors which are covalent modifiers, this compound is a reversible inhibitor.
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