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Phosphodiesterase Inhibitor

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141. Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors †The authors declare no competing interests. Full Text available with Trip Pro

Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors †The authors declare no competing interests. Ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1, EC 3.1.4.1) is a metalloenzyme that belongs to the NPP family, which comprises seven subtypes (NPP1-7). NPP1 hydrolyzes a wide range of phosphodiester bonds, e.g. in nucleoside triphosphates, (cyclic) dinucleotides, and nucleotide sugars yielding nucleoside 5'-monophosphates as products. Its main substrate is ATP which (...) is adenosine 5'-α,β-methylene-γ-thiotriphosphate (Ki = 20 nM vs. p-Nph-5'-TMP, human membrane-bound NPP1). Non-nucleotide-derived NPP1 inhibitors comprise polysulfonates, polysaccharides, polyoxometalates and small heterocyclic compounds. The polyoxometalate [TiW11CoO40]8- (PSB-POM141) is the most potent and selective NPP1 inhibitor described to date (Ki = 1.46 nM vs. ATP, human soluble NPP1); it displays an allosteric mechanism of inhibition and represents a useful pharmacological tool for evaluating

2017 Medchemcomm

142. Phosphodiesterase-5 inhibition suppresses colonic inflammation-induced tumorigenesis via blocking the recruitment of MDSC Full Text available with Trip Pro

Phosphodiesterase-5 inhibition suppresses colonic inflammation-induced tumorigenesis via blocking the recruitment of MDSC Phosphodiesterase 5 (PDE-5) is a major isoform of cGMP phosphodiesterase in diverse tissues and plays a critical role in regulating intracellular cGMP concentrations. However, the distribution and expression of PDE-5 in colitis-related colon cancer was still unclear, not even the function and mechanism. Western blotting and ELISA were performed to detect colonic PDE-5 (...) expression and the prevention role of PDE-5 inhibition in AOM/DSS-induced tumorigenesis model. More importantly, PDE-5 inhibitor Sildenafil inhibited colonic tumorigenesis dependent on inflammation and suppressed DSS-induced colitis. Molecular mechanism investigation indicated that Sildenafil regulated inflammation microenvironment via directly inhibiting MDSC infiltration in colonic tissue. The study provides solid evidence for the use of PDE-5 inhibitor in preventing and treating colonic inflammation

2017 American journal of cancer research

143. Potential synergistic effect of phosphodiesterase inhibitors with chemotherapy in lung cancer Full Text available with Trip Pro

Potential synergistic effect of phosphodiesterase inhibitors with chemotherapy in lung cancer Purpose: Lung cancer remains the leading cause of cancer-related deaths worldwide and novel therapeutic approaches targeting crucial pathways are urgently needed to improve its treatment. Differentiation-based therapeutics (Methylxanthines) and phosphodiesterase inhibitors (type 4 and 5), have been implicated in cancer treatment. Our objectives were to capture any potential anti-tumor effect (...) of these drug combinations with chemotherapeutic agents in vitro. Methods: Theophylline as Methylxanthines, Roflumilast as phosphodiesterase type 4 (PDE4) inhibitor and Sildenafil as phosphodiesterase type 5 (PDE5) inhibitor are the drugs that we combined with the chemotherapeutic agents (Docetaxel, Cisplatin and Carboplatin) in vitro. Lung cancer cell lines (NCI-H1048-Small cell lung cancer-SCLC, A549- Non-small cell lung cancer-NSCLC) were purchased from ATCC LGC Standards. At indicated time-point

2017 Journal of Cancer

144. Phosphodiesterase type 5 inhibitors usage and prostate cancer: a match-paired analysis Full Text available with Trip Pro

Phosphodiesterase type 5 inhibitors usage and prostate cancer: a match-paired analysis To treat erectile dysfunction (ED), phosphodiesterase type 5 inhibitors (PDE5i) are commonly used. However, to date, only a few studies exist evaluate a possible effect on the incidence of prostate cancer. One such study completed by the authors' institution suggested men who use PDE5i for ED may have a lower incidence of prostate cancer. This study was meant to address some of the shortcomings of the former

2017 Translational andrology and urology

145. Inhibition of phosphodiesterase-5 suppresses calcineurin/NFAT- mediated TRPC6 expression in pulmonary artery smooth muscle cells Full Text available with Trip Pro

Inhibition of phosphodiesterase-5 suppresses calcineurin/NFAT- mediated TRPC6 expression in pulmonary artery smooth muscle cells The up-regulation of transient receptor potential channel 6 (TRPC6) has been found to contribute to the proliferation of pulmonary artery smooth muscle cells (PASMCs), and inhibition of phosphodiesterase-5 (PDE5) has been shown to suppress TRPC6 expression in PASMCs. However, the molecular mechanisms underlying the up-regulation of TRPC6 expression and PDE5 modulation (...) , luciferase reporter assay showed that NFATc4 directly regulated the expression of TRPC6 in PASMCs. Inhibition of PDE5 by sildenafil suppressed ET-1-induced activation of calcineurin/NFATc4 signaling pathway and consequent TRPC6 up-regulation in PASMCs, while these inhibitory effects of sildenafil were abolished by PKG inhibitor Rp-8Br-cGMPs. Taken together, our study indicates that ET-1 stimulates TRPC6 expression by activation of calcineurin/NFATc4 signaling pathway, and inhibition of PDE5 suppresses

2017 Scientific reports

146. Replacing a phosphodiesterase-5 inhibitor with riociguat in patients with connective tissue disease-associated pulmonary arterial hypertension: a case series Full Text available with Trip Pro

Replacing a phosphodiesterase-5 inhibitor with riociguat in patients with connective tissue disease-associated pulmonary arterial hypertension: a case series Patients with pulmonary arterial hypertension associated with connective tissue disease (PAH-PAH-CTD) such as systemic sclerosis (SSc) have a poorer response to treatment and increased mortality compared with patients with idiopathic PAH. Current treatment options for PAH-CTD include prostanoids, phosphodiesterase type-5 inhibitors (PDE-5i

2017 Pulmonary circulation

147. Selective Inhibitors of Phosphodiesterase 4B (PDE-4B) May Provide a Better Treatment for CNS, Metabolic, Autoimmune, and Inflammatory Diseases Full Text available with Trip Pro

Selective Inhibitors of Phosphodiesterase 4B (PDE-4B) May Provide a Better Treatment for CNS, Metabolic, Autoimmune, and Inflammatory Diseases 29152042 2018 11 13 1948-5875 8 11 2017 Nov 09 ACS medicinal chemistry letters ACS Med Chem Lett Selective Inhibitors of Phosphodiesterase 4B (PDE-4B) May Provide a Better Treatment for CNS, Metabolic, Autoimmune, and Inflammatory Diseases. 1132-1133 10.1021/acsmedchemlett.7b00425 Abdel-Magid Ahmed F AF Therachem Research Medilab (India) Pvt. Ltd

2017 ACS medicinal chemistry letters

148. Inhibition of Cyclic Adenosine Monophosphate-Specific Phosphodiesterase by Various Food Plant-Derived Phytotherapeutic Agents Full Text available with Trip Pro

Inhibition of Cyclic Adenosine Monophosphate-Specific Phosphodiesterase by Various Food Plant-Derived Phytotherapeutic Agents Background: Phosphodiesterases (PDEs) play a major role in the regulation of cyclic adenosine monophosphate (cAMP)- and cyclic guanosine monophosphate (cGMP)-mediated pathways. Their inhibitors exhibit anti-inflammatory, vasodilatory and antithrombotic effects. Therefore, consumption of foods with PDE-inhibiting potential may possess beneficial influence on the risk (...) of cardiovascular diseases. Methods: Four plant extracts (Arbutus unedo, Camellia sinensis, Cynara scolymus, Zingiber officinale) with promising ingredient profiles and physiological effects were tested for their ability to inhibit cAMP-specific PDE in vitro in a radioactive assay. Results: Strawberry tree fruit (Arbutus unedo) and tea (Camellia sinensis) extracts did not inhibit PDE markedly. Alternatively, artichoke (Cynara scolymus) extract had a significant inhibitory influence on PDE activity (IC50 = 0.9

2017 Medicines

149. Multiple Behavior Phenotypes of the Fragile-X Syndrome Mouse Model Respond to Chronic Inhibition of Phosphodiesterase-4D (PDE4D) Full Text available with Trip Pro

Multiple Behavior Phenotypes of the Fragile-X Syndrome Mouse Model Respond to Chronic Inhibition of Phosphodiesterase-4D (PDE4D) Fragile-X syndrome (FXS) patients display intellectual disability and autism spectrum disorder due to silencing of the X-linked, fragile-X mental retardation-1 (FMR1) gene. Dysregulation of cAMP metabolism is a consistent finding in patients and in the mouse and fly FXS models. We therefore explored if BPN14770, a prototypic phosphodiesterase-4D negative allosteric

2017 Scientific reports

150. Inhibition of Phosphodiesterase 5 and Increasing the Level of Cyclic Guanosine 3′,5′ Monophosphate by Hydroalcoholic Achillea wilhelmsii C. Koch Extract in Human Breast Cancer Cell Lines MCF-7 and MDA-Mb-468 Full Text available with Trip Pro

Inhibition of Phosphodiesterase 5 and Increasing the Level of Cyclic Guanosine 3′,5′ Monophosphate by Hydroalcoholic Achillea wilhelmsii C. Koch Extract in Human Breast Cancer Cell Lines MCF-7 and MDA-Mb-468 This study aimed to investigate the effect of hydroalcoholic Achillea wilhelmsii C. Koch extract (HAWE) on phosphodiesterase 5 (PDE5) gene expression and cyclic guanosine 3',5' monophosphate (cGMP) signaling in the MCF-7 and MDA-Mb-468 cell lines. The effective dose (ED50) of HAWE

2017 Breast cancer : basic and clinical research

151. Sildenafil, a Phosphodiesterase Type 5 Inhibitor, Downregulates Osteopontin in Human Peripheral Blood Mononuclear Cells Full Text available with Trip Pro

Sildenafil, a Phosphodiesterase Type 5 Inhibitor, Downregulates Osteopontin in Human Peripheral Blood Mononuclear Cells The aim of this study was to investigate the ability of sildenafil to regulate osteopontin (OPN) gene and protein in peripheral blood mononuclear cells (PBMCs) from healthy blood donors. OPN is expressed by a wide variety of cell types, including immune cells. OPN functions are linked to various physiological and pathological conditions. Sildenafil is a selective inhibitor (...) of type 5 phosphodiesterase. Sildenafil has recently been found to have immunomodulatory effects in animal models and in studies performed in humans. PMA-stimulated and unstimulated PBMCs from 16 healthy blood donors (men) were cultured with sildenafil (at concentrations of 400 ng/ml and 4 µg/ml). OPN level in culture supernatants was measured by enzyme-linked immunosorbent assay. The analysis of OPN gene expression was performed by real-time PCR. Cell viability was assessed by trypan blue staining

2017 Archivum Immunologiae et Therapiae Experimentalis

152. Phosphodiesterase Inhibitors as a Therapeutic Approach to Neuroprotection and Repair Full Text available with Trip Pro

Phosphodiesterase Inhibitors as a Therapeutic Approach to Neuroprotection and Repair A wide diversity of perturbations of the central nervous system (CNS) result in structural damage to the neuroarchitecture and cellular defects, which in turn are accompanied by neurological dysfunction and abortive endogenous neurorepair. Altering intracellular signaling pathways involved in inflammation and immune regulation, neural cell death, axon plasticity and remyelination has shown therapeutic benefit (...) in experimental models of neurological disease and trauma. The second messengers, cyclic adenosine monophosphate (cyclic AMP) and cyclic guanosine monophosphate (cyclic GMP), are two such intracellular signaling targets, the elevation of which has produced beneficial cellular effects within a range of CNS pathologies. The only known negative regulators of cyclic nucleotides are a family of enzymes called phosphodiesterases (PDEs) that hydrolyze cyclic nucleotides into adenosine monophosphate (AMP

2017 International journal of molecular sciences

153. Psiguajadials A–K: Unusual Psidium Meroterpenoids as Phosphodiesterase-4 Inhibitors from the Leaves of Psidium guajava Full Text available with Trip Pro

Psiguajadials A–K: Unusual Psidium Meroterpenoids as Phosphodiesterase-4 Inhibitors from the Leaves of Psidium guajava Bioassay-guided fractionation of the ethanolic extract of the leaves of Psidium guajava led to the isolation of 11 new Psidium meroterpenoids, psiguajadials A-K (1-11), along with 17 known ones (12-28). Their structures and absolute configurations were elucidated by spectroscopic methods and comparison of experimental and calculated ECD. Compounds 1 and 2 represent two (...) unprecedented skeletons of 3,5-diformyl-benzyl phloroglucinol-coupled sesquiterpenoid, while 3 is the first example of Psidium meroterpenoids coupling via an oxepane ring. Putative biosynthetic pathways towards 1 and 2 are proposed. Compounds 1-13 and 16-26 exhibited moderate inhibitory activities against phosphodiesterase-4 (PDE4), a drug target for asthma and chronic obstructive pulmonary disease, with IC50 values in the range of 1.34-7.26 μM.

2017 Scientific reports

154. The Phosphodiesterase 10A Inhibitor PF-2545920 Enhances Hippocampal Excitability and Seizure Activity Involving the Upregulation of GluA1 and NR2A in Post-synaptic Densities Full Text available with Trip Pro

The Phosphodiesterase 10A Inhibitor PF-2545920 Enhances Hippocampal Excitability and Seizure Activity Involving the Upregulation of GluA1 and NR2A in Post-synaptic Densities Phosphodiesterase regulates the homeostasis of cAMP and cGMP, which increase the strength of excitatory neural circuits and/or decrease inhibitory synaptic plasticity. Abnormally, synchronized synaptic transmission in the brain leads to seizures. A phosphodiesterase 10A (PDE10A) inhibitor PF-2545920 has recently attracted

2017 Frontiers in molecular neuroscience

155. Roles of roflumilast, a selective phosphodiesterase 4 inhibitor, in airway diseases Full Text available with Trip Pro

Roles of roflumilast, a selective phosphodiesterase 4 inhibitor, in airway diseases Asthma and chronic obstructive pulmonary disease (COPD) are common chronic respiratory diseases. Both diseases have incompletely distinct pathophysiology, clinical manifestation, and treatment responsiveness. Pulmonary and systemic inflammations are the hallmarks of COPD. Most asthma responds to inhaled corticosteroid (ICS) treatment. In contrast, COPD is a corticosteroid-resistant disease. Bronchodilators (...) are a preferred treatment method of COPD, with the aim of improving symptoms and preventing exacerbation. In addition, corticosteroid insensitivity is an underlying mechanism in severe asthma. An overlap of features between asthma and COPD, which was described as asthma-COPD overlap syndrome (ACOS) is not uncommon in practice. Novel nonsteroidal therapies focusing on inflammation in asthma and COPD have been developed. Selective phosphodiesterase 4 (PDE4) inhibitor is a promising class of drugs that has been

2017 Journal of thoracic disease

156. Phosphodiesterase type 5 inhibition may reduce diastolic function in women with ischemia but no obstructive coronary artery disease Full Text available with Trip Pro

Phosphodiesterase type 5 inhibition may reduce diastolic function in women with ischemia but no obstructive coronary artery disease Ischemia, in the absence of obstructive coronary artery disease, is prevalent in women, and associated with increased risk for major cardiovascular events. Coronary microvascular dysfunction is prevalent in these patients, and associated with impaired diastolic function. Despite our general understanding, however, optimal treatment of this cohort remains elusive.To (...) address this knowledge gap, we performed an open-label treatment trial to assess whether phosphodiesterase type 5 inhibition improves coronary microvascular perfusion and diastolic function in women with signs and symptoms of ischemia but no evidence of obstructive coronary artery disease. Left ventricular morphology and function, along with myocardial perfusion reserve index, were assessed by contrast-enhanced cardiac magnetic resonance imaging.A total of five women enrolled of which four completed

2017 Journal of medical case reports

157. Phosphodiesterase-4 inhibition restored hippocampal long term potentiation after primary blast Full Text available with Trip Pro

debated. Our group previously reported that in vitro primary blast exposure reduced long-term potentiation (LTP), the electrophysiological correlate of learning and memory, in rat organotypic hippocampal slice cultures (OHSCs) and that primary blast affects key proteins governing LTP. Recent studies have investigated phosphodiesterase-4 (PDE4) inhibition as a therapeutic strategy for reducing LTP deficits following inertia-driven TBI. We investigated the therapeutic potential of PDE4 inhibitors (...) Phosphodiesterase-4 inhibition restored hippocampal long term potentiation after primary blast Due to recent military conflicts and terrorist attacks, blast-induced traumatic brain injury (bTBI) presents a health concern for military and civilian personnel alike. Although secondary blast (penetrating injury) and tertiary blast (inertia-driven brain deformation) are known to be injurious, the effects of primary blast caused by the supersonic shock wave interacting with the skull and brain remain

2017 Experimental neurology

158. Phosphodiesterase type 5 inhibitor to riociguat transition is associated with hemodynamic and symptomatic improvement in pulmonary hypertension Full Text available with Trip Pro

Phosphodiesterase type 5 inhibitor to riociguat transition is associated with hemodynamic and symptomatic improvement in pulmonary hypertension Riociguat is a soluble guanylate cyclase stimulator approved for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. We studied the clinical and hemodynamics effects of transitioning 12 pulmonary hypertension patients from Phosphodiesterase type 5 inhibitor (PDE5i) to riociguat, and demonstrated

2017 Pulmonary circulation

159. Novel cilostamide analogs, phosphodiesterase 3 inhibitors, produce positive inotropic but differential lusitropic and chronotropic effects on isolated rat atria Full Text available with Trip Pro

Novel cilostamide analogs, phosphodiesterase 3 inhibitors, produce positive inotropic but differential lusitropic and chronotropic effects on isolated rat atria Recently, we showed that some new synthetic compounds structurally related to cilostamide (4-(1,2-dihydro-2-oxoquinolin-6-hydroxy)- N-cyclohexyl-N-methylbutanamide), a selective phosphodiesterase 3 (PDE3) inhibitor, produce inotropic effect comparable to that of IBMX (3-isobutyl-1-methylxanthine), a non-selective PDE inhibitor (...) with isoprenaline, produced the highest inotropic effect while it did not affect the basal contraction rate and almost blocked the isoprenaline chronotropic effect.Combination of mc2 with isoprenaline had synergistic effect on inotropic effect, but this combination reduced isoprenaline chronotropic effect; therefore, these effects cannot be related to reducing B-adrenergic receptors activity. These compounds showed different effects; probably all of them were not mediated via PDE3 inhibition and other

2017 Iranian journal of basic medical sciences

160. The use of antimuscarinics, phosphodiesterase type V inhibitors and phytotherapy for lower urinary tract symptoms in men Full Text available with Trip Pro

The use of antimuscarinics, phosphodiesterase type V inhibitors and phytotherapy for lower urinary tract symptoms in men Besides the mainstay of α-blockers and 5α-reductase inhibitors, other forms of medical therapy complete the armamentarium in the treatment of lower urinary tract symptoms (LUTS) in men. These treatments can target specific symptoms as well as associated symptoms that would affect the quality of life of the patients. Many patients are bothered by storage symptoms, more so than (...) the voiding symptoms. Antimuscarinics are efficacious and safe, provided the patients do not have high post void residual urine. Many patients with LUTS also have erectile dysfunction, and phosphodiesterase type V inhibitors are effective in relieving both LUTS as well as erectile dysfunction for such patients. Phytotherapy provides a popular and safe treatment for LUTS, however, the efficacy of the treatment has not been proven in well conducted prospective randomized controlled studies.

2017 Asian Journal of Urology

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