Literature DB >> 18819796

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

Victoria Magrioti1, George Naxakis, Dimitra Hadjipavlou-Litina, Alexandros Makriyannis, George Kokotos.   

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.

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Year:  2008        PMID： 18819796      PMCID： PMC3712614          DOI： 10.1016/j.bmcl.2008.09.039

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  48 in total

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3.  Identification by nuclear magnetic resonance spectroscopy of an active-site hydrogen-bond network in human monoacylglycerol lipase (hMGL): implications for hMGL dynamics, pharmacological inhibition, and catalytic mechanism.

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  3 in total

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