phosphodiesterase inhibitor

Enprofylline (Enprofilina), a bronchodilator, acts primarily as a competitive nonselective phosphodiesterase inhibitor. Enprofylline is used in asthma, chronic obstructive pulmonary disease, and in the management of sickle cell disease, diabetic neuropathy, and cerebrovascular insufficiency.

Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.

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.

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

PDE IV-IN-1 is a potent phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory activity for the treatment of asthma, chronic obstructive pulmonary disease and other inflammatory diseases, and is a potential compound for the study of depression.

CM-675 is a dual inhibitor of phosphodiesterase 5 (PDE5) and class I histone deacetylases (IC50s: 114 nM and 673 nM for PDE5 and HDAC1) with the potential to treat Alzheimer's disease.

UK 227786 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.

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.

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.

WAY127093B racemate is the racemic mixture of WAY127093B, a phosphodiesterase IV inhibitor with demonstrated oral activity in rats and guinea pigs.

Gisadenafil (UK-369003), a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM, prevents the degradation of cGMP.

Oglemilast (GRC 3886) suppresses pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast is an effective and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 0.5 nM for PDE4D3). Oglemilast has the potential for inflammatory airway diseases.

PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50>1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.

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].

BC 11-38 is a potent, selective PDE biodepressant which is mainly effective against PDE11 (IC50 : 0.28 μM).

inhibitor of phosphodiesterase type 5 (PDE5).This compound is unstable in powder form and other related salt forms are recommended.

T-0156 is a novel, potent and selective phosphodiesterase type 5 inhibitor that inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) with low affinity for PDE6, PDE1, PDE2, PDE3 and PDE4.

Mopidamol (RA 233) is a phosphodiesterase inhibitor, a dipyridamole derivative, with anticancer activity that prevents retinal vascular defects in experimental diabetes.

Dasantafil (SCH446132) is a small molecule phosphodiesterase-5A (PDE5A) inhibitor used to treat genitourinary disorders and study erectile dysfunction.

HT-0712 is a phosphodiesterase 4 (PDE4) inhibitor.

Imazodan hydrochloride (CI-914 HCl) is a potent and selective type III phosphodiesterase inhibitor used in the treatment of chronic congestive heart failure.