- A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity.
A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity.
Bioorganic & medicinal chemistry letters (2008-09-30)
Victoria Magrioti, George Naxakis, Dimitra Hadjipavlou-Litina, Alexandros Makriyannis, George Kokotos
PMID18819796
ABSTRACT
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 (K(i) 21.8 microM) 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.