U-46619 Glycine methyl ester

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.

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