Description
Arachidonoyl ethanolamide (AEA; ) was the first endogenous cannabinoid (CB) to be isolated and characterized as an agonist acting on the same receptors (CB
1 and CB
2) as Δ
9-
THC . Since that time, a number of related endocannabinoids have been isolated, most notably 2-
arachidonoyl glycerol (2-
AG; ). The phosphate ester of AEA, AEA-
P, has been tested as a water soluble prodrug version of AEA in the treatment of C
6 glioma cells
in vivo. Here it acts with essentially the same potency as AEA. However, when tested for inhibition of AEA binding to isolated rat brain CB
1 receptors, AEA-
P is about 5-
fold less potent as an agonist with a K
i of about 200 nM. The phosphate esters of AEA and its analogs are also structural variants of lysophosphatidic acid (LPA). However, the effects of AEA-
P on the various LPA receptors have not been tested.
