A neuropeptide with diverse biological activities
Dipyridamole-d16 is intended for use as an internal standard for the quantification of dipyridamole by GC- or LC-MS. Dipyridamole is a phosphodiesterase 5A (PDE5A) inhibitor (IC50 = 574 nM) that prevents platelet aggregation by increasing cGMP levels and blocking the reuptake of adenosine via red blood cells.1,2 It also scavenges the free radicals that inactivate cyclooxygenase, leading to the inhibition of platelet activation and thrombin generation.1 Dipyridamole has also been shown to inhibit PDE11A with an IC50 value of 370 nM and equilibrative nucleoside transporter 1 (ENT1) with a Ki value of 8.18 nM.3,4 Formulations containing dipyridamole in combination with aspirin have been used to prevent stroke and other cardiovascular events.
1.Rondina, M.T., and Weyrich, A.S.Targeting phosphodiesterases in anti-platelet therapyAntiplatelet Agents. Handbook of Experimental Pharmacology210225-238(2012) 2.Watanabe, N., Adachi, H., Takase, Y., et al.4-(3-Chloro-4-methoxybenzyl)aminophthalazines: Synthesis and inhibitory activity toward phosphodiesterase 5J. Med. Chem.43(13)2523-2529(2000) 3.Fawcett, L., Baxendale, R., Stacey, P., et al.Molecular cloning and characterization of a distinct human phosphodiesterase gene family: PDE11AProc. Natl. Acad. Sci. USA97(7)3702-3707(2000) 4.Lin, W., and Buolamwini, J.K.Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitorsJ. Med. Chem.50(16)3906-3920(2007)
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