U-46619 is a stable analog of the endoperoxide PGH2, and a TP receptor agonist. It exhibits properties similar to TXA2, causing platelet shape change, aggregation, and contraction of vascular smooth muscle. Mean EC50 values for shape change in human, rat, and rabbit platelets are 4.8, 6.0, and 7.3 nM respectively, and for aggregation, are 82, 145, and 65 nM, respectively. U-46619 glycine methyl ester contains a modification at the C-1 position of U-46619 that may uniquely alter its binding properties to the TP receptor or any of the PGH2-metabolizing enzymes. As a stable PGH2 analog, it could therefore be a useful tool to explore the inhibition of various enzymes in the arachidonic acid metabolic pathway. U-46619 glycine methyl ester may also serve as a lipophilic prodrug form of U-46619 that will alter its distribution and pharmacokinetic properties. There are no published reports on the biological activity of U-46619 glycine methyl ester.
