Dipyridamole-d16

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 K_i 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)