Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis.1 It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation.1,2 PGD2 is also produced in the brain via a soluble, secreted PGD-synthase also known as β-trace.3,4 In the brain, PGD2 produces normal physiological sleep and lowering of body temperature.3,4 PGD2 methyl ester is a more lipid-soluble, cell-permeable prodrug form of PGD2.5 It binds to the human and murine PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2.6
1
Roberts, L.J., and Sweetman, B.J. Metabolic fate of endogenously synthesized prostaglandin D2 in a human female with mastocytosis. Prostaglandins30383-400(1985).
2
Giles, H., and Leff, P. The biology and pharmacology of PGD2. Prostaglandins35277-300(1988).
3
Hayaishi, O. Sleep-wake regulation by prostaglandins D2 and E2. J Biol Chem26314593-14596(1988).
4
Onoe, H., Ueno, R., Fujita, I., et al. Prostaglandin D2, a cerebral sleep-inducing substance in monkeys. Proc Natl Acad Sci USA854082-4086(1988).
5
Suzuki, F., Hayashi, H., Ito, S., et al. Methyl ester of prostaglandin D2 as a delivery system of prostaglandin D2 into brain. Biochem Biophys Acta917224-230(1987).
6
Hirai, H., Abe, H., Tanaka, K., et al. Gene structure and functional properties of mouse CRTH2, a prostaglandin D2 receptor. Biochem Biophys Res Commun307797-802(2003).
Roberts, L.J., and Sweetman, B.J. Metabolic fate of endogenously synthesized prostaglandin D2 in a human female with mastocytosis. Prostaglandins30383-400(1985).
Hayaishi, O. Sleep-wake regulation by prostaglandins D2 and E2. J Biol Chem26314593-14596(1988).
Giles, H., and Leff, P. The biology and pharmacology of PGD2. Prostaglandins35277-300(1988).
Onoe, H., Ueno, R., Fujita, I., et al. Prostaglandin D2, a cerebral sleep-inducing substance in monkeys. Proc Natl Acad Sci USA854082-4086(1988).
Hirai, H., Abe, H., Tanaka, K., et al. Gene structure and functional properties of mouse CRTH2, a prostaglandin D2 receptor. Biochem Biophys Res Commun307797-802(2003).
Suzuki, F., Hayashi, H., Ito, S., et al. Methyl ester of prostaglandin D2 as a delivery system of prostaglandin D2 into brain. Biochem Biophys Acta917224-230(1987).