Vesnarinone inhibits nucleoside and nucleobase transport

Abstract Vesnarinone is a novel synthetic oral inotropic agent that has been successfully used for treatment of patients with congestive heart failure. In addition to its cardiotonic activity, the drug has been proposed to have mild cytostatic and anti-HIV-1 effects. We have observed that vesnarinone profoundly inhibits radiolabeled thymidine and uridine incorporation into cells despite its modest inhibitory effect on DNA synthesis, RNA synthesis or cell proliferation. Here we demonstrate that vesnarinone inhibits both nucleoside and nucleobase transport in mammalian cells. This pharmacological action may be involved in some of its multiple biological effects. Key Wonts: nucleoside transport, nucleobase transport, inotropic agent, anti-tumor effect, HIV-1