U-46619 Glycine methyl ester

A stable analog of the endoperoxide PGH2, and a TP receptor agonist. 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. 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 be a useful tool to explore the inhibition of various enzymes in the arachidonic acid metabolic pathway. Also may serve as a lipophilic prodrug form of U-46619 that will alter its distribution and pharmacokinetic properties.

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