Exploring the fatty acid amide hydrolase and cyclooxygenase inhibitory properties of novel amide derivatives of ibuprofen
Alessandro Deplano, Jessica Karlsson, Mona Svensson, Federica Moraca, Bruno Catalanotti, Christopher J. Fowler, Valentina Onnis
Abstract
value of 0.26 µM and an α value of 4.9. At a concentration of 10 µM, the compound did not inhibit the cyclooxygenation of arachidonic acid by either ovine COX-1 or human recombinant COX-2. However, this concentration of Ibu-AM68 greatly reduced the ability of the COX-2 to catalyse the cyclooxygenation of the endocannabinoid 2-arachidonoylglycerol. It is concluded that Ibu-AM68 is a dual-acting FAAH/substrate-selective COX inhibitor.
Topics & Concepts
Fatty acid amide hydrolaseAnandamideChemistryCyclooxygenaseIbuprofenArachidonic acidAmidaseEndocannabinoid systemAmideCannabinoidPharmacologyBiochemistryIC50EnzymeStereochemistryCannabinoid receptorAntagonistReceptorIn vitroBiologyCannabis and Cannabinoid ResearchDrug-Induced Hepatotoxicity and ProtectionDrug Transport and Resistance Mechanisms