(±)-2-Methyl arachidonoyl-2’-fluoroethylamide (2-Methyl-2’-fluoro AEA) is an analog of anandamide (AEA) in which the alcohol of the ethanolamide group has been removed and replaced with a fluorine atom. This substitution confers considerably increased binding affinity for the CB1 receptor. It also confers additional selectivity, in that binding to CB2 is decreased relative to AEA. However, the in vivo activity of 2-fluoro AEA is enhanced much less than the binding affinity, because the analog remains a good substrate for FAAH and is rapidly hydrolyzed by this enzyme. 2-Methyl-2’-fluoro AEA is further modified by the addition of an .alpha.-methyl group at the C-2 position of arachidonic acid. This substitution confers enhanced metabolic stability. 2-Methyl-2’-fluoro AEA can fully substitute for .DELTA.9-THC in animal self-administration tests, whereas AEA and 2-fluoro AEA cannot.
产品描述
An analog of AEA in which the alcohol of the ethanolamide group has been replaced with a fluorine atom, which increases the binding affinity and selectivity for the CB1 receptor; in vivo activity is enhanced much less than the binding affinity, because the analog is rapidly hydrolyzed by AEA; the addition of an α-methyl group at the C-2 position of arachidonic acid confers enhanced metabolic stability; can fully substitute for Δ9-THC in animal self-administration tests, whereas AEA and 2-fluoro AEA cannot