4.5 Article

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

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 20, 页码 5424-5427

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.09.039

关键词

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

资金

  1. European Social Fund
  2. National Resources-(EPEAEK II) PYTHAGORAS
  3. National Institutes on Drug Abuse [DA3801]

向作者/读者索取更多资源

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. (C) 2008 Elsevier Ltd. All rights reserved.

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