Linoleoyl ethanolamide is an endocannabinoid detected in porcine brain and murine peritoneal macrophages which contains linoleate in place of the arachidonate moiety of arachidonyl ethanolamide （AEA）. It has weak affinity for the cannabinoid 1 （CB1） and CB2 receptors， exhibiting Ki values of 10 uM and 25 uM， respectively. However， it is only approximately 4-fold less potent than AEA at causing catalepsy in mice （ED50 of 26.5 mg/kg）. In addition， linoleoyl ethanolamide increases ERK phosphorylation and AP-1-dependent transcription approximately 1.5 fold at 15 uM in a CB-receptor-independent manner. However， cellular toxicity is readily apparent at concentrations of 10-20 uM. Linoleoyl ethanolamide inhibits human fatty acid amide hydrolase-dependent hydrolysis of AEA with a Ki value of 9.0 uM， but also is hydrolyzed effectively by the enzyme.
产品描述
An endocannabinoid that contains linoleate in place of the arachidonate moiety of AEA； has been detected in porcine brain and murine peritoneal macrophages and has weak affinity for the CB1 and CB2 receptors （Kis =10 uM and 25 uM， respectively）； 4-fold less potent than AEA at causing catalepsy in mice （ED50 = 26.5 mg/kg）； increases ERK phosphorylation and AP-1-dependent transcription approximately 1.5 fold at 15 uM in a CB-receptor-independent manner； inhibits human FAAH-dependent hydrolysis of AEA （Ki = 9.0 uM）， but is also effectively hydrolyzed by the enzyme
