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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Amidohydrolases / chemistry
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Analgesics / chemical synthesis*
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Analgesics / chemistry
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Analgesics / pharmacology
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Animals
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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents / pharmacology
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Aspirin / pharmacology
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Cannabinoid Receptor Modulators / chemistry
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Enzyme Inhibitors / pharmacology
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Indomethacin / chemistry
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Inflammation
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Kinetics
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Models, Chemical
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Monoacylglycerol Lipases / antagonists & inhibitors*
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Monoacylglycerol Lipases / chemistry
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Rats
Substances
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Analgesics
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Anti-Inflammatory Agents
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Cannabinoid Receptor Modulators
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Enzyme Inhibitors
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Monoacylglycerol Lipases
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Amidohydrolases
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fatty-acid amide hydrolase
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Aspirin
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Indomethacin