Inhibition of fatty acid amide hydrolase, a key endocannabinoid metabolizing enzyme, by analogues of ibuprofen and indomethacin.
@article{Holt2007InhibitionOF, title={Inhibition of fatty acid amide hydrolase, a key endocannabinoid metabolizing enzyme, by analogues of ibuprofen and indomethacin.}, author={Sandra Holt and Ben Paylor and Linda Boldrup and Kirsi Alajakku and S{\'e}verine Vandevoorde and A K Sundstr{\"o}m and Maria Teresa Cocco and Valentina Onnis and Christopher John Fowler}, journal={European journal of pharmacology}, year={2007}, volume={565 1-3}, pages={ 26-36 } }
65 Citations
Exploring the fatty acid amide hydrolase and cyclooxygenase inhibitory properties of novel amide derivatives of ibuprofen
- Biology, ChemistryJournal of enzyme inhibition and medicinal chemistry
- 2020
Ibu-AM68 is a dual-acting FAAH/substrate-selective COX inhibitor that reduces the gastrointestinal damage produced by non-steroidal anti-inflammatory agents such as sulindac and indomethacin in experimental animals.
Inhibitory properties of ibuprofen and its amide analogues towards the hydrolysis and cyclooxygenation of the endocannabinoid anandamide
- Chemistry, BiologyJournal of enzyme inhibition and medicinal chemistry
- 2013
Eight ibuprofen analogues were investigated and compound 2 was confirmed to be active in vivo in a murine model of visceral nociception, but the effects of the compound were not blocked by CB receptor antagonists.
Inhibition of Endocannabinoid Metabolism by the Metabolites of Ibuprofen and Flurbiprofen
- MedicinePloS one
- 2014
It is concluded that the primary metabolites of ibuprofen and flurbiprofen retain some of the properties of the parent compound with respect to inhibition of endocannabinoid metabolism, however, these effects are unlikely to contribute to the actions of theparent compounds in vivo.
The fatty acid amide hydrolase and cyclooxygenase-inhibitory properties of novel amide derivatives of carprofen.
- Chemistry, BiologyBioorganic chemistry
- 2020
Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors.
- Biology, ChemistryJournal of medicinal chemistry
- 2010
The synthesis and evaluation for their FAAH inhibitory activities of a series of 18 paracetamol esters are described, and it is concluded that the compound may be a useful template for the design of potent novel inhibitors of FAAH.
Inhibition of fatty acid amide hydrolase and cyclooxygenase by the N-(3-methylpyridin-2-yl)amide derivatives of flurbiprofen and naproxen.
- Chemistry, BiologyEuropean journal of pharmacology
- 2013
Novel propanamides as fatty acid amide hydrolase inhibitors.
- Biology, ChemistryEuropean journal of medicinal chemistry
- 2017
Discovery and development of endocannabinoid-hydrolyzing enzyme inhibitors.
- Biology, ChemistryCurrent topics in medicinal chemistry
- 2010
The inactivation of FAAH and MGL by specific enzyme inhibitors increases the levels of AEA and 2-AG, respectively, producing therapeutic effects such as pain relief and depression of anxiety.
Overview of the chemical families of fatty acid amide hydrolase and monoacylglycerol lipase inhibitors.
- Biology, ChemistryCurrent topics in medicinal chemistry
- 2008
The purpose of this review is to give an overview of the families of synthetic inhibitors of FAAH and MAGL, which contain few members and most of them exhibit a lack of selectivity.
Design, synthesis and in vitro and in vivo biological evaluation of flurbiprofen amides as new fatty acid amide hydrolase/cyclooxygenase-2 dual inhibitory potential analgesic agents
- BiologyJournal of enzyme inhibition and medicinal chemistry
- 2021
Flu-AM4 is identified as a dual-action FAAH/substrate-selective COX inhibitor with anti-inflammatory and analgesic activity in animal pain models, underscore the potential usefulness of such dual- action compounds.
References
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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.
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