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https://www.readbyqxmd.com/read/28515693/rolipram-improves-outcome-in-a-rat-model-of-infant-sepsis-induced-cardiorenal-syndrome
#1
Clark R Sims, Sharda P Singh, Shengyu Mu, Neriman Gokden, Dala Zakaria, Trung C Nguyen, Philip R Mayeux
While the mortality rate associated with sepsis in children has fallen over the years, it still remains unacceptably high. The development of both acute cardiac dysfunction and acute kidney injury during severe sepsis is categorized as type 5 cardiorenal syndrome (CRS) and is poorly understood in infants. To address this lack of understanding and the need for an appropriate animal model in which to conduct relevant preclinical studies, we developed a model of infant sepsis-induced CRS in rat pups then evaluated the therapeutic potential of the phosphodiesterase (PDE) 4 inhibitor, rolipram...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28414142/doxofylline-does-not-increase-formoterol-induced-camp-nor-mkp-1-expression-in-asm-cells-resulting-in-lack-of-anti-inflammatory-effect
#2
Brijeshkumar S Patel, Michael J Kugel, Gina Baehring, Alaina J Ammit
The xanthine doxofylline has been examined in clinical trials and shown to have efficacy and greater tolerability than theophylline in asthma and chronic obstructive pulmonary disease. The 'novofylline' doxofylline has demonstrated bronchodilatory and anti-inflammatory actions in in vivo and ex vivo experimental models of respiratory disease. However, there are limited studies in vitro. We address this herein and examine whether doxofylline has anti-inflammatory impact on primary cultures of airway smooth muscle (ASM) cells...
April 13, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28330503/caffeine-modulates-glucocorticoid-induced-expression-of-ctgf-in-lung-epithelial-cells-and-fibroblasts
#3
Markus Fehrholz, Kirsten Glaser, Christian P Speer, Silvia Seidenspinner, Barbara Ottensmeier, Steffen Kunzmann
BACKGROUND: Although caffeine and glucocorticoids are frequently used to treat chronic lung disease in preterm neonates, potential interactions are largely unknown. While anti-inflammatory effects of glucocorticoids are well defined, their impact on airway remodeling is less characterized. Caffeine has been ascribed to positive effects on airway inflammation as well as remodeling. Connective tissue growth factor (CTGF, CCN2) plays a key role in airway remodeling and has been implicated in the pathogenesis of chronic lung diseases such as bronchopulmonary dysplasia (BPD) in preterm infants...
March 23, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28263828/6-hydroxy-5-7-dimethoxy-flavone-suppresses-the-neutrophil-respiratory-burst-via-selective-pde4-inhibition-to-ameliorate-acute-lung-injury
#4
Yung-Fong Tsai, Tzu-Chi Chu, Wen-Yi Chang, Yang-Chang Wu, Fang-Rong Chang, Shun-Chin Yang, Tung-Ying Wu, Yu-Ming Hsu, Chun-Yu Chen, Shih-Hsin Chang, Tsong-Long Hwang
Over-activated neutrophils produce enormous oxidative stress and play a key role in the development of acute and chronic inflammatory diseases. 6-Hydroxy-5,7-dimethoxy-flavone (UFM24), a flavone isolated from the Annonaceae Uvaria flexuosa, showed inhibitory effects on human neutrophil activation and salutary effects on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice. UFM24 potently inhibited superoxide anion (O2(•-)) generation, reactive oxidants, and CD11b expression, but not elastase release, in N-formyl-l-methionyl-l-leucyl-l-phenylalanine (fMLF)-activated human neutrophils...
March 3, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28167453/the-role-of-%C3%AE-arrestin-2-on-fear-anxious-related-memory-in-a-rat-model-of-post-traumatic-stress-disorder
#5
Jinlan Ding, Fang Han, Lili Wen, Bing Xiao, Yuxiu Shi
BACKGROUND: Post-traumatic stress disorder (PTSD) can be categorised as a disorder of dysregulated fear processing. In the formation and development of PTSD, whether fear/anxious-related memory is regulated by β-arrestin-2, and happened along the signal transduction pathways remains unknown. METHOD: We used single prolonged stress (SPS) as the animal model of PTSD. Next, elevated plus maze tests (EPM) was performed to examine fear/anxious memory- related behaviors...
April 15, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28152479/inhibitor-of-phosphodiestearse-4-improves-memory-deficits-oxidative-stress-neuroinflammation-and-neuropathological-alterations-in-mouse-models-of-dementia-of-alzheimer-s-type
#6
Amit Kumar, Nirmal Singh
The study investigates the potential of Rolipram a phosphodiesterase-4 inhibitor in cognitive deficits induced by streptozotocin (STZ, 3mg/kg intracerebroventricularly) and natural ageing in mice. Morris water maze (MWM) test was employed to evaluate learning and memory of the animals. Extent of oxidative stress was measured by estimating the levels of brain glutathione (GSH) and thiobarbituric acid reactive species (TBARS). Brain acetylcholinestrase (AChE) activity was also estimated. The brain activity of myeloperoxidase (MPO) was measured as a marker of inflammation...
April 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28046551/we-ab-bra-09-registration-of-preoperative-mri-to-intraoperative-radiographs-for-automatic-vertebral-target-localization
#7
T De Silva, A Uneri, M Ketcha, S Reaungamornrat, J Goerres, S Vogt, G Kleinszig, J Wolinsky, J H Siewerdsen
PURPOSE: Accurate localization of target vertebrae is essential to safe, effective spine surgery, but wrong-level surgery occurs with surprisingly high frequency. Recent research yielded the "LevelCheck" method for 3D-2D registration of preoperative CT to intraoperative radiographs, providing decision support for level localization. We report a new method (MR-LevelCheck) to perform 3D-2D registration based on preoperative MRI, presenting a solution for the increasingly common scenario in which MRI (not CT) is used for preoperative planning...
June 2016: Medical Physics
https://www.readbyqxmd.com/read/27766379/aryl-1-3-5-triazine-ligands-of-histamine-h4-receptor-attenuate-inflammatory-and-nociceptive-response-to-carrageen-zymosan-and-lipopolysaccharide
#8
Szczepan Mogilski, Monika Kubacka, Dorota Łażewska, Małgorzata Więcek, Monika Głuch-Lutwin, Małgorzata Tyszka-Czochara, Karolina Bukowska-Strakova, Barbara Filipek, Katarzyna Kieć-Kononowicz
OBJECTIVE AND DESIGN: Histamine H4 receptor (H4R) offers a great potential for new therapeutic strategies for the treatment of inflammation-based diseases. The aim of this study is to present the pharmacological profile of two recently synthesized ligands of H4R with particular reference to their anti-inflammatory and analgesic activity. MATERIALS AND SUBJECTS: We used mice and rats in the in vivo tests. We also used murine RAW 264.7 cells and isolated guinea-pig ileum in in vitro test...
January 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/27739411/inhibition-of-uterine-contractility-by-thalidomide-analogs-via-phosphodiesterase-4-inhibition-and-calcium-entry-blockade
#9
Eduardo Fernández-Martínez, Héctor Ponce-Monter, Luis E Soria-Jasso, Mario I Ortiz, José-Antonio Arias-Montaño, Guillermo Barragán-Ramírez, Cynthia Mayén-García
Uterine relaxation is crucial during preterm labor. Phosphodiesterase-4 (PDE-4) inhibitors have been proposed as tocolytics. Some thalidomide analogs are PDE-4 inhibitors. The aim of this study was to assess the uterus-relaxant properties of two thalidomide analogs, methyl 3-(4-nitrophthalimido)-3-(3,4-dimethoxyphenyl)-propanoate (4NO2PDPMe) and methyl 3-(4-aminophthalimido)-3-(3,4-dimethoxyphenyl)-propanoate (4APDPMe) and were compared to rolipram in functional studies of spontaneous phasic, K⁺-induced tonic, and Ca(2+)-induced contractions in isolated pregnant human myometrial tissues...
October 7, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27735066/anti-inflammatory-therapies-in-atopic-dermatitis
#10
REVIEW
A Heratizadeh, T Werfel
The pathogenesis of atopic dermatitis (AD) is multifactorial and complex. Consequently, clinical signs and symptoms vary strongly depending on individually relevant trigger factors and the stage of the disease. So far, treatment of AD was commonly limited to topical treatment or, in more severe cases, to systemic drugs mostly approved for other indications than AD. However, emerging data on new anti-inflammatory agents have been published in the recent years. As these new substances specifically focus on immune responses in AD, these are partially considered as possible 'breakthrough' in the treatment of AD...
December 2016: Allergy
https://www.readbyqxmd.com/read/27713015/in-vivo-effective-dibenzo-b-d-furan-1-yl-thiazoles-as-novel-pde-4-inhibitors
#11
Gopalan Balasubramanian, Sukunath Narayanan, Lavanya Andiappan, Thirunavukkarasu Sappanimuthu, Saravanan Thirunavukkarasu, Shamundeeswari Sundaram, Saravanakumar Natarajan, Naresh Sivaraman, Sridharan Rajagopal, Fakrudeen Ali Ahamed Nazumudeen, Sanjeev Saxena, Santosh L Vishwakarma, Shridhar Narayanan, Ganapavarapu V R Sharma, Chidambaram V Srinivasan, Narasimhan Kilambi
Herein we report the synthesis, PDE-4B and TNF-α inhibitory activities of a few dibenzo[b,d]furan-1-yl-thiazole derivatives. The hydroxycyclohexanol amide derivatives 14, 18, 24, 29, 31 and 33 exhibited promising in vitro PDE-4B and TNF-α inhibitory activities. Compound 24 showed good systemic availability in preclinical animal models and was also found to be non-toxic (exploratory mutagenicity test). Further it exhibited promising results in in vivo asthma/COPD and Uveitis models.
September 9, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27695125/synthesis-pharmacological-profile-and-docking-studies-of-new-sulfonamides-designed-as-phosphodiesterase-4-inhibitors
#12
Isabelle Karine da Costa Nunes, Everton Tenório de Souza, Suzana Vanessa S Cardozo, Vinicius de Frias Carvalho, Nelilma Correia Romeiro, Patrícia Machado Rodrigues E Silva, Marco Aurélio Martins, Eliezer J Barreiro, Lídia Moreira Lima
Prior investigations showed that increased levels of cyclic AMP down-regulate lung inflammatory changes, stimulating the interest in phosphodiesterase (PDE)4 as therapeutic target. Here, we described the synthesis, pharmacological profile and docking properties of a novel sulfonamide series (5 and 6a-k) designed as PDE4 inhibitors. Compounds were screened for their selectivity against the four isoforms of human PDE4 using an IMAP fluorescence polarized protocol. The effect on allergen- or LPS-induced lung inflammation and airway hyper-reactivity (AHR) was studied in A/J mice, while the xylazine/ketamine-induced anesthesia test was employed as a behavioral correlate of emesis in rodents...
2016: PloS One
https://www.readbyqxmd.com/read/27613392/pharmacological-strategies-to-reduce-exacerbation-risk-in-copd-a-narrative-review
#13
REVIEW
Marc Miravitlles, Anthony D'Urzo, Dave Singh, Vladimir Koblizek
Identifying patients at risk of exacerbations and managing them appropriately to reduce this risk represents an important clinical challenge. Numerous treatments have been assessed for the prevention of exacerbations and their efficacy may differ by patient phenotype. Given their centrality in the treatment of COPD, there is strong rationale for maximizing bronchodilation as an initial strategy to reduce exacerbation risk irrespective of patient phenotype. Therefore, in patients assessed as frequent exacerbators (>1 exacerbation/year) we propose initial bronchodilator treatment with a long-acting muscarinic antagonist (LAMA)/ long-acting β2-agonist (LABA)...
September 10, 2016: Respiratory Research
https://www.readbyqxmd.com/read/27597413/development-of-highly-potent-phosphodiesterase-4-inhibitors-with-anti-neuroinflammation-potential-design-synthesis-and-structure-activity-relationship-study-of-catecholamides-bearing-aromatic-rings
#14
Zhong-Zhen Zhou, Bing-Chen Ge, Qiu-Ping Zhong, Chang Huang, Yu-Fang Cheng, Xue-Mei Yang, Hai-Tao Wang, Jiang-Ping Xu
In this study, catecholamides (7a-l) bearing different aromatic rings (such as pyridine-2-yl, pyridine-3-yl, phenyl, and 2-chlorophenyl groups) were synthesized as potent phosphodiesterase (PDE) 4 inhibitors. The inhibitory activities of these compounds were evaluated against the core catalytic domains of human PDE4 (PDE4CAT), full-length PDE4A4, PDE4B1, PDE4C1, and PDE4D7 enzymes, and other PDE family members. Eight of the synthesized compounds were identified as having submicromolar IC50 values in the mid-to low-nanomolar range...
November 29, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27592021/systematic-review-and-quality-appraisal-of-cost-effectiveness-analyses-of-pharmacologic-maintenance-treatment-for-chronic-obstructive-pulmonary-disease-methodological-considerations-and-recommendations
#15
REVIEW
Simon van der Schans, Lucas M A Goossens, Melinde R S Boland, Janwillem W H Kocks, Maarten J Postma, Job F M van Boven, Maureen P M H Rutten-van Mölken
BACKGROUND: Worldwide, chronic obstructive pulmonary disease (COPD) is a highly prevalent chronic lung disease with considerable clinical and socioeconomic impact. Pharmacologic maintenance drugs (such as bronchodilators and inhaled corticosteroids) play an important role in the treatment of COPD. The cost effectiveness of these treatments has been frequently assessed, but studies to date have largely neglected the impact of treatment sequence and the exact stage of disease in which the drugs are used in real life...
January 2017: PharmacoEconomics
https://www.readbyqxmd.com/read/27525671/assessing-the-new-and-emerging-treatments-for-atopic-dermatitis
#16
Lawrence F Eichenfield, Sheila F Friedlander, Eric L Simpson, Alan D Irvine
The newer and emerging treatments for atopic dermatitis (AD) focus on blockade of inflammatory cytokines, especially those that derive from T helper cell type 2 (TH2) and are associated with a pathway of immunoglobulin E (IgE) sensitization. Among the proinflammatory cytokines that have been identified as promising therapeutic targets are chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2), IgE, thymic stromal lymphopoietin (TSLP), and several monoclonal antibodies that block key cytokine pathways in the innate immune response...
June 2016: Seminars in Cutaneous Medicine and Surgery
https://www.readbyqxmd.com/read/27445731/multiple-drug-treatments-that-increase-camp-signaling-restore-long-term-memory-and-aberrant-signaling-in-fragile-x-syndrome-models
#17
Catherine H Choi, Brian P Schoenfeld, Aaron J Bell, Joseph Hinchey, Cory Rosenfelt, Michael J Gertner, Sean R Campbell, Danielle Emerson, Paul Hinchey, Maria Kollaros, Neal J Ferrick, Daniel B Chambers, Steven Langer, Steven Sust, Aatika Malik, Allison M Terlizzi, David A Liebelt, David Ferreiro, Ali Sharma, Eric Koenigsberg, Richard J Choi, Natalia Louneva, Steven E Arnold, Robert E Featherstone, Steven J Siegel, R Suzanne Zukin, Thomas V McDonald, Francois V Bolduc, Thomas A Jongens, Sean M J McBride
Fragile X is the most common monogenic disorder associated with intellectual disability (ID) and autism spectrum disorders (ASD). Additionally, many patients are afflicted with executive dysfunction, ADHD, seizure disorder and sleep disturbances. Fragile X is caused by loss of FMRP expression, which is encoded by the FMR1 gene. Both the fly and mouse models of fragile X are also based on having no functional protein expression of their respective FMR1 homologs. The fly model displays well defined cognitive impairments and structural brain defects and the mouse model, although having subtle behavioral defects, has robust electrophysiological phenotypes and provides a tool to do extensive biochemical analysis of select brain regions...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27415981/treating-2-diseases-with-1-drug-pde-4-inhibitor-for-copd-and-psoriasis
#18
LETTER
Kathryn Michels, Miles Hagner, Mohamad El Zein, Osama Dasa, Ragheb Assaly
No abstract text is available yet for this article.
January 2017: American Journal of Therapeutics
https://www.readbyqxmd.com/read/27388992/pde4-inhibition-as-potential-treatment-of%C3%A2-epidermolysis-bullosa-acquisita
#19
Hiroshi Koga, Andreas Recke, Gestur Vidarsson, Hendri H Pas, Marcel F Jonkman, Takashi Hashimoto, Anika Kasprick, Saeedeh Ghorbanalipoor, Hermann Tenor, Detlef Zillikens, Ralf J Ludwig
Pemphigoid diseases such as epidermolysis bullosa acquisita (EBA) may be difficult to treat. In pemphigoid diseases, mucocutaneous blistering is caused by autoantibodies to hemidesmosomal antigens; in EBA the autoantigen is type VII collagen. Despite growing insights into pemphigoid disease pathogenesis, corticosteroids are still a mainstay of treatment. In experimental EBA, myeloid cell activation is a key event leading to blistering. Activation of these cells depends on phosphodiesterase (PDE) 4. We therefore evaluated the potential for PDE4 inhibition in EBA: PDE4 was highly expressed in inflammatory cells and in the epidermis of patients compared with healthy skin samples...
November 2016: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/27169612/the-discovery-of-roflumilast-for-the-treatment-of-chronic-obstructive-pulmonary-disease
#20
Mario Cazzola, Luigino Calzetta, Paola Rogliani, Maria Gabriella Matera
INTRODUCTION: Cyclic adenosine monophosphate (cAMP) phosphodiesterase (PDE)4 is an intracellular target that can be exploited to the treat chronic obstructive pulmonary disease (COPD), given that it is expressed in all inflammatory cells implicated in this inflammatory airways disease. At the present time, roflumilast is the only PDE4 inhibitor that has received regulatory approval for use in patients with COPD. AREAS COVERED: The preclinical, clinical and post-marketing development of roflumilast is described...
July 2016: Expert Opinion on Drug Discovery
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