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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
#1
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...
October 20, 2016: 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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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...
August 24, 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
#8
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...
September 3, 2016: PharmacoEconomics
https://www.readbyqxmd.com/read/27525671/assessing-the-new-and-emerging-treatments-for-atopic-dermatitis
#9
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
#10
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
#11
Kathryn Michels, Miles Hagner, Mohamad El Zein, Osama Dasa, Ragheb Assaly
No abstract text is available yet for this article.
July 12, 2016: American Journal of Therapeutics
https://www.readbyqxmd.com/read/27388992/pde4-inhibition-as-potential-treatment-of%C3%A2-epidermolysis-bullosa-acquisita
#12
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...
July 5, 2016: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/27169612/the-discovery-of-roflumilast-for-the-treatment-of-chronic-obstructive-pulmonary-disease
#13
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
https://www.readbyqxmd.com/read/27164008/a-novel-therapeutic-paradigm-for-patients-with-extensive-alopecia-areata
#14
Yael Renert-Yuval, Emma Guttman-Yassky
INTRODUCTION: Alopecia areata (AA) is a common, T-cell mediated, hair-centered skin disease that lacks efficacious, long-term therapies for extensive disease. Systemic immune suppressants are usually used, despite their nonspecific actions, often associated with substantial side effects. Although, the Th1 pathway was suggested as pivotal in the disease, recent studies suggest that Th2, Th9, phosphodiesterase (PDE) 4, and IL-23 axes might contribute to AA pathogenesis. AREAS COVERED: This paper provides an overview of activated immune pathways in AA and possible therapeutic modalities...
August 2016: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/27150141/pharmacological-profile-of-gpd-1116-an-inhibitor-of-phosphodiesterase-4
#15
Takashi Nose, Miwa Kondo, Masashi Shimizu, Hiroki Hamura, Yusuke Yamaguchi, Takako Sekine, Kouki Ishitani
We have previously reported that GPD-1116, an inhibitor of phosphodiesterase (PDE) 4, exhibits anti-inflammatory effects in a model of cigarette smoke-induced emphysema in senescence-accelerated P1 mice. In the present study, we further characterized the pharmacological profile of GPD-1116 in several experiments in vitro and in vivo. GPD-1116 and its metabolite GPD-1133 predominantly inhibited not only human PDE4, but also human PDE1 in vitro. Moreover, GPD-1116 was effective in several disease models in animals, including acute lung injury, chronic obstructive pulmonary disease (COPD), asthma and pulmonary hypertension; the effective doses of GPD-1116 were estimated to be 0...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27060014/synergistic-effect-between-5-ht4-receptor-agonist-and-phosphodiesterase-4-inhibitor-in-releasing-acetylcholine-in-pig-gastric-circular-muscle-in-vitro
#16
Romain A Lefebvre, Inge Van Colen, Vicky Pauwelyn, Joris H De Maeyer
5-HT4 receptor agonists have a gastroprokinetic effect by facilitating acetylcholine release from cholinergic nerves innervating gastrointestinal smooth muscle. The role of phosphodiesterase (PDE) 4 in the signal transduction pathway of the 5-HT4 receptors located on the cholinergic neurons towards the circular muscle layer in pig stomach was investigated by analysis of acetylcholine release. Circular muscle strips were prepared from pig proximal stomach and tritium outflow, induced by electrical field stimulation, was studied as a marker for acetylcholine release after incubation with [(3)H]-choline...
June 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27058148/rolipram-improves-cognition-reduces-anxiety-and-despair-like-behaviors-and-impacts-hippocampal-neuroplasticity-after-transient-global-cerebral-ischemia
#17
Lígia Mendes Soares, Jochen De Vry, Harry W M Steinbusch, Humberto Milani, Jos Prickaerts, Rúbia M Weffort de Oliveira
Cognitive impairment, anxiety- and depressive-like symptoms are well recognized outcome of cerebral ischemia in clinical and preclinical settings. Rolipram, a phosphodiesterase-4 (PDE-4) inhibitor, improves cognition and produces anxiolytic- and antidepressant-like effects in rodents. Rolipram also exerts anti-inflammatory effects and enhances survival of newborn hippocampal neurons in mice subjected to transient global cerebral ischemia. Here, we evaluated the effects of chronic rolipram treatment in mice subjected to transient global brain ischemia...
June 21, 2016: Neuroscience
https://www.readbyqxmd.com/read/27053149/two-new-isoxazolines-from-the-husks-of-xanthoceras-sorbifolia-bunge
#18
Hui-Qi Ge, Guo-Sheng Wan, Da Wang, Ji-Ming Wu, Bo-Hang Sun, Li-Jun Wu, Hui-Yuan Gao
Two new isoxazoline compounds, 1-oxa-2-azaspiro[4.5]dec-2-ene-8β-ol (1) and 1-oxa-2-azaspiro[4.5]dec-2-ene-8α-ol (2), were isolated from the husks of fruits of Xanthoceras sorbifolia Bunge and their structures were determined by spectroscopic analyses, including X-ray crystallography, HRESI-MS, UV, IR, and 1D and 2D NMR (HSQC, HMBC, NOESY) methods. Neither compound showed significant inhibitory effects on butyrylcholinesterase (BuchE) and acetylcholinesterase (AChE), nor the selected tumor cells growth. Based on an online activity prediction program (PASS ONLINE), the structures with isoxazoline skeletons were found to show potential anti-asthmatic (AM) and anti-anaphylaxis (AP) activities; moreover, compounds 1 and 2 were predicted to possess high affinities for many enzymes involved in AM and AP according to the RCSB Protein Data Bank...
August 2016: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/27006107/identification-and-in-vivo-evaluation-of-a-fluorine-18-rolipram-analogue-18-f-mni-617-as-a-radioligand-for-pde4-imaging-in-mammalian-brain
#19
David Thomae, Thomas J Morley, Hsiaoju S Lee, Olivier Barret, Cristian Constantinescu, Caroline Papin, Ronald M Baldwin, Gilles D Tamagnan, David Alagille
Phosphodiesterase (PDE) 4 is the most prevalent PDE in the central nervous system (CNS) and catalyzes hydrolysis of intracellular cAMP, a secondary messenger. By therapeutic inhibition of PDE4, intracellular cAMP levels can be stabilized, and the symptoms of psychiatric and neurodegenerative disorders including depression, memory loss and Parkinson's disease can be ameliorated. Radiotracers targeting PDE4 can be used to study PDE4 density and function, and evaluate new PDE4 therapeutics, in vivo in a non-invasive way, as has been shown using the carbon-11 labeled PDE4 inhibitor R-(-)-rolipram...
May 15, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/26954311/improvement-of-nail-and-scalp-psoriasis-using-apremilast-in-patients-with-chronic-psoriasis-phase-2b-and-3-52-week-randomized-placebo-controlled-trial-results
#20
Catherine M Nguyen, Argentina Leon, Melissa Danesh, Kourosh Beroukhim, Jashin J Wu, John Koo
INTRODUCTION: A significant portion of patients with psoriasis have scalp and nail involvement. It has been reported that 40% to 45% of patients with psoriasis have nail psoriasis, and up to 80% have scalp involvement. Nail and scalp psoriasis have often been found to be difficult to treat, due to the poor penetration and poor compliance of topical medication. Oral and biologic therapies have shown significant efficacy but often with undesirable side effects. Herein, we analyze the efficacy of apremilast, an oral phosphodiesterase-4 (PDE-4) inhibitor, in the treatment of nail and scalp psoriasis at 16-, 32-, and 52 weeks...
March 2016: Journal of Drugs in Dermatology: JDD
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