2'-Fluoro aea

Description

Arachidonoyl-2'-fluoroethylamide (2-fluoro AEA) is an analog of anandamide in which the alcohol of the ethanolamide group has been removed and replaced with a fluorine atom. This substitution adds considerably increased binding affinity for the CB₁ receptor (K_is = 26.7 and 908 nM for CB₁ and CB₂, respectively). It also contributes additional selectivity, in that binding to CB₂ is decreased relative to AEA.¹ 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.

The Uses of 2'-Fluoro aea

Arachidonoyl-2'-fluoroethylamide is a CB1 receptor agonist and an analog of Anandamide (A637220), which is an endogenous cannabinoid and TRPV1 receptor agonist.

What are the applications of Application

Arachidonoyl 2′-fluoroethylamide is a CB1 receptor agonist

References

1. Lin, S., Khanolkar, A.D., Fan, P., et al. Novel analogues of arachidonylethanolamide (anandamide): Affinities for the CB₁ and CB₂ cannabinoid receptors and metabolic stability J. Med. Chem. 41(27),5353-5361(1998).