2-arachidonyl glycerol (2-AG) exhibits cannabinoid (CB) agonist activity at the CB1 receptor,1 is an important endogenous monoglyceride species,2 and is thus considered to be the natural ligand for the CB1 receptor. 2-AG can also be metabolized by cyclooxygenase-2 and specific prostaglandin H2 (PGH2) isomerases to form PG 2-glyceryl esters.3 Fluprostenol serinol amide (Flu-SA) is a stable analog of PGF2α 2-glyceryl ester that has much greater stability. The biological activity of Flu-SA has not yet been determined.
1
Sugiura, T., Kodaka, T., Kondo, S., et al. Is the cannabinoid CB1 receptor a 2-arachidonoylglycerol receptor? Structural requirements for triggering a Ca2+ transient in NG108-15 cells. J Biochem 122 890-895 (1997).
2
Kondo, S., Kondo, H., Nakane, S., et al. 2-Arachidonoylglycerol, an endogenous cannabinoid receptor agonist: Identification as one of the major species of monoacylglycerols in various rat tissues, and evidence for its generation through Ca2+-dependent and -independent mechanisms. FEBS Lett 429 152-156 (1998).
3
Kozak, K.R., Crews, B.C., Morrow, J.D., et al. Metabolism of the endocannabinoids, 2-arachidonylgycerol and anandamide, into prostaglandin, thromboxane, and prostacyclin glycerol esters and ethanolamides. J Biol Chem 277(47) 44877-44885 (2002).