Abstract
Biosynthesis Inhibition: O-5596, a new inhibitor of the biosynthesis of the endocannabinoid, 2-arachidonoylglycerol, was synthesized and found to be potent (IC(50)=100 nM) and selective versus other proteins and enzymes of the endocannabinoid system in vitro and active in vivo at reducing food intake in mice.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Alkenes / chemical synthesis*
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Alkenes / chemistry
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Alkenes / pharmacology*
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Animals
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Arachidonic Acids / biosynthesis*
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Arachidonic Acids / chemistry
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Cell Line
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Drug Stability
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Eating / drug effects
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Endocannabinoids
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Glycerides / biosynthesis*
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Glycerides / chemistry
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Humans
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Lipoprotein Lipase / antagonists & inhibitors
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Lipoprotein Lipase / metabolism
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Mice
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Organophosphorus Compounds / chemical synthesis*
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Organophosphorus Compounds / chemistry
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Organophosphorus Compounds / pharmacology*
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Receptor, Cannabinoid, CB1 / antagonists & inhibitors
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Receptor, Cannabinoid, CB1 / metabolism
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Receptor, Cannabinoid, CB2 / antagonists & inhibitors
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Receptor, Cannabinoid, CB2 / metabolism
Substances
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Alkenes
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Arachidonic Acids
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Endocannabinoids
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Enzyme Inhibitors
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Glycerides
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O-5596
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Organophosphorus Compounds
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Receptor, Cannabinoid, CB1
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Receptor, Cannabinoid, CB2
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glyceryl 2-arachidonate
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DAGLA protein, human
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Lipoprotein Lipase