Description
2-
Arachidonyl glycerol (2-
AG) exhibits cannabinoid agonist activity at the central cannabinoid (CB
1) receptor, is an important endogenous monoglyceride species, and is thus considered to be the natural ligand for the CB
1 receptor
1,2. 2-
AG can also be metabolized by COX-
2 to form prostaglandin (PG) 2-
glyceryl esters.
3 These 2-
glyceryl esters rapidly equilibrate to form 90:10 mixtures favoring the more stable 1-
glyceryl ester. 17-
phenyl trinor PGF
2α serinol amide is a stable analog of PGF
2α 2-
glyceryl ester incorporating an activity-
enhancing 17-
phenyl substitution. The biological activity of 17-
phenyl trinor PGF
2α serinol amide has not yet been determined.
References
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(4),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(2),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).