pde iii

OR-1896 is the active metabolite of Levosimendan, a highly specific phosphodiesterase (PDE III) inhibitor, a vasodilator with partial anti-inflammatory properties that produces vasodilation in different types of blood vessels through activation of ATP-sensitive (KATP) and other potassium channels.OR-1896 can be used to study heart failure and vascular dysfunction. OR-1896 can be used to study heart failure and vascular dysfunction.

Senazodan is a sensitiser of Ca2+, and shows inhibition effect on PDE III.

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM. Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM.

EMD57439 is a selective PDE-III inhibitor, showing no significant increase in c-AMP concentration and producing little change in Ca(50).

Saterinone is a potent and selective phosphodiesterase III inhibitor and a potent antagonist of the vascular α-1-adrenoceptor. Saterinone has vasodilatory properties and can be used in the acute treatment of chronic heart failure. Saterinone inhibited crude cAMP phosphodiesterase (PDE) activity in guinea pig right ventricular homogenates The ic50 value is 2.3 × 10(-5) mol l.

Dazonone (Imidazo[2,1-b]quinazolin-2(3H)-one, 6-chloro-1,5-dihydro-3-methyl-) is a specific PDE III inhibitors.

RS 25344 hydrochloride is a phosphodiesterase (PDE) 4 inhibitor

Saterinone hydrochloride is an inhibitor of phosphodiesterase III (PDE III).

Win-62005 is an inhibitor of cyclic AMP phosphodiesterase III (PDE III)(Kis: 25 and 26 nM for rat heart and canine aorta).

Zardaverine (BY 290) is an orally available, selective and potent PDE3 4 inhibitor with bronchodilator activity and anti-hepatocarcinogenic activity.Zardaverine's action in platelets is mediated by PDE III isoenzymes and can be used in studies of acute renal failure and chronic airflow obstruction.

CI-930 is a PDE-III inhibitor with broad-spectrum activity. It exerts its anti-aggregation effects through a dual mechanism: enhancing cAMP levels and selectively inhibiting the synthesis of TXA2 in platelets. CI-930 effectively inhibits platelet aggregation induced by AA, U-46619, ADP, collagen, and PAF, with IC50 values of 0.91, 0.73, 2.12, 2.35, and 7.15 mumols L, respectively.

8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA) and a potent inhibitor of cyclic GMP-specific phosphodiesterase (PDE VA) with an inhibitory concentration (IC50) of 0.9 μM. It also inhibits PDE III and PDE IV while significantly activating Epac, demonstrating diverse pharmacological activities [1] [2].

ORM-3819 is a potent and selective PDE III inhibitor. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization.

Enoximone sulfoxide is a selective phosphodiesterase III (PDE3) inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. Enoximone prevents the degradation of cAMP by PDE, which prolongs signal transduction and its subsequent effects. It is used in patients with congestive heart failure.

Enoximone is a selective inhibitor of phosphodiesterase III (PDE3), with treatment of congestive heart failure.