pde

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.

Pentoxifylline (PTX) modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It also inhibits platelet aggregation and improves blood flow by increasing erythrocyte and leukocyte flexibility.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

Vinpocetine (RGH-4405) is a selective inhibitor of cyclic GMP phosphodiesterase (PDE).

Dipyridamole (Persantin) is a Platelet Aggregation Inhibitor. The physiologic effect of dipyridamole is by means of Decreased Platelet Aggregation.

Doxofylline (Doxophylline) is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has shown similar efficacy to theophylline but with significantly fewer side effects in animal and human studies.

Norbraylin is a natural product from Toddalia asiatica.

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

Tiflucarbine is a potential non-selective 5-HT agonist with antidepressant activity.Tiflucarbine dose-dependently increased the specific activity of soluble calmodulin (CaM)-dependent phosphodiesterase in rat brain.

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.

WAY-313170 Inhibits hedgehog signaling and phosphodiesterase.

5-Bromoimidazo[1,2-a]pyrazine inhibits phosphodiesterase and beta-adrenergic receptors.5-Bromoimidazo[1,2-a]pyrazine shows antibronchospastic activity in vitro.

PDE-I2 is a parasite schizogony inhibitor.

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

PDE9-IN-(S)-C33 ((S)-C33) is a potent and selective inhibitor of PDE9 (IC50 = 11 nM). PDE9-IN-(S)-C33 can be used for central nervous system diseases and diabetes research.

PDE7-IN-2 is an inhibitor of phosphodiesterase 7 (IC50 = 2.1 µM) and can be used in Parkinson's disease studies.

PDE9-IN-1 is a selective and orally bioavailable Inhibitor of PDE9A(IC50 of 8.7 nM).

PDE4B-IN-2 (A 33) is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.

PDE10-IN-1 (SEP-0372814) is used for treating CNS and metabolic disorders.

K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ that binds to the farnesyl binding pocket of PDEδ (Kd of 8 nM).

PDE5-IN-9 inhibits Phosphodiesterase PDE1c and is used to treat hypertension, heart failure, myocardial infarction, kidney failure, asthma, bronchitis, and dementia.

PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5 (IC50 of 0.31 nM).

Lanopepden (GSK 1322322) is a potent peptide deformylase inhibitor effective against Staphylococcus aureus strains ATCC 29213 and ATCC 25923, and is applicable in the study of pneumonia, dermatological, and infectious diseases.

Lanopepden mesylate is a peptide deformylase inhibitor against Staphylococcus aureus.