Abstract
Oleoylethanolamide and palmitoylethanolamide are members of the fatty acid ethanolamide family, also known as acylethanolamides. Their physiological effects, including glucose homeostasis, anti-inflammation, anti-anaphylactic, analgesia, and hypophagia, have been reported. They have affinity for different receptor proteins, including nuclear receptors such as PPARα, channels such as TRPV1, and membrane receptors such as GPR119 and GPR55. In the present review, the pathophysiological functions of fatty acid ethanolamides have been discussed from the perspective of receptor pharmacology and drug discovery.
Highlights
Arachidonylethanolamide (AEA, known as anandamide), oleoylethanolamide (OEA), and palmitoylethanolamide (PEA) are members of the acylethanolamide or fatty acid ethanolamide family, and are each composed of a fatty acid and an ethanolamine linked together by an amide bond [1]
GPR119 expression in pancreatic β-cells and intestinal L-cells makes it as an attractive therapeutic target in type 2 diabetes; stimulation of glucose-dependent insulin secretion from β-cell by increased plasma GLP-1 released by L-cells provides new avenues for diabetes treatment using GLP-1 analogs and dipeptidyl peptidase 4 inhibitors
PEA caused a concentration-dependent increase in outflow facility in an anterior segment porcine organ culture model, which was speculated to be mediated by GPR55 and peroxisome proliferator-activated receptor-α (PPARα) [93]
Summary
Arachidonylethanolamide (AEA, known as anandamide), oleoylethanolamide (OEA), and palmitoylethanolamide (PEA) are members of the acylethanolamide or fatty acid ethanolamide family, and are each composed of a fatty acid and an ethanolamine linked together by an amide bond [1]. These acylethanolamides are present in both animals and plants [2,3]. All acylethanolamides have a common ethanolamide structure, they differ with respect to the attached fatty acid. Specific receptor proteins recognize them by their differences in the chain length and degree of unsaturation of the fatty acids, which act as agonists/antagonists or activators/blockers. GPR119 and GPR55 are discussed along with the proposed ligands, OEA and PEA, from the perspective of the pharmacology of intercellular lipid mediators and drug discovery
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