phosphodiesterase 3

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

Phosphodiesterase-IN-3 (Example 20) is an inhibitor of phosphodiesterase 4B, with IC50 values for PDE4B1 and PDE4D3 of less than 10 nM and between 10-100 nM, respectively. Phosphodiesterase-IN-3 shows potential for research in idiopathic pulmonary fibrosis.

IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5/26.3/31.7 μM). IBMX enhances the intracellular cAMP level.

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

Sp-cAMPS sodium salt is an analog of cAMP that serves as a potent activator of cAMP-dependent PKA I and PKA II, and as a competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 μM. It also binds the PDE10 GAF domain with an EC50 of 40 μM [1] [2] [3].

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

Parogrelil Free Base (NM-702 Free Base) is a selective phosphodiesterase 3 inhibitor with bronchodilatory and anti-inflammatory effects, inhibits leukotriene (LT)D(4) and histamine-induced constriction of isolated guinea pig tracheal strips, and can be used in the study of bronchial asthma.

Anagrelide (Xagrid) is a Platelet-reducing Agent. The mechanism of action of anagrelide is as a Phosphodiesterase 3 Inhibitor. The physiologic effect of anagrelide is by means of Decreased Platelet Production.

Cilostazol (OPC 21) is a Phosphodiesterase 3 Inhibitor. The mechanism of action of cilostazol is as a Phosphodiesterase 3 Inhibitor.

Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.

Milrinone (Win 47203) is a Phosphodiesterase 3 Inhibitor. The mechanism of action of milrinone is as a Phosphodiesterase 3 Inhibitor.

Amrinone (Inocor) is a positive inotropic cardiotonic (cardiotonic agent) with vasodilator properties, phosphodiesterase 3 inhibitory activity.

Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor,and is an antispasmodic drug, used to enhance cervical dilation during childbirth. Drotaverine hydrochloride is structurally related to papaverine

VP3.15 dihydrobromide is a potent, orally bioavailable, and CNS-penetrant dual inhibitor of phosphodiesterase (PDE7) and glycogen synthase kinase (GSK)3, with IC50 values of 1.59 μM and 0.88 μM, respectively.

ATX inhibitor 1 is a potent ATX inhibitor with IC50 values of 1.23 nM (FS-3) and 2.18 nM (bis-pNPP).

Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist with a Kd of 3 nM, which inhibits CaM-dependent phosphodiesterase (IC50 = 0.15 μM) and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase (IC50 = 0.35 μM). It also induces apoptosis in certain cancer cell lines.

Milrinone Lactate is a positive inotropic cardiotonic compound. Milrinone Lactate has vasodilator properties, inhibiting cAMP phosphodiesterase type 3 activity in the myocardium and vascular smooth muscle.

NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3).

PDE1-IN-3 is a selective inhibitor of human phosphodiesterase 1 (PDE1).

PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.

Prinoxodan is a potent phosphodiesterase 3 (PDE3) inhibitor. It exerts cardiotonic and vasodilatory effects by increasing intracellular cAMP levels, used for heart failure and cardiovascular research.

VP3.15 is an orally bioavailable and CNS-penetrant dual inhibitor of phosphodiesterase (PDE)7- GSK3 (IC50s: 1.59 μM and 0.88 μM for PDE7 and GSK-3).

K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 μM, respectively.

LAS-31180 is a phosphodiesterase 3 inhibitor. It also has positive inotropic and vasodilator properties.