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Overview
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Background
Iloprost is a second generation synthetic analog of prostacyclin derived from carbacyclin, exhibiting approximately 10-fold greater potency than the first generation stable analogs of prostacyclin, represented by carbacyclin. Iloprost binds with high affinity to the prostanoid receptors, with Ki values being 11, 11 and 56 nM for the human recombinant IP, EP1 and EP3 receptors, respectively. Prostacyclin is a prostaglandin member of the eicosanoid family of lipid molecules, which inhibits platelet activation and dilates blood vessels through interaction with G-protein-coupled prostanoid receptors.
1. Schrör K, Darius H, Matzky R, et al. The antiplatelet and cardiovascular actions of a new carbacyclin derivative (ZK 36 374)--equipotent to PGI2 in vitro. Naunyn-Schmiedeberg's Archives of Pharmacology, 1981, 316(3): 252-255.
2. Abramovitz M, Adam M, Boie Y, et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochimica et Biophysica Acta, 2000, 1483(2): 285-293.
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