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

作者：Magrioti Victoria; Naxakis George; Hadjipavlou Litina Dimitra; Makriyannis Alexandros; Kokotos George^*

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(20): 5424-5427.

DOI：10.1016/j.bmcl.2008.09.039

• 1,2-diamines
• endocannabinoids
• fatty acid amide hydrolase
• FAAH
• inhibitor
• monoacyglycerol lipase
• MGL

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 mu M) 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.

• 出版日期2008-10-15
• 单位东北大学