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” 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…