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.

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

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.

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.

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

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

Ibudilast (MN-166)(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor. It is approved for use as an anti-inflammatory in Japan.

Proxyphylline (7-(2-Hydroxypropyl)theophylline) is a dual of adenosine A1 A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.

Trapidil (Avantrin) is a coronary vasodilator agent. It was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease.

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

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).

Moracin M, a phenolic compound found in the skin of Morus alba Linn., effectively inhibits phosphodiesterase-4 (PDE4), exhibiting IC50 values of 2.9 μM and 4.5 μM for PDE4D2 and PDE4B2, respectively, and showing significantly lesser activity on PDE5A1 and PDE9A2 with values over 40 μM and 100 μM, respectively. This compound demonstrates notable anti-inflammatory activity.

Robustine is a natural product, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro.

Norbraylin is a natural product from Toddalia asiatica.

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.

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.

WAY-313170 Inhibits hedgehog signaling and phosphodiesterase.

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

PDE-I2 is a parasite schizogony inhibitor.

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.