A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity

A variety of long chain 1,2-diamines and related compounds were synthesized and tested for their activity on fatty acid amide hydrolase (FAAH) and monoacyglycerol lipase (MGL). (2S,9Z)-Octadec-9-ene-1,2-diamine selectively inhibits MGL (Ki 21.8 μμM) without significantly affecting FAAH. This compound exhibited interesting in vivo analgesic and anti-inflammatory properties, suggesting that selective inhibitors of MGL may be valuable novel agents for the treatment of inflammatory pain.

The synthesis of a selective MGL inhibitor presenting analgesic and anti-inflammatory activity is reported.Figure optionsDownload as PowerPoint slide