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Effects of homologues and analogues of palmitoylethanolamide upon the inactivation of the endocannabinoid anandamide
TLDR
Palmitoylisopropylamide may prove useful as a template for design of compounds that reduce the cellular accumulation and metabolism of AEA without affecting either CB1 or CB2 receptors.
Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2‐arachidonoylglycerol
TLDR
It is concluded that compounds like α‐Methyl‐1‐AG, O‐2203 and O-2204 may be useful as leads for the discovery of selective MAGL inhibitors that lack direct effects upon cannabinoid receptors.
Acidic Nonsteroidal Anti-inflammatory Drugs Inhibit Rat Brain Fatty Acid Amide Hydrolase in a pH-dependent Manner
TLDR
The data are consistent with the conclusion that the non-ionised forms of the acidic NSAIDs are responsible for the inhibition of fatty acid amide hydrolase.
Design, synthesis and biological evaluation of new endocannabinoid transporter inhibitors.
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.
TLDR
It is hoped that these compounds, particularly the most potent in this series (compound 5, UCM707, with IC(50) values for anandamide uptake and FAAH of 0.8 and 30 microM, respectively), will provide useful tools for the elucidation of the role of the an andamide transporter system in vivo.
Effects of pH on the inhibition of fatty acid amidohydrolase by ibuprofen
TLDR
The higher potency of ibuprofen at lower pH values raises the possibility that in certain types of inflamed tissue, the concentration of this compound following oral administration may be sufficient to inhibit FAAH.
Ibuprofen inhibits rat brain deamidation of anandamide at pharmacologically relevant concentrations. Mode of inhibition and structure-activity relationship.
TLDR
It is concluded that ibuprofen inhibits anandamide deamidation at pharmacologically relevant concentrations and that there is some specificity to the inhibition produced by ib uprofen and suprofen.
Inhibition of anandamide hydrolysis by the enantiomers of ibuprofen, ketorolac, and flurbiprofen.
TLDR
There is no dramatic enantiomeric selectivity of NSAID compounds as inhibitors of fatty acid amide hydrolase enzyme(s) responsible for the hydrolysis of anandamide, and the enantiomers of flurbiprofen and R-ketorolac are the most potent NSAID inhibitors of omega-3 acid Hydrolase yet reported.
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