Quick hit: Ibuprofen as a FAAH Inhibitor

Some recent highlights and curiosities from the amazing world of cannabis science and therapeutics.
By Adrian Devitt-Lee On February 20, 2019

Nonsteroidal antiinflammatory drugs (NSAIDs) are one of the most common classes of painkillers, which includes aspirin, ibuprofen, celecoxib, and other pharmaceuticals. Their primary target is an enzyme called cyclooxygenase-2 (COX-2), which metabolizes many lipids (including endocannabinoids!) into a class of inflammatory molecules called prostaglandins. The side effects of NSAIDs are largely due to the inhibition of the related COX-1 enzyme, which can cause significant gastrointestinal problems. But ibuprofen distinguishes itself from other NSAIDs because it is also a FAAH inhibitor, meaning it slows the breakdown of anandamide and related molecules, including PEA and OEA. (These molecules are called fatty-acid ethanolamines.) A new paper by Italian chemists examines the molecular structure of ibuprofen, and explains how slight changes to ibuprofen’s structure can strengthen its ability to inhibit FAAH. Studying the so-called “structure-activity relationship” of existing drugs, as these scientists have done, aids the development of new pharmaceuticals.

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Adrian Devitt-Lee, a Project CBD contributing writer, is a graduate from Tufts University with a degree in mathematics and chemistry.