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Trequinsin is a phosphodiesterase (PDE) 3 inhibitor that is dependent on cyclic AMP (cAMP), with IC50 values of 0.04 and 0.03 nM for PDE3A and PDE3B, respectively, in T84 human colonic adenocarcinoma cell lysates.[1] In cultured primary rat juxtaglomerular cells, trequinsin stimulates cAMP accumulation when used at a concentration of 10 μM and increases cell membrane capacitance in a patch clamp assay.[2] Trequinsin also competitively inhibits the multidrug resistant protein 5-mediated export of cGMP from Chinese hamster lung fibroblasts with a Ki value of 240 nM.[3] In vivo, trequinsin reduces collagen-induced platelet aggregation in rabbits when administered intravenously at a rate of 3 μg/kg per minute, as well as the collagen-induced decrease in mean arterial blood pressure when administered alone or in combination with prostacyclin.[4]

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