Oleoyl ethanolamide (OEA) is an endogenous agonist for proliferator-activated receptor α (PPARα) that suppresses food intake, promotes lipolysis, and reduces weight gain in rodents. The biological effects of OEA are terminated by fatty-acid amide hydrolase and N-acylethanolamine-hydrolyzing acid amidase. AM3102 is an OEA analog that stimulates PPARα transcriptional activity with an EC50 value of 100 nM and prolongs feeding latency in rodents with an ED50 value of 2.4 mg/kg. It is resistant to enzymatic hydrolysis and is as potent as OEA in enhancing transcriptional activity of PPARα and reducing food intake in free-feeding rats. AM3102 demonstrates weak affinity for the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 33 and 26 μM, respectively.
