Phosphodiesterase inhibitors. Medical search. FAQ

Inhibition of cyclic nucleotide phosphodiesterase can be used to affect vasodilation. (fpnotebook.com)
Ibudilast , a neuroprotective and bronchodilator drug used mainly in the treatment of asthma and stroke, inhibits PDE-4 to the greatest extent, but also shows significant inhibition of other PDE subtypes, and so can be viewed either as a selective PDE-4 inhibitor or a non-selective phosphodiesterase inhibitor depending on the dose used. (wikidoc.org)
Weiss, B.: Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase. (wikidoc.org)
Is phosphodiesterase inhibition a new mechanism of antidepressant action? (wikidoc.org)
It inhibits PDE4 to the greatest extent, but also shows significant inhibition of other PDE subtypes, and so acts as a selective PDE4 inhibitor or a non-selective phosphodiesterase inhibitor, depending on the dose. (wikipedia.org)
Phosphodiesterase 4 (PDE4) inhibition restores the suppressive effects of 3′,5′-cyclic adenosine monophosphate in lymphocytes. (bloodjournal.org)
PDE4D inhibition, along with PDE4A inhibition also appears to be responsible for the antidepressant effects of PDE4 inhibitors. (wikipedia.org)
Similarly PDE4B inhibition appears to be required for the antipsychotic effects of PDE4 inhibitors, in line with this view PDE4B polymorphisms and altered gene expression in the central nervous system have been associated with schizophrenia and bipolar disorder in a postmortem study. (wikipedia.org)
The clinical development of PDE4 inhibitors has been hampered by their potent emetic effects, which appear to be related to their inhibition of PDE4D which is expressed in the area postrema. (wikipedia.org)
Phosphodiesterase enzymes are often targets for pharmacological inhibition due to their unique tissue distribution, structural properties, and functional properties. (wikipedia.org)
Inhibitors of PDE can prolong or enhance the effects of physiological processes mediated by cAMP or cGMP by inhibition of their degradation by PDE. (wikipedia.org)

A preliminary observational study by the investigators has shown that tadalafil, a selective phosphodiesterase-5 inhibitor (PDE-5) decreases pulmonary vascular resistance(PVR) in patients of eisenmenger syndrome (ES) resulting in increase in pulmonary blood flow (Qp), systemic oxygen saturation (SaO2), functional class and exercise capacity. (clinicaltrials.gov)
Mukhopadhyay S, Nathani S, Yusuf J, Shrimal D, Tyagi S. Clinical efficacy of phosphodiesterase-5 inhibitor tadalafil in Eisenmenger syndrome--a randomized, placebo-controlled, double-blind crossover study. (clinicaltrials.gov)
Previously, through the use of an extensive screening process, we found that vardenafil, a phosphodiesterase 5 (PDE-5) inhibitor significantly reverses MDR in ABCB1 overexpressing cancer cells, and its efficacy was greater than that of tadalafil, another PDE-5 inhibitor. (nih.gov)

6. The method of claim 5, wherein the Type V phosphodiesterase is sildenafil or a pharmaceutically acceptable salt thereof. (google.com.au)
Sildenafil (Viagra) is an inhibitor of cGMP-specific phosphodiesterase type 5, which enhances the vasodilatory effects of cGMP in the corpus cavernosum and is used to treat erectile dysfunction. (wikipedia.org)
citation needed] Sildenafil are PDE V inhibitors and are widely used in the treatment of erectile dysfunction. (wikipedia.org)
Those using protease inhibitors are recommended to limit their use of sildenafil to no more than one 25 mg dose every 48 hours. (wikipedia.org)

Usually, this refers to cyclic nucleotide phosphodiesterase, an enzyme that breaks the phosphodiester bond in the second messenger molecules cAMP and cGMP. (fpnotebook.com)
Usually, phosphodiesterase refers to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. (wikipedia.org)

A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), therefore preventing the inactivation of the intracellular second messengers , cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), by the respective PDE subtype(s). (wikidoc.org)
2 , 3 The therapeutic utility of controlling the intracellular levels of cyclic-AMP, and of cyclic guanosine monophosphate (cyclic-GMP), with PDE inhibitors is well established. (bloodjournal.org)

It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. (wikipedia.org)
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor. (wikipedia.org)

It also acts as an adenosine reuptake inhibitor. (wikipedia.org)

The potential for selective phosphodisterase inhibitors to be used as therapeutic agents was predicted as early as 1977 by Weiss and Hait. (wikidoc.org)
The potential for selective phosphodiesterase inhibitors to be used as therapeutic agents was predicted in the 1970s. (wikipedia.org)

The action of phosphodiesterase inhibitor may lead to an increase in the level of cAMP and opening of the calcium channel on the surface of the cell. (medicalzone.net)

Piclamilast, a more potent inhibitor than rolipram. (wikipedia.org)

This project aims to unite global efforts to target the highly druggable class of enzymes called cyclic nucleotide phosphodiesterases (PDEs) in the fight for neglected parasitic diseases (NPD). (europa.eu)
1 The synthesis and degradation of cyclic-AMP are tightly controlled by 2 classes of enzymes, adenylyl cyclases and phosphodiesterases (PDEs), respectively. (bloodjournal.org)
The published specification DE 28 11 780 describes imidazotriazinones as bronchodilators having spasmolytic activity and inhibitory activity against phosphodiesterases which metabolize cyclic adenosin monophosphate (cAMP-PDEs, nomenclature according to Beavo: PDE-III and PDE-IV). (patentsencyclopedia.com)
An inhibitory action against phosphodiesterases which metabolize cyclic guanosin monophosphate (cGMP-PDEs, nomenclature according to Beavo and Reifsnyder (Trends in Pharmacol. (patentsencyclopedia.com)
The compounds according to the invention are potent inhibitors either of one or of more of the phosphodiesterases which metabolize cyclic guanosin 3',5'-monophosphate (cGMP-PDEs). (patentsencyclopedia.com)
Phosphodiesterases (PDEs) are a superfamily of enzymes. (wikipedia.org)

The human genome contains at least 21 genes involved in determining the intracellular levels of cAMP and cGMP by the expression of phosphodiesterase proteins or PDE's. (wikipedia.org)
The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. (wikipedia.org)

In the decade of the '70s, various PDE isoenzymes were defined which led to the development of the second generation of PDE inhibitors. (textbookx.com)
During the past five years, molecular biology has revealed a superfamily of these phosphodiesterase isoenzymes. (textbookx.com)
Primary sequences of cyclic nucleotide phosphodiesterase isoenzymes and the design of selective inhibitors. (springer.com)
11, 150-155, 1990) these are the phosphodiesterase isoenzymes PDE-I, PDE-II and PDE-V. An increase of the cGMP concentration can lead to beneficial antiaggregatory, antithrombotic, antiprolific, antivasospastic, vasodilative, natriuretic and diuretic effects. (patentsencyclopedia.com)

PDE1 (phosphodiesterase type 1) is a phosphodiesterase enzyme also known as calcium- and calmodulin-dependent phosphodiesterase. (wikipedia.org)

Any substance that inhibits phosphodiesterase, an enzyme that catalyzes the breaking of a phosphodiester bond. (fpnotebook.com)
citation needed] Zaprinast inhibits the growth of asexual blood-stage malaria parasites (P. falciparum) in vitro with an ED50 value of 35 μM, and inhibits PfPDE1, a P. falciparum cGMP-specific phosphodiesterase, with an IC50 value of 3.8 μM. (wikipedia.org)

1. A method for treating erectile dysfunction in a male individual, comprising locally administering to the individual an effective amount of a pharmaceutical composition consisting essentially of a Type V, cGMP-specific phosphodiesterase inhibitor or a pharmaceutically acceptable salt, ester, amide or prodrug thereof. (google.com.au)
18. A pharmaceutical formulation for treating erectile dysfunction in an individual, comprising a urethral dosage form of a phosphodiesterase inhibitor, a carrier suitable for transurethral drug administration, and, optionally, a transurethral permeation enhancer, wherein the phosphodiesterase inhibitor is a Type V, cGMP-specific phosphodiesterase inhibitor, or a pharmaceutically acceptable salt ester, amide or prodrug thereof. (google.com.au)
Given that phototransduction relies on the hydrolysis of cGMP via phosphodiesterase 6 (PDE6), we examined ROS growth and shedding in zebrafish treated with cGMP-specific PDE inhibitors. (arvojournals.org)

Patients on treatment with prostanoids, endothelial receptor antagonists (ERA), PDE-5 inhibitors or any other vasodilators with in 1month prior to screening were excluded. (clinicaltrials.gov)
particularly the underuse of ACE inhibitors and β-blockers and aldosterone antagonists which have been shown to provide mortality benefit. (wikipedia.org)

Phosphodiesterase inhibitor is useful in treating patient due to exacerbation of the congestive cardiac failure or acute cardiac failure. (medicalzone.net)

Non-selective inhibitors of cyclic nucleotide phosphodiesterase (PDE), such as theophylline, have been used extensively since 1958. (textbookx.com)
Bronchodilatory substances such as the phosphodisterase inhibitor (PDE-I) theophylline stimulate mucociliary activity. (lu.se)

Enoximone (INN, trade name Perfan) is an imidazole phosphodiesterase inhibitor. (wikipedia.org)

A phosphodiesterase (PDE) is an enzyme that breaks a phosphodiester bond. (wikipedia.org)

Uzunov, P. and Weiss, B.: Separation of multiple molecular forms of cyclic adenosine 3',5'-monophosphate phosphodiesterase in rat cerebellum by polyacrylamide gel electrophoresis. (wikidoc.org)

Effect of cilostazol, a cyclic AMP phosphodiesterase inhibitor, on the proliferation of rat aortic smooth muscle cells in culture. (sigmaaldrich.com)

It is a potent (IC50 = 36nM) inhibitor of phosphodiesterase-II. (wikipedia.org)

Currently a variety of these new inhibitors are under test as potential anti-inflammatory drugs. (textbookx.com)
Recent studies have shown Quinazoline type PDE7 inhibitor to be potent anti-inflammatory and neuroprotective agents. (wikipedia.org)
Selective phosphodiesterase-4 inhibitors increase cyclic adenosine-3′,5′-monophosphate (cAMP) levels, resulting in a broad spectrum of anti-inflammatory effects in almost all inflammatory cells. (drugs.com)

Cilostazol, a cyclic AMP phosphodiesterase inhibitor, has been used as an antiplatelet agent. (sigmaaldrich.com)
Phosphodiesterase inhibitor with antiplatelet activity. (wikipedia.org)

Al-Alaiyan S, Al-Omran A, Dyer D. The use of phosphodiesterase inhibitor (dipyridamole) to wean from inhaled nitric oxide. (springer.com)

Weiss, B. and Hait, W.N.: Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents. (wikidoc.org)
The results of these studies support the pharmacological validation of the Trypanosome PDEB family as novel therapeutic approach for HAT and provide valuable information for the design of potent TbrPDEB1 inhibitors that could be used for the treatment of this disease. (dndi.org)
Preclinical Characterization of Selective Phosphodiesterase 10A Inhibitors: a New Therapeutic Approach to the Treatment of Schizophrenia" (PDF). (wikipedia.org)

However, the phosphodiesterase inhibitor may carries its own side effects such as cardiac arrhythmias, nausea, vomiting and thrombocytopenia. (medicalzone.net)
Aminophylline causes bronchodilation, diuresis†, central nervous system and cardiac stimulation, and gastric acid secretion by blocking phosphodiesterase which increases tissue concentrations of cyclic adenosine monophosphate (cAMP) which in turn promotes catecholamine stimulation of lipolysis, glycogenolysis, and gluconeogenesis, and induces release of epinephrine from adrenal medulla cells. (wikipedia.org)

These phosphodiesterase inhibitors are used primarily as remedies for erectile dysfunction , as well as having some other medical applications such as treatment of pulmonary hypertension . (wikidoc.org)
Preliminary studies show that phosphodiesterase inhibitors can be beneficial for purposes other than treating erectile dysfunction. (diabetesincontrol.com)

The method involves the local administration of a phosphodiesterase inhibitor or a pharmaceutically acceptable salt, ester, amide or derivative thereof within the context of an effective dosing regimen. (google.com.au)

It is one of the 11 families of phosphodiesterase (PDE1-PDE11). (wikipedia.org)

The team's goal was to establish if the use of phosphodiesterase inhibitors in men with type 2 diabetes increased mortality. (diabetesincontrol.com)
More research is needed in this area to support the use of phosphodiesterase inhibitors in type 2 diabetic men for its increased mortality benefit. (diabetesincontrol.com)
Phosphodiesterase inhibitors may have a mortality benefit for type 2 diabetic men. (diabetesincontrol.com)
Phosphodiesterase type-5 inhibitor use in type 2 diabetes is associated with a reduction in all-cause mortality. (diabetesincontrol.com)
2. The method of claim 1, wherein the phosphodiesterase inhibitor is a Type V phosphodiesterase inhibitor. (google.com.au)
4. The method of claim 3, wherein the Type V phosphodiesterase inhibitor is zaprinast. (google.com.au)
5. The method of claim 3, wherein the Type V phosphodiesterase is a pyrazolopyrimidinone. (google.com.au)
Roflumilast, type 4 phosphodiesterase inhibitor, attenuates inflammation in rats with ulcerative. (deepdyve.com)
BAY 60-7550 is a type 2 phosphodiesterase inhibitor. (wikipedia.org)

Selective phosphodiesterase-4 inhibitors are used in the treatment of severe Chronic Obstructive Pulmonary Disease ( COPD ) to reduce the risk of COPD exacerbations. (drugs.com)
It is used in the treatment of congestive heart failure and is selective for phosphodiesterase 3. (wikipedia.org)

any substance or agent which suppresses, prevents or opposes the actions or biosynthesis of phosphodiesterases. (fpnotebook.com)

The phosphodiesterase inhibitors available for use included Viagra, Cialis, and Levitra. (diabetesincontrol.com)

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