Abstract
A series of novel oxime carbamates have been identified as potent inhibitors of the key regulatory enzyme of the endocannabinoid signaling system, fatty acid amide hydrolase (FAAH). In this Letter, the rationale behind the discovery and the biological evaluations of this novel class of FAAH inhibitors are presented. Both in vitro and in vivo results of selected targets are discussed, along with inhibition kinetics and molecular modeling studies.(1).
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Amidohydrolases / antagonists & inhibitors*
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Amidohydrolases / physiology
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Animals
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Cannabinoid Receptor Modulators / physiology
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Carbamates / chemistry*
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Carbamates / metabolism
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Carbamates / pharmacology
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Cell Line
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Crystallography, X-Ray
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Drug Discovery / methods*
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Humans
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Oximes / chemistry*
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Oximes / metabolism
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Oximes / pharmacology*
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Protein Binding / physiology
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Protein Structure, Tertiary
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Rats
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Signal Transduction / drug effects
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Signal Transduction / physiology
Substances
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Cannabinoid Receptor Modulators
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Carbamates
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Oximes
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Amidohydrolases
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fatty-acid amide hydrolase