Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
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Prostaglandins such as prostacy-clin elicit their molecular, pharmacological and biochemical effects through binding and activation of specific receptor sites. The prostanoid receptors are identified as the IP, EP1, EP2, EP3, EP4, DP (now DP1), FP and TP receptor. The IP, EP2, EP4 and DP1 receptors are classically known to be Gs-coupled receptors linked to cyclic AMP (cAMP) generation. Treprostinil sodium is a highly potent DP1 and EP2 agonist with EC50 values of 0.6 ± 0.1 and 6.2 ± 1.2 nM, respectively. Treprostinil had high affinity for the DP1, EP2 and IP receptors with Ki values of 4.4, 3.6 and 32 nM, respectively, low affinity for EP1 and EP4 receptors and even lower affinity for EP3, FP and TP receptors[3]. 10 μM treprostinil inhibited ECFC (endothelial colony forming cells) proliferation in media containing either high or low serum concentrations. Treprostinil significantly stimulated ECFC+MSC (mesenchymal stem cells) induced vessel formation with a significant increase of microvessel density[4].
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