Phosphodiesterase inhibitors. Medical search. FAQ

The effects of non-selective and selective phosphodiesterase (PDE) inhibitors on membrane activity and synaptic plasticity of MSNs will also be reviewed. (ox.ac.uk)

Review: Modulation of striatal neuron activity by cyclic nucleotide signaling and phosphodiesterase inhibition. (ox.ac.uk)

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)
PDE4 inhibitors have proven potential as anti-inflammatory drugs, especially in inflammatory pulmonary diseases such as asthma, COPD, and rhinitis. (wikipedia.org)
PDE4 inhibitors may have antidepressive effects and have also recently been proposed for use as antipsychotics. (wikipedia.org)
Treatment with a PDE4 inhibitor raised the deficient cAMP levels and restored some functionality to Hippocampus-based memory functions. (wikipedia.org)
Inhibitors of phosphodiesterase type 4 (PDE4) act by increasing intracellular concentrations of cyclic AMP, which has a broad range of anti-inflammatory effects on various key effector cells involved in asthma and chronic obstructive pulmonary disease (COPD). (nih.gov)
The therapeutic ratio for PDE4 inhibitors is thought to be determined by selectivity on receptor subtypes for relative effects on PDE4B (anti-inflammatory) and PDE4D (emesis). (nih.gov)
The emerging results of clinical trials on PDE4 inhibitors in asthma and COPD should be interpreted with cautious optimism since much of the evidence has been published only in abstract form to date. (nih.gov)
Ultimately, clinicians will want to know whether PDE4 inhibitors are anything more than expensive "designer" theophylline, the archetypal non-selective phosphodiesterase inhibitor. (nih.gov)
PDE4 inhibitors have proven potential as anti-inflammatory drugs especially in airway diseases. (wikidoc.org)
PDE4 inhibitors have a high therapeutic and commercial potential as non-steroidal disease controllers in inflammatory airway diseases such as asthma, COPD and rhinitis. (wikidoc.org)
PDE4 inhibitors may have an antidepressant action and have also recently been proposed for use as antipsychotic medications. (wikidoc.org)
Phosphodiesterase 4 (PDE4) inhibition restores the suppressive effects of 3′,5′-cyclic adenosine monophosphate in lymphocytes. (bloodjournal.org)
We describe the successful clinical repurposing of PDE4 inhibitors in B-cell malignancies, and propose that given their anti-inflammatory/immunomodulatory activity, these agents will suppress BCR signals without the toxicity associated with other targeted biological doublets. (bloodjournal.org)
Here, we review a decade-long exploration of the contribution of cyclic-AMP and PDE4 to the pathogenesis of B-cell lymphoma, 5 ⇓ ⇓ ⇓ - 9 culminating with the first-in-cancer clinical trial of a PDE4 inhibitor in advanced B-cell malignancies. (bloodjournal.org)
The inhaled PDE4 inhibitor showed a larger reduction of moderate to severe exacerbations in a subgroup of patients with chronic bronchitis. (pharmaceutical-technology.com)
With little low-hanging fruit remaining, therapies with novel mechanisms of actions are highly prized, therefore, when the inhaled phosphodiesterase-4 inhibitor (PDE4) CHF6001, demonstrated its marked effect on inflammatory biomarkers, it attracted much attention at the 2019 European Respiratory Society (ERS) congress in Madrid. (pharmaceutical-technology.com)
Pharmacological treatment centres essentially around short-acting bronchodilators for patients in low risk categories through long-acting bronchodilators and inhaled corticosteroids to most recently, add-on therapy with the phosphodiesterase-4 (PDE4) inhibitor roflumilast . (smw.ch)
The effects of repeated treatment with the phosphodiesterase-4 (PDE4) inhibitors rolipram, piclamilast, and 4-(2-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-phenylethyl)pyridine (CDP840), which differ in their interactions with high- and low-affinity binding conformers of the enzyme, were contrasted to those of acute treatment on cAMP signaling, hippocampal cell proliferation, and immobility in the forced-swim test in rats. (aspetjournals.org)
In addition, repeated treatment with the PDE4 inhibitors increased proliferation and survival of newborn cells in the hippocampus and produced antidepressant-like effects on behavior, as evidenced by decreased immobility in the forced-swim test. (aspetjournals.org)
El-Adawy, Samar A. 2018-03-01 00:00:00 BackgroundRoflumilast (Rof), a phosphodiesterase 4 (PDE4) inhibitor, has been shown to be an effective agent in inflammatory diseases and marketed for chronic obstructive pulmonary disease. (deepdyve.com)
3. The PDE1/PDE5 inhibitor zaprinast inhibited both cyclic AMP and cyclic GMP PDE activity in both pellet and supernatant fractions of cell homogenates by a maximum of around 25% (IC(50) 1 - 5 microM), while rolipram (PDE4 selective) inhibited only cyclic AMP hydrolysis. (strath.ac.uk)
Selective PDE4 inhibitors as potent anti-inflammatory drugs for the treatment of airway diseases. (semanticscholar.org)
Highly selective PDE4 inhibitors are currently under evaluation for the treatment of asthma and/or chronic obstructive pulmonary disease. (eurekaselect.com)
Due to the broad anti-inflammatory/immunomodulatory action of PDE4 inhibitors, it has been proposed that PDE4 inhibitors might also be efficacious for skin disorders such as atopic dermatitis. (eurekaselect.com)
Consequently, PDE4 inhibitors including cilomilast and AWD 12-281 have been tested in several models of allergic and irritant skin inflammation. (eurekaselect.com)
These PDE4 inhibitors displayed strong anti-inflammatory action in models of allergic contact dermatitis in mice, in the arachidonic acid induced skin inflammation in mice and in ovalbumin sensitised guinea pigs. (eurekaselect.com)
The determination of cytokines in skin homogenates revealed that both Th1 as well as Th2 cytokines are suppressed by PDE4 inhibitors, indicating an anti-inflammatory activity in both the Th2 dominated acute phase as well as the Th1 dominated chronic phase of atopic dermatitis. (eurekaselect.com)
Results of early clinical trials with both topically (cipamfylline, CP80,633) and systemically (CC-10004) active PDE4 inhibitors demonstrated efficacy in atopic dermatitis and in the case of CC-10004, also in psoriasis. (eurekaselect.com)
Results concerning clinical efficacy of this potent and selective PDE4 inhibitor are anxiously awaited. (eurekaselect.com)
The original study now reported has disclosed a new potential target, myometrial phosphodiesterase-4 (PDE4), for tocolysis. (afar.info)
One particular isoform, PDE4B2, is overexpressed in the human myometrium at the end of pregnancy, and we observed a change of the myorelaxant properties of selective PDE4 inhibitors at this time. (afar.info)
In addition, PDE4 inhibitors block the production of LPS-induced inflammatory cytokines by myometrial explants. (afar.info)
Thus, a combination of myorelaxant and anti-inflammatory properties make the PDE4 inhibitors particularly attractive as a target for the prevention of threatened infection-induced preterm delivery and its consequences for the premature infant. (afar.info)
Moracin M, a phenolic component in the skin of Morus alba L., is a potent phosphodiesterase-4 (PDE4) inhibitor with IC 50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. (medchemexpress.com)
Administration of the PDE3 inhibitors cilostazol or cilostamide together with the PDE4 inhibitor rollpram blocked mitogenic synthesis of DNA, as determined by [ 3 H]-thymidine incorporation into renal cortical DNA, in FA-treated rats. (elsevier.com)
IBMX is a broad-spectrum phosphodiesterase ( PDE ) inhibitor, with IC 50 s of 6.5, 26.3 and 31.7 μM for PDE3 , PDE4 and PDE5 , respectively. (medchemexpress.com)
Rolipram is a selective phosphodiesterases PDE4 inhibitor with IC 50 s of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. (medchemexpress.com)
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4) , activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). (medchemexpress.com)
A particular phosphodiesterase, phosphodiesterase-4 ("PDE4", also known as "PDE-IV"), which is a high affinity, cAMP specific, type IV PDE, has generated interest as potential targets for the development of novel antiasthmatic and anti-inflammatory compounds. (allindianpatents.com)
A major concern with the use of PDE4 inhibitors is the side effect of emesis which has been observed for several candidate compounds as described in C.Burnouf et al. (allindianpatents.com)
Adv. In Pharmacol, 44:33-89(1998), there is great interest and research of therapeutic PDE4 inhibitors. (allindianpatents.com)
International Patent Publication W09422852 describes quinolines as PDE4 inhibitors. (allindianpatents.com)
International Patent Publication WO9907704 describes 1-aryl-1,8-naphthylidin-4-one derivatives as PDE4 inhibitors. (allindianpatents.com)
U.S. Patent No. 5,580,888 describes PDE4 inhibitors that are styryl derivatives. (allindianpatents.com)
U.S. Patent No. 5,550,137 describes PDE4 inhibitors that are phenylaminocarbonyl derivatives. (allindianpatents.com)
Patent No. 5,340,827 describes PDE4 inhibitors that are phenylcarboxamide compounds. (allindianpatents.com)

Increasing the availability of cyclic guanosine monophosphate (cGMP) by inhibition of phosphodiesterase-5 (PDE5) is a relatively new, but promising therapeutic strategy. (biomedsearch.com)
Preclinical studies suggest a favorable myocardial effect of PDE5 inhibitors by blocking adrenergic, hypertrophic and pro-apoptotic signaling, thereby supporting their use in HF. (biomedsearch.com)
Larger, controlled trials are now on-going to assess the safety, efficacy and tolerability of PDE5 inhibitors on morbidity and mortality in patients with both systolic and diastolic heart failure. (biomedsearch.com)
Sildenafil is a phosphodiesterase type 5 (PDE5) selective inhibitor. (medscape.com)
Vardenafil is a PDE5 selective inhibitor. (medscape.com)
Tadalafil is a PDE5 selective inhibitor. (medscape.com)
Clinical evidence in men with erectile dysfunction (ED) shows that the phosphodiesterase type 5 (PDE5) inhibitors sildenafil citrate, tadalafil, and vardenafil hydrochloride have favorable safety and efficacy profiles. (jaoa.org)
However, as mild vasodilators, the PDE5 inhibitors are also associated with hemodynamic effects that may be clinically significant, especially when treating men with ED who have comorbid cardiovascular disease. (jaoa.org)
Hemodynamic studies have shown that therapeutic dosages of the PDE5 inhibitors produce only mild and transient changes in mean systolic and diastolic blood pressure and heart rate in healthy men as well as those with ischemic heart disease or chronic stable angina. (jaoa.org)
Overall, PDE5 inhibitors are safe and effective in most patient populations, including men with ischemic cardiovascular disease or those receiving antihypertensive agents, and men with diabetes or those who have undergone nerve-sparing retropubic radical prostatectomy. (jaoa.org)
With the entry of three novel PDE5 inhibitors into the therapeutic armamentarium for ED, differentiating properties of the new agents may confer clinical benefits that physicians as well as patients and their partners should consider when selecting a PDE5 inhibitor. (jaoa.org)
1 , 2 Data from a wide range of clinical trials demonstrate that the oral phosphodiesterase type 5 (PDE5) inhibitors offer efficacy in the treatment of this disorder. (jaoa.org)
Further, as each of these agents-shorter-acting sildenafil citrate and vardenafil hydrochloride, and longer-acting tadalafil-was developed, it proved to confer benefits over placebo in healthy men, in men with comorbidities such as diabetes and cardiovascular disease (CVD), and in men with surgically induced ED. All the PDE5 inhibitors are generally safe and well tolerated, a finding that greatly enhances any and all efficacy benefits. (jaoa.org)
The present studies determined whether clinically relevant phosphodiesterase 5 (PDE5) inhibitors interacted with clinically relevant chemotherapies to kill gastrointestinal/genitourinary cancer cells. (aspetjournals.org)
In bladder cancer cells, regardless of H-RAS mutational status, at clinically achievable doses, PDE5 inhibitors interacted in a greater than additive fashion with doxorubicin/mitomycin C/gemcitabine/cisplatin/paclitaxel to cause cell death. (aspetjournals.org)
In pancreatic tumor cells expressing mutant active K-RAS, PDE5 inhibitors interacted in a greater than additive fashion with doxorubicin/gemcitabine/paclitaxel to cause cell death. (aspetjournals.org)
The most potent PDE5 inhibitor was sildenafil. (aspetjournals.org)
Knock down of PDE5 expression recapitulated the combination effects of PDE5 inhibitor drugs with chemotherapy drugs. (aspetjournals.org)
PDE5 inhibitors enhanced and prolonged the induction of DNA damage as judged by Comet assays and γ histone 2AX ( γ H2AX) and checkpoint kinase 2 (CHK2) phosphorylation. (aspetjournals.org)
As in dark-reared zebrafish, shedding was reduced in larvae and adults treated with the PDE5/6 inhibitors sildenafil and vardenafil but not with the PDE5 inhibitor tadalafil. (arvojournals.org)
Vardenafil has higher affinity to phosphodiesterase-5 (PDE5) than sildenafil and lower administered dosage for the treatment of erectile dysfunction. (aspetjournals.org)
The structure shows that the conformation of the H-loop in the PDE5A1-vardenafil complex is different from those of any known structures of the unliganded PDE5 and its complexes with the inhibitors. (aspetjournals.org)
The conformational variation of both PDE5 and the inhibitors provides structural insight into the different potencies of the drugs. (aspetjournals.org)
The most successful examples of this class of drugs are the PDE5 inhibitors ( Fig. 1 ) sildenafil (Viagra), vardenafil (Levitra), and tadalafil (Cialis), which have been used for treatment of male erectile dysfunction (Rotella et al. (aspetjournals.org)
Although these four PDE5 inhibitors have been successfully approved as the drugs for treatment of human diseases, the enthusiasm for development of novel PDE5 inhibitors continues. (aspetjournals.org)
Chemical structures of PDE5 inhibitors. (aspetjournals.org)
Therapeutic options targeting the NO-sGC-cGMP axis include phosphodiesterase type 5 (PDE5) inhibitors, such as sildenafil and tadalafil, and the sGC stimulator riociguat. (radcliffecardiology.com)
Increasing the amount of cGMP present through the use of PDE5 inhibitors or a sGC stimulator could lead to inhibition of the phosphodiesterase type 3 subtype, in turn leading to increased levels of cyclic adenosine monophosphate resulting in a positive inotropic effect. (radcliffecardiology.com)
TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC 50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH) . (medchemexpress.cn)
Sildenafil (UK-92480) is a potent phosphodiesterase type 5 ( PDE5 ) inhibitor with an IC 50 of 5.22 nM. (medchemexpress.com)
PDE5 inhibitors. (patentsencyclopedia.com)
More specifically, the invention relates to methods of treating multidrug resistance that arises, e.g., during administration of chemotherapeutic/antineoplastic (anticancer) agents for treatment of cancer, with a PDE5 inhibitor (e.g., sildenafil, vardenafil, and tadalafil). (patentsencyclopedia.com)
The invention also relates to methods of treating cancer, e.g., multidrug resistant cancer, using a PDE5 inhibitor in combination with an antineoplastic therapeutic agent. (patentsencyclopedia.com)
Further, the invention relates to pharmaceutical compositions for treating multidrug resistant cancers comprising a PDE5 inhibitor, or a combination of a PDE5 inhibitor and an antineoplastic agent. (patentsencyclopedia.com)
1. A method of treating multidrug resistance in a cancer cell in a subject in need thereof by inhibiting ABCB1 transporter activity, comprising administering to the subject a therapeutically effective amount of a phosphodiesterase 5 (PDE5) inhibitor. (patentsencyclopedia.com)
3. The method of claim 2, wherein the PDE5 inhibitor is sildenafil. (patentsencyclopedia.com)
6. The method of claim 1, wherein the PDE5 inhibitor is administered in combination with an antineoplastic agent. (patentsencyclopedia.com)
15. A method of treating multidrug resistance in a cancer cell in a subject in need thereof by inhibiting ABCC10 transporter activity, comprising administering to the subject a therapeutically effective amount of a PDE5 inhibitor. (patentsencyclopedia.com)
17. The method of claim 16, wherein the PDE5 inhibitor is sildenafil. (patentsencyclopedia.com)
18. The method of claim 16, wherein the PDE5 inhibitor is vardenafil. (patentsencyclopedia.com)
Background: Phosphodiesterase 5 inhibitors (PDE5-Is) are a mainstay in the therapy of erectile dysfunction (ED). The primary end point of clinical efficacy, both in clinical studies and normal practice, is represented by the International Index of Erectile Function (IIEF). (elsevier.com)
Generic Viagra (Sildenafil Citrate) comes under the group of drugs PDE5-inhibitors. (pde-5.com)

abstract = "Coronary Artery Toxicity in Beagle Dogs Given Indolidan, a Type III Phosphodiesterase Inhibitor. (elsevier.com)

Roflumilast, type 4 phosphodiesterase inhibitor, attenuates inflammation in rats with ulcerative. (deepdyve.com)
Can roflumilast, a phosphodiesterase-4 inhibitor, improve clinical outcomes in patients with moderate-to-severe chronic obstructive pulmonary disease? (biomedcentral.com)

Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases. (fpnotebook.com)
Compounds that specifically inhibit PHOSPHODIESTERASE 3. (harvard.edu)
Using this assay, phosphodiesterase type 5 inhibitors (PDE5i) and selective oestrogen receptor modulators (SERMs) were identified to significantly inhibit myofibroblast transformation. (urotoday.com)
PDE inhibitors are potent inotropic and vasodilator drugs, which have also been shown to inhibit tumor necrosis factor alpha (TNF-alpha) production. (aspetjournals.org)
They inhibit the cGMP-specific isoform 5 of phosphodiesterase, resulting in cGMP accumulation, which, for example in smooth muscle cells, reduces muscular tone. (eurekaselect.com)
Phosphodiesterase inhibitor such as amrinone or milrinone will inhibit and block the action of phosphodiesterase/ phosphodiesterase isozyme III which present on the vascular smooth muscle and cardiac muscle. (medicalzone.net)
The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction. (patentsencyclopedia.com)

Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1. (sigmaaldrich.com)
By enzymatically hydrolyzing the terminal phosphodiester bond at the 3'-ends of DNA breaks, tyrosyl-DNA phosphodiesterase (Tdp1) repairs topoisomerase-DNA covalent complexes and processes the DNA ends for DNA repair. (sigmaaldrich.com)
The Development of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. (auckland.ac.nz)
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a key enzyme involved in the repair of TOP1-associated DNA breaks via hydrolysis of 3'-phosphotyrosine bonds. (sussex.ac.uk)

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. (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)
Preliminary studies show that phosphodiesterase inhibitors can be beneficial for purposes other than treating erectile dysfunction. (diabetesincontrol.com)
Phosphodiesterases (PDEs) are enzymes that modulate cyclic nucleotide signaling and as such are clinical targets for a range of disorders including congestive heart failure, erectile dysfunction, and inflammation. (rcsb.org)
4 These agents are in clinical testing or have been US Food and Drug Administration (FDA)-approved for the treatment of multiple conditions, from cardiac failure to fertility, from neurodegeneration to inflammatory/autoimmunity conditions and erectile dysfunction (see Maurice et al 4 for a comprehensive review on PDE inhibitors). (bloodjournal.org)
The PDE inhibitors are used in males to treat erectile dysfunction. (journals.co.za)
What is the evidence for Phosphodiesterase Type 5 Inhibitors in the treatment for erectile dysfunction? (scireproject.com)
1. Phosphodiesterase Type 5 Inhibitors (PDE5i) can be used safely and effectively for treatment of erectile dysfunction (ED) in men with SCI and are recommended as first-line treatment. (scireproject.com)
While in many forms of erectile dysfunction, these agents seem to be very effective, it becomes clear that endothelial dysfunction is an attractive target of PDE 5 inhibitors and may also be the underlying cause in many types of erectile dysfunction. (eurekaselect.com)

The potential for selective phosphodiesterase inhibitors as therapeutic agents was predicted as early as 1977 by Weiss and Hait. (wikipedia.org)
Weiss, B. and Hait, W.N.: Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents. (wikidoc.org)
These neuronal plasticity enhancement properties make PDE1 inhibitors good candidates as therapeutic agents in many neurological conditions. (frontiersin.org)
The development of more specific drugs may pave the way for the use of PDE1 inhibitors as therapeutic agents in cases of neurodevelopmental conditions such as fetal alcohol spectrum disorders and in degenerative disorders such as Alzheimer's and Parkinson's. (frontiersin.org)
Phosphodiesterase (PDE) inhibitors are used as therapeutic agents for management of congestive heart failure. (aspetjournals.org)

The current portfolio of inhibitors have clinical potential for treating sleeping sickness, Chagas' disease and leishmaniasis. (europa.eu)
Phosphodiesterase Inhibitor-Based Vasodilation Improves Oxygen Delivery and Clinical Outcomes Following Stage 1 Palliation. (harvard.edu)
It will be invaluable for everyone who wants to choose the most suitable PDE inhibitor for their research or who is dealing with such drugs in a clinical setting. (textbookx.com)
Theophylline, a non-specific phosphodiesterase inhibitor, is also licensed for the treatment of COPD, however its usefulness in clinical practice is restricted by adverse effects, limited efficacy and its potential for drug interactions. (smw.ch)
In pulmonary arterial hypertension, endothelin receptor antagonist and phosphodiesterase-5 inhibitor combination therapy significantly improved 6-minute walking distance, clinical worsening and N-terminal pro-brain natriuretic peptide compared with the monotherapy but did not offer any advantage in improving pulmonary vascular resistance. (springer.com)
This article discusses the similarities and differences between phosphodiesterase type 5 inhibitors and sGC stimulator based on pharmacological action and clinical trials, and considers which is better for the treatment of pulmonary arterial hypertension. (radcliffecardiology.com)
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension. (medchemexpress.cn)
Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. (medchemexpress.com)

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)
Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator. (medchemexpress.com)

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)
1. The cyclic nucleotide phosphodiesterases (PDEs) present in an insulin secreting cell line, BRIN - BD11, were characterized using calcium/calmodulin, IGF-1, isoenzyme-selective PDE inhibitors and RT - PCR. (strath.ac.uk)
Collateral recruitment involves nitric oxide (NO)-dependent vasodilatation, and the effects of endogenous NO may be enhanced by preventing cGMP degradation by phosphodiesterases (PDEs). (biomedcentral.com)
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)

Liquid chromatography-high resolution mass spectrometry (LC-HRMS) determination of stimulants, anorectic drugs and phosphodiesterase 5 inhibitors (PDE5I) in food supplements. (sigmaaldrich.com)
Aim : To determine the rate of newly detected underlying disease in men receiving their first (index) phosphodiesterase type 5 inhibitor (PDE5i) prescription. (herts.ac.uk)

PDE3 is sometimes referred to as cGMP-inhibited phosphodiesterase. (wikipedia.org)
The PDE3 family comprises two highly homologous subtypes expressed in different tissues, and inhibitors of this family have been shown to increase lipolysis in adipocytes. (rcsb.org)
We report here the three-dimensional structures of the catalytic domain of human PDE3B in complex with a generic PDE inhibitor and a novel PDE3 selective inhibitor. (rcsb.org)
These structures explain the dual cAMP/cGMP binding capabilities of PDE3, provide the molecular basis for inhibitor specificity, and can supply a valid platform for the design of improved compounds. (rcsb.org)
administration of the potent PDE3 inhibitor lixazinone or, to a lesser degree, cilostazol suppressed these high PCNA levels, whereas rolipram alone had no effect. (elsevier.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)
Currently a variety of these new inhibitors are under test as potential anti-inflammatory drugs. (textbookx.com)

A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s). (wikipedia.org)
These agents increase the vasodilatory effects of nitric oxide by inhibiting the enzyme phosphodiesterase type 5, which in turn increases sensitivity for erections. (medscape.com)
Exogeous NO may lead to down regulation of endogenous NO production, and further lead to rapid hydrolization of cyclic guanosine 3′, 5′ monophosphate (cGMP), the smooth muscle relaxant, by the enzyme phosphodiesterase. (springer.com)

IBMX is a nonselective inhibitor of most class I PDE families. (aspetjournals.org)

Effects of a selective inhibitor of cyclic AMP phosphodiesterase on the pial microcirculation in feline cerebral ischemia. (ahajournals.org)
In hepatocytes which had been preincubated with the cyclic AMP phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (IBMX), glucagon elicited a stable desensitized state where resensitization failed to occur even 20 min after exposure of hepatocytes to glucagon. (biochemj.org)
The action of IBMX in stabilizing the glucagon-mediated desensitized state was mimicked by the non-methylxanthine cyclic AMP phosphodiesterase inhibitor Ro-20-1724 [4-(3-butoxy-4-methoxylbenzyl)-2-imidazolidinone]. (biochemj.org)
This action can be detected by attenuating the degradation of cyclic AMP by using inhibitors of cyclic AMP phosphodiesterase. (biochemj.org)

Al-Alaiyan S, Al-Omran A, Dyer D. The use of phosphodiesterase inhibitor (dipyridamole) to wean from inhaled nitric oxide. (springer.com)
But the important contraindication is the concomitant use of PDE 5 inhibitors with any drug serving as a nitric oxide donor, as this combination can lead to significant arterial hypotension. (eurekaselect.com)

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)
Nojiri T, Yamamoto K, Maeda H, Takeuchi Y, Ose N, Susaki Y, Inoue M, Okumura M. A Double-Blind Placebo-Controlled Study of the Effects of Olprinone, a Specific Phosphodiesterase III Inhibitor, for Preventing Postoperative Atrial Fibrillation in Patients Undergoing Pulmonary Resection for Lung Cancer. (harvard.edu)
The objective of this meta-analysis was to evaluate the effect of an endothelin receptor antagonist and phosphodiesterase-5 inhibitor combination in pulmonary arterial hypertension. (springer.com)
Phosphodiesterase type 5 inhibitors, such as sildenafil, and the sGC stimulator riociguat are currently used in the treatment of pulmonary arterial hypertension. (radcliffecardiology.com)
Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease: Cochrane systematic review is a topic covered in the Cochrane Abstracts . (unboundmedicine.com)
Cochrane Abstracts , Evidence Central , evidence.unboundmedicine.com/evidence/view/Cochrane/435597/all/Phosphodiesterase_4_inhibitors_for_chronic_obstructive_pulmonary_disease:_Cochrane_systematic_review. (unboundmedicine.com)

6. The method of claim 5, wherein the Type V phosphodiesterase is sildenafil or a pharmaceutically acceptable salt thereof. (google.com.au)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation. (allindianpatents.com)

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)

The phosphodiesterase-5 inhibitor vardenafil is a potent inhibitor of ABCB1/P-glycoprotein transporter. (nih.gov)

Phosphodiesterase type 1 (PDE1) inhibitors can enhance levels of the second messengers cAMP/cGMP leading to the expression of neuronal plasticity-related genes, neurotrophic factors, and neuroprotective molecules. (frontiersin.org)
Therefore, because of PDE1 inhibitors are good candidates as plasticity enhancers, there is potential for its use as a therapeutic approach in this conditions. (frontiersin.org)
Here we will provide a brief overview of the mechanisms of action of PDE1 inhibitors and discuss the potential for the therapeutic use of these drugs in neurological disorders, focusing on neuronal plasticity improvement. (frontiersin.org)

The different forms or subtypes of phosphodiesterase were initially isolated from rat brains by Uzunov and Weiss in 1972 and were soon afterward shown to be selectively inhibited in the brain and in other tissues by a variety of drugs. (wikipedia.org)
The cardioprotective property and subsequent improved mortality of phosphodiesterase inhibitors can be attributed to this class of drugs' ability to increase levels of cyclic GMP. (diabetesincontrol.com)
Phosphodiesterase III inhibitor is one of the most useful drugs for cardiogenic shock. (ahajournals.org)
Although some studies showed the efficacy of phosphodiesterase (PDE) inhibitors as neuronal plasticity enhancers, little is known about the effectiveness of these drugs to improve plasticity in cases of mental retardation. (jneurosci.org)
One of the most promising new targets for trypanocidal drugs to emerge in recent years is the cyclic AMP (cAMP) phosphodiesterase (PDE) activity encoded by TbrPDEB1 and TbrPDEB2 . (asm.org)
Selective phosphodiesterases (PDE) inhibitors are the new group of antiasthmatic drugs, which integrate antiinflammatory activity with bronchoconstriction counteraction. (viamedica.pl)
Selective inhibitors of phosphodiesterase type 4 are used as alternative or assist drugs in treatment of respiratory system diseases. (viamedica.pl)
One of the most common medical treatments for ED in older people is a class of drugs called phosphodiesterase-5 (PDE 5) inhibitors . (medicalnewstoday.com)
Nowadays, medical treatments available on the market comprise two classes of drugs, acetylcholinesterase (AchE) inhibitors (i.e. donepezil, galantamine, and rivastigmine) and N -methyl-D-aspartate (NMDA) receptor antagonist (i.e. memantine). (intechopen.com)

Which medications in the drug class Phosphodiesterase (type 5) Enzyme Inhibitors are used in the treatment of Cauda Equina and Conus Medullaris Syndromes? (medscape.com)
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)
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia. (semanticscholar.org)

Using a combination of electrophysiological and optical imaging techniques, we show here that vinpocetine, a PDE type I inhibitor, restores ocular dominance plasticity in the ferret model of fetal alcohol exposure. (jneurosci.org)
Here, we try to restore ocular dominance plasticity in alcohol-exposed ferrets using the PDE type 1 inhibitor vinpocetine. (jneurosci.org)

1. This study was undertaken to investigate the possible contribution of the blockade of eotaxin generation to the anti-eosinophilotactic effect of phosphodiesterase (PDE) type 4 inhibitors. (semanticscholar.org)
In some experiments, the putative synergistic interaction between PDE type 4 inhibitors and the beta2-agonist salbutamol was also assessed. (semanticscholar.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)

Selective serotonin reuptake inhibitors and Alzheimer's disease. (alzforum.org)
Phosphodiesterase inhibitors say NO to Alzheimer's disease. (alzforum.org)

In order to study serine/threonine protein phosphatases involved in the regulation of rat adipocyte PDE3B, we investigated the phosphorylation and activation of PDE3B in vivo in response to phosphatase inhibitors and the dephosphorylation and deactivation of PDE3B in vitro by phosphatases purified from rat adipocyte homogenates. (portlandpress.com)

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)

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)
Phosphodiesterase are enzymes that catalyze the hydrolysis of the 3′ cyclic phosphate bonds of adenosine and/or guanosine 3′, 5′ cyclic monophosphate ( Beavo, 1995 ). (frontiersin.org)
We evaluated the effects of cilostazol, a selective inhibitor of cyclic adenosine monophosphate phosphodiesterase, on the pial vessels of adult cats subjected to endothelial damage followed by middle cerebral artery occlusion. (ahajournals.org)

Any substance that inhibits phosphodiesterase, an enzyme that catalyzes the breaking of a phosphodiester bond. (fpnotebook.com)
Selectively inhibits phosphodiesterase type III (PDE III) in cardiac and smooth vascular muscle, resulting in reduced afterload, reduced preload, and increased inotropy. (medscape.com)
W-7 hydrochloride inhibits the Ca 2+ -calmodulin -dependent phosphodiesterase and myosin light chain kinase with IC 50 values of 28 μM and 51 µM, respectively. (medchemexpress.com)

ACE inhibitors are beneficial in all stages of chronic heart failure. (medscape.com)

Imai T, Matsukawa H, Takagi T, Tsuruma K, Shimazawa M, Hara H. The phosphodiesterase III inhibitor cilostazol protects the brain microvasculature from collagenase injury. (harvard.edu)

Claimed newer and more-selective inhibitors are icariin, an active component of Epimedium grandiflorum, and possibly 4-Methylpiperazine and Pyrazolo Pyrimidin-7-1, components of the lichen Xanthoparmelia scabrosa. (wikipedia.org)
Modulation of eotaxin formation and eosinophil migration by selective inhibitors of phosphodiesterase type 4 isoenzyme. (semanticscholar.org)
article{Silva2001ModulationOE, title={Modulation of eotaxin formation and eosinophil migration by selective inhibitors of phosphodiesterase type 4 isoenzyme. (semanticscholar.org)

Pharmacological modulation of myocardial tumor necrosis factor alpha production by phosphodiesterase inhibitors. (aspetjournals.org)

CARDURA® (doxazosin mesylate) is a quinazoline compound that is a selective inhibitor of the alpha1 subtype of alphaadrenergic receptors. (rxlist.com)

A Dual Phosphodiesterase Inhibitor, Zardaverine (type 3/4), Enhan. (ingentaconnect.com)
The goal of this study was to improve post-thaw motility of boar semen by supplementing the thawing medium with a phosphodiesterase inhibitor, Zardaverine. (ingentaconnect.com)
The dual phosphodiesterase inhibitor (type 3/4) Zardaverine significantly enhanced the motility of thawed spermatozoa without adverse effects. (ingentaconnect.com)

PDE molecules contain a variable regulatory domain and a conserved catalytic domain but show distinct substrate specificity and inhibitor selectivity. (aspetjournals.org)

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Agents used predominantly for their inotropic effects include cardiac glycosides and phosphodiesterase inhibitors. (medscape.com)
Phosphodiesterase inhibitor is useful in treating patient due to exacerbation of the congestive cardiac failure or acute cardiac failure. (medicalzone.net)
However, the phosphodiesterase inhibitor may carries its own side effects such as cardiac arrhythmias, nausea, vomiting and thrombocytopenia. (medicalzone.net)

Anatomy20

Organisms12

Diseases3

Chemicals and Drugs136

Analytical, Diagnostic and Therapeutic Techniques and Equipment4

Psychiatry and Psychology1

Phenomena and Processes24

Disciplines and Occupations1

Information Science2

Selective1

Inhibition1

PDE446

PDE542

Abstract1

Roflumilast2

Inhibit7

Tyrosyl-DNA phosphodiesterase4

Erectile10

Therapeutic agents5

Clinical8

Theophylline3

PDEs7

PDE5i2

PDE35

Anti-inflammatory3

Enzyme phosphodiesterase3

Nonselective1

Cyclic AMP phosphodiesterase4

Nitric2

Pulmonary6

Pharmaceutically acceptable salt thereof2

Antagonists1

Potent inhibitor1

PDE13

Drugs9

Treatment3

Vinpocetine2

Type 4 inhibitors2

Isoenzymes4

Alzheimer's2

Vitro1

Intracellular1

Adenosine3

Inhibits3

Chronic1

Cilostazol1

Selective inhibitors3

Modulation1

Subtype1

Zardaverine3

Selectivity1

Tocriset3

Cardiac3