Document Detail


A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity.
MedLine Citation:
PMID:  18819796     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Victoria Magrioti; George Naxakis; Dimitra Hadjipavlou-Litina; Alexandros Makriyannis; George Kokotos
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2008-09-12
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  18     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2008 Oct 
Date Detail:
Created Date:  2008-10-20     Completed Date:  2009-04-24     Revised Date:  2013-08-01    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  5424-7     Citation Subset:  IM    
Affiliation:
Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Athens 15771, Greece.
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MeSH Terms
Descriptor/Qualifier:
Amidohydrolases / chemistry
Analgesics / chemical synthesis*,  chemistry,  pharmacology
Animals
Anti-Inflammatory Agents / chemical synthesis*,  pharmacology
Aspirin / pharmacology
Cannabinoid Receptor Modulators / chemistry
Chemistry, Pharmaceutical / methods*
Drug Design
Enzyme Inhibitors / pharmacology
Indomethacin / chemistry
Inflammation
Kinetics
Models, Chemical
Monoacylglycerol Lipases / antagonists & inhibitors*,  chemistry
Rats
Grant Support
ID/Acronym/Agency:
DA3801/DA/NIDA NIH HHS; R01 DA003801/DA/NIDA NIH HHS
Chemical
Reg. No./Substance:
0/Analgesics; 0/Anti-Inflammatory Agents; 0/Cannabinoid Receptor Modulators; 0/Enzyme Inhibitors; 50-78-2/Aspirin; 53-86-1/Indomethacin; EC 3.1.1.23/Monoacylglycerol Lipases; EC 3.5.-/Amidohydrolases; EC 3.5.1.-/fatty-acid amide hydrolase
Comments/Corrections

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