Dipyridamole

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 It inhibits replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero E6 cells when used at a concentration of 100 nM.⁵ Formulations containing dipyridamole in combination with aspirin (Item No. 70260) have been used to prevent stroke and other cardiovascular events.⁶

WARNING This product is not for human or veterinary use.

1. Rondina, M.T., and Weyrich, A.S. Targeting phosphodiesterases in anti-platelet therapy. Antiplatelet Agents. Handbook of Experimental Pharmacology 210, 225-238 (2012).

2. Watanabe, N., Adachi, H., Takase, Y., et al. 4-(3-Chloro-4-methoxybenzyl)aminophthalazines: Synthesis and inhibitory activity toward phosphodiesterase 5. J. 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: PDE11A. Proc. Natl. Acad. Sci. USA 97(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 inhibitors. J. Med. Chem. 50(16), 3906-3920 (2007).

5. Liu, X., Li, Z., Liu, S., et al. Potential therapeutic effects of dipyridamole in the severely Ill patients with COVID-19. Acta. Pharm. Sin. B (2020).

6. Coccheri, S. Antiplatelet drugs - do we need new options? Drugs 70(7), 887-908 (2010).

Nam, G.S., Kim, S., Kwon, Y.-S., et al. A new function for MAP4K4 inhibitors during platelet aggregation and platelet-mediated clot retraction. Biochem. Pharmacol. 188, 114519 (2021).