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Phosphodiesterase Inhibitors1-Methyl-3-isobutylxanthine3',5'-Cyclic-AMP PhosphodiesterasesRolipramPhosphoric Diester HydrolasesPurinones4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinoneCyclic AMP3',5'-Cyclic-GMP PhosphodiesterasesCyclic Nucleotide Phosphodiesterases, Type 4TheophyllinePhosphodiesterase 3 InhibitorsPhosphodiesterase 4 InhibitorsCyclic GMPMilrinoneCyclic Nucleotide Phosphodiesterases, Type 3Phosphodiesterase 5 InhibitorsPapaverinePyrrolidinonesCyclic Nucleotide Phosphodiesterases, Type 5Phosphodiesterase ICyclic Nucleotide Phosphodiesterases, Type 12',3'-Cyclic-Nucleotide PhosphodiesterasesColforsinPentoxifyllineBucladesineSulfonesXanthines8-Bromo Cyclic Adenosine MonophosphateNucleotides, CyclicPyridazinesAdenylate CyclasePurinesIsoproterenolEnoximoneVinca AlkaloidsAmrinoneAminophyllineBufo bufoCyclic AMP-Dependent Protein KinasesCyclic Nucleotide Phosphodiesterases, Type 2Dose-Response Relationship, DrugPhotoreceptor CellsCyclic Nucleotide Phosphodiesterases, Type 6KineticsDibutyryl Cyclic GMPPiperazinesCalciumGuanylate CyclaseDipyridamoleErectile DysfunctionAlprostadilPhthalazinesPyridonesThionucleotidesAdenosinePhenylisopropyladenosineCyclic Nucleotide Phosphodiesterases, Type 7Guinea PigsEnzyme ActivationCells, CulturedProstaglandins IPenile ErectionCyclic GMP-Dependent Protein KinasesSecond Messenger SystemsStimulation, ChemicalIsoquinolinesNitric OxideProstaglandins E, SyntheticVasodilator AgentsTransducinRats, Inbred StrainsNitroprussideTetrazolesCattleImidazolesCholera ToxinNicotinic AcidsIloprostIsoenzymesRod Cell Outer SegmentReceptors, Adrenergic, betaTriazinesOxadiazolesAdrenergic beta-AgonistsEnzyme InhibitorsRats, WistarCaffeineAtrial Natriuretic FactorPropranololMuscle, SmoothCardiotonic AgentsDrug SynergismSignal TransductionProstaglandins ERats, Sprague-DawleyTime FactorsAdenosine-5'-(N-ethylcarboxamide)NaphthyridinesMethylene Blue
PDE5PDE5iNovel PhosphodiesteraseErectile dysfunctionPhosphodiester bond of cAMPCGMPAntagonistsProtease inhibitorCalcineurin inhibitorsPDE3SelectiveCyclicTherapeuticPotentRolipramEnzymesCytochromeEnzymePatientsPathwayCombinationConcomitantAdditiveSignificantlyTreatmentInflammatoryTherapiesEffectsSubtypesLevitraMedicinesHumanActivityAgents
PDE510
  • Phosphodiesterase type 5 (PDE5) inhibitors are the principal oral agents used in ED. (medscape.com)
  • PDE5 inhibitors rely on the role of nitric oxide (NO) in inducing vasodilatation. (medscape.com)
  • Tadalafil is a PDE5-selective inhibitor that is chemically unrelated to sildenafil and vardenafil. (medscape.com)
  • Avanafil is a PDE5 inhibitor that inhibits cGMP degradation and thereby enhances the effects of NO in smooth muscle relaxation of the corpus cavernosum. (medscape.com)
  • It was recognised that papaverine and pentoxifylline mediated vasorelaxation by a number of mechanisms including non-selective PDE inhibition and these drugs can be considered as forerunners to the clinically successful PDE5 inhibitors used today for the treatment of erectile dysfunction. (biomedjournal.com)
  • Men who take nitrate drugs cannot use PDE5 inhibitors. (limamemorial.org)
  • PDE5 inhibitors can also interact with other medications. (limamemorial.org)
  • Talk to your doctor about whether PDE5 inhibitor drugs are a safe choice for you. (limamemorial.org)
  • Recently, several randomized controlled trials (RCTs) explored the effects of α-blockers with or without phosphodiesterase type 5 inhibitors (PDE5-Is) for lower urinary tract symptoms secondary to benign prostatic hyperplasia (LUTS/BPH). (uroweb.org)
  • PDE5 inhibitors are contraindicated in patients taking any form of organic nitrates. (findlaw.com)
PDE5i3
  • A proportion of pulmonary arterial hypertension (PAH) patients do not reach treatment goals with phosphodiesterase-5 inhibitors (PDE5i). (ersjournals.com)
  • What are the benefits and harms of medicines that increase blood flow to the extremities (phosphodiesterase 5 inhibitors (PDE5i)) compared to placebo for the treatment of Raynaud's phenomenon? (cochrane.org)
  • Phosphodiesterase 5 inhibitors (PDE5i) are a class of medicines used in the treatment of erectile dysfunction and high blood pressure in the lungs. (cochrane.org)
Novel Phosphodiesterase1
  • Areas covered: This manuscript reviews the current literature on preclinical and clinical studies regarding topical E6005/RVT-501, a novel phosphodiesterase 4 inhibitor. (elsevierpure.com)
Erectile dysfunction2
Phosphodiester bond of cAMP2
  • Phosphodiesterases (PDEs) hydrolyze the phosphodiester bond of cAMP and cGMP to form the inactive 5′-AMP and 5′-GMP. (biomedjournal.com)
  • As in somatic cells, sperm intracellular cAMP concentration is regulated by the opposite action of two enzymes: the adenylyl cyclases (AC), which synthesize cAMP from ATP, and the phosphodiesterases (PDE), which break the phosphodiester bond of cAMP to form 5'-adenosine monophosphate (AMP). (plos.org)
CGMP6
  • 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)
  • PDE3 is sometimes referred to as cGMP-inhibited phosphodiesterase. (wikipedia.org)
  • The homeostatic role of phosphodiesterases (PDEs) as related to the intracellular levels of cAMP and cGMP was first described by Sutherland (Sutherland, Rall, 1958) who, due to this, was awarded the Nobel Prize for Physiology and Medicine in 1971. (biomedjournal.com)
  • Phosphodiesterase 9 (PDE9), a specifically hydrolytic enzyme with the highest affinity for cyclic guanosine monophosphate (cGMP) among the phosphodiesterase family, controls cGMP in cardiac myocytes and is strongly upregulated in human heart failure, suggesting its potential as a promising therapeutic target in heart failure. (protheragen.com)
  • The family of phosphodiesterases (PDEs) are regulatory hydrolase enzymes that play a crucial role in modulating cyclic nucleotides, including cGMP and cAMP, which are involved in a wide range of physiological processes. (protheragen.com)
  • Among all PDEs, PDE9 has the highest affinity for cGMP, making it an attractive target for inhibitors that regulate cGMP levels. (protheragen.com)
Antagonists1
  • Current therapies to reduce obstruction, such as α1-adrenoceptor antagonists and 5α-reductase inhibitors, are not effective in all patients. (lu.se)
Protease inhibitor8
  • Prezcobix (darunavir and cobicistat) is a combination of a human immunodeficiency virus ( HIV -1) protease inhibitor and a CYP3A inhibitor and is indicated for the treatment of HIV-1 infection in adult patients. (rxlist.com)
  • As [HA565 trade name] is used as a pharmacokinetic enhancer with other protease inhibitors, the product information for the particular protease inhibitor must be consulted. (who.int)
  • The recommended dose is 100 mg ritonavir once or two times per day, depending on the concurrently used protease inhibitor. (who.int)
  • For children who are undergoing anti-tuberculosis treatment with rifampicin, higher dosages of ritonavir may be needed for pharmacokinetic enhancement of the combined protease inhibitor. (who.int)
  • Depending on the specific protease inhibitor with which it is co-administered, ritonavir may be appropriate for use with caution in patients with renal insufficiency. (who.int)
  • For specific dosing information in patients with renal impairment, refer to the product information of the co-administered protease inhibitor. (who.int)
  • In the absence of pharmacokinetic studies in patients with stable severe hepatic impairment (Child Pugh grade C) without decompensation, caution should be exercised when ritonavir is used as a pharmacokinetic enhancer as increased levels of the co-administered protease inhibitor may occur. (who.int)
  • Specific recommendations for use of ritonavir as a pharmacokinetic enhancer in patients with hepatic impairment are dependent on the protease inhibitor with which it is co-administered. (who.int)
Calcineurin inhibitors1
  • Introduction: Local adverse effects of steroid use and the burning sensation of calcineurin inhibitors impair patients' adherence to treatment and decrease the treatment response in atopic dermatitis (AD). (elsevierpure.com)
PDE34
  • PDE3 inhibitors can be thought of as a backdoor approach to cardiac stimulation, whereas β-agonists go through the front door to produce the same cardiac effects. (biomedjournal.com)
  • PDE3 was identified as a potential therapeutic target in cardiovascular disease and asthma, and indeed, PDE3 inhibitors have subsequently been shown to relax vascular and airway smooth muscle, inhibit platelet aggregation and induce lipolysis. (biomedjournal.com)
  • Phosphodiesterase 3 ( PDE3 ) is one member of the PDE family and has two subtypes, PDE3A and PDE3B. (cancer-research-network.com)
  • PDE3 inhibitors suppress meiosis in oocytes by decreasing the level of cAMP and blocking the extrusion of the first polar body. (cancer-research-network.com)
Selective6
  • The potential for selective phosphodiesterase inhibitors as therapeutic agents was predicted as early as 1977 by Weiss and Hait. (wikipedia.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)
  • By increasing our understanding of the physiological roles of the individual PDE isoforms, in parallel with the development of even more selective inhibitors of these enzymes, it is highly likely that better therapeutically active drugs will emerge. (biomedjournal.com)
  • BioLink2022 is a highly selective oral PDE9 small molecule inhibitor in early clinical development for the treatment of chronic heart failure. (protheragen.com)
  • The active ingredients of Poxet-60 tablets is Dapoxetine 60mg , a Selective Serotonin Reuptake Inhibitor (SSRI) that specifically treats Premature Ejaculation (PE), as it works quickly and gives results within two hours and is quickly discharged from the body within a period of 24 hours. (pde-5.com)
  • The active ingredient of Poxet-60 tablets is a selective serotonin reuptake inhibitor (SSRI) known as Dapoxetine, that treats and prevents the recurrence or persistence of PE. (pde-5.com)
Cyclic2
  • Sperm intracellular cAMP levels depend on the activity of adenylyl cyclases, mostly SACY, though transmembrane-containing adenylyl cyclases are also present, and on the activity of cyclic nucleotide phosphodiesterases (PDE) whose role is to degrade cAMP into 5'-AMP. (plos.org)
  • Goupil S, Maréchal L, El Hajj H, Tremblay M-È, Richard FJ, Leclerc P (2016) Identification and Localization of the Cyclic Nucleotide Phosphodiesterase 10A in Bovine Testis and Mature Spermatozoa. (plos.org)
Therapeutic2
  • The ubiquitous presence of this enzyme means that non-specific inhibitors have a wide range of actions, the actions in the heart, and lungs being some of the first to find a therapeutic use. (wikipedia.org)
  • Phosphodiesterase inhibitors (PDIs) have important vascular and myocardial protective effects and thus have shown therapeutic usefulness in the clinical settings for treatment of patients with heart failure, pulmonary hypertension, and coronary artery disease. (biomedjournal.com)
Potent3
  • Piclamilast, a more potent inhibitor than rolipram. (wikipedia.org)
  • It is a potent PDE9 inhibitor that characterized by high selectivity, low brain penetration, and target tissue distribution. (protheragen.com)
  • The structures reveal their novel mode of action as competitive ligands for the binding site of an incoming DNA substrate, and point the way to generating novel and potent inhibitors of TDP2. (rcsb.org)
Rolipram1
  • The effects of IBMX were mimicked by rolipram, an inhibitor of the cAMP-specific phosphodiesterase IV. (arizona.edu)
Enzymes1
  • Cobicistat is a mechanism-based inhibitor of cytochrome P450 (CYP) enzymes of the CYP3A family. (rxlist.com)
Cytochrome1
  • Strong cytochrome P450 (CYP) 3A inhibitors may increase exposure to doxazosin and increased risk of hypotension. (nih.gov)
Enzyme1
  • A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE) selectively in the brain. (biomedjournal.com)
Patients5
  • The goal of this study was to determine whether a phosphodiesterase-4D (PDE4D) allosteric inhibitor (BPN14770) would improve cognitive function and behavioral outcomes in patients with fragile X syndrome (FXS). (nature.com)
  • Cilostazol, a phosphodiesterase III inhibitor, has been shown to significantly improve high on-treatment platelet reactivity in patients receiving both aspirin and clopidogrel and has antiproliferative effects (inhibiting neointimal hyperplasia and smooth muscle proliferation), thus reducing the risk of restenosis after coronary stent implantation. (nih.gov)
  • HA565 trade name] is indicated as a pharmacokinetic enhancer for protease inhibitors when these are used in combination therapy with other antiretroviral agents for the treatment of HIV-1 infected patients. (who.int)
  • However, some patients report that they experienced serious side effects, including cardiovascular issues after taking PDE-5 inhibitors. (findlaw.com)
  • [ 6 ] Patients should not have taken a phosphodiesterase inhibitor for at least 48 hours before the exam. (medscape.com)
Pathway1
  • To delineate these effects, we used PKA pathway inhibitors (adenylyl cyclase [AC], cAMP, and PKA) to modulate the effects of alcohol on dust-stimulated TNF-a release in the bronchial epithelial cell line, BEAS-2B. (cdc.gov)
Combination1
  • In the current study, the β-adrenergic receptor agonist isoproterenol, alone or in combination with the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (IBMX), was used to increase cAMP in neutrophils. (arizona.edu)
Concomitant1
  • Concomitant administration of doxazosin tablets with a phosphodiesterase-5 (PDE-5) inhibitor can result in additive blood pressure lowering effects and symptomatic hypotension. (nih.gov)
Additive1
Significantly2
  • The soluble adenylyl cyclase inhibitor, KH7, however, significantly increased the inflammatory response to hog barn dust. (cdc.gov)
  • phosphodiesterase 4 inhibitors significantly elevated cAMP and enhanced alcohol-mediated inhibition of dust-stimulated TNF-a release. (cdc.gov)
Treatment1
  • Treatment with a PDE4 inhibitor raised the deficient cAMP levels and restored some functionality to Hippocampus-based memory functions. (wikipedia.org)
Inflammatory1
  • PDE4 inhibitors have proven potential as anti-inflammatory drugs, especially in inflammatory pulmonary diseases such as asthma, COPD, and rhinitis. (wikipedia.org)
Therapies1
  • Consequently, TDP2 is an interesting target for the development of small molecule inhibitors that could restore sensitivity to topoisomerase-directed therapies. (rcsb.org)
Effects2
  • PDE4 inhibitors may have antidepressive effects and have also been proposed for use as antipsychotics. (wikipedia.org)
  • Table 1 summarizes the functions of each PDE and the cardiovascular effects of specific inhibitors. (biomedjournal.com)
Subtypes2
  • The different forms or subtypes of phosphodiesterase were initially isolated from rat brains in the early 1970s and were soon afterward shown to be selectively inhibited in the brain and in other tissues by a variety of drugs. (wikipedia.org)
  • At least seven phosphodiesterase (PDE) classes are known, many with subtypes identified by structure and function. (medscape.com)
Levitra1
  • Technically, Levitra is considered an oral phosphodiesterase type-5 inhibitor. (findlaw.com)
Medicines1
  • Phosphodiesterase-5 inhibitors (PDE-5 inhibitors) are commonly used oral medicines for erection problems. (healthlinkbc.ca)
Human1
  • Darunavir is an inhibitor of the human immunodeficiency virus ( HIV -1) protease . (rxlist.com)
Activity2
  • Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a 5'-tyrosyl DNA phosphodiesterase important for the repair of DNA adducts generated by non-productive (abortive) activity of topoisomerase II (TOP2). (rcsb.org)
  • Microtubule inhibitors potently decreased FXR reporter gene activity. (nature.com)
Agents1
  • The Khamisiyah ammunition storage that housed chemical warfare agents such as sarin, an acetylcholinesterase (AChE) inhibitor, was demolished during the GW, releasing toxicants into the atmosphere affecting deployed troops. (cdc.gov)