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Phosphodiesterase 4

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https://www.readbyqxmd.com/read/28638635/crystal-structure-of-an-apremilast-ethanol-hemisolvate-hemihydrate-solvatomorph
#1
Yun-Deng Wu, Xiao-Hong Liu, Jian Xu, Si-Han Zhang, Kun Shen, Ling Sun, Yong-Mei He, Yan Ma, Ai-Hua Zhang
The title compound, C22H24N2O7S·0.5C2H5OH·0.5H2O {systematic name: (S)-4-acetamido-2-[1-(3-eth-oxy-4-meth-oxy-phen-yl)-2-(methyl-sulfon-yl)eth-yl]iso-indo-line-1,3-dione ethanol hemisolvate hemihydrate}, is a novel solvatomorph of apremilast (AP), which is an inhibitor of phosphodiesterase 4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The asymmetric unit contains one mol-ecule of AP and disordered mol-ecules of ethanol and water, both with half occupancy. The dihedral angle between the planes of the phenyl ring and the iso-indole ring is 67...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28637505/human-lung-and-monocyte-derived-macrophages-differ-with-regard-to-the-effects-of-%C3%AE-2-adrenoceptor-agonists-on-cytokine-release
#2
Tatiana Victoni, Hélène Salvator, Charlotte Abrial, Marion Brollo, Luis Cristovão Sobrino Porto, Vincent Lagente, Emmanuel Naline, Stanislas Grassin-Delyle, Philippe Devillier
BACKGROUND: β2-adrenoceptor agonists have been shown to reduce the lipopolysaccharide (LPS)-induced cytokine release by human monocyte-derived macrophages (MDMs). We compare the expression of β2-adrenoceptors and the inhibitory effect of formoterol and salmeterol on the LPS-induced release of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and a range of chemokines (CCL2, 3, 4, and IL-8) by human lung macrophages (LMs) and MDMs. METHODS: LMs were isolated from patients undergoing resection and MDMs were obtained from blood monocytes in the presence of GM-CSF...
June 21, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28620954/propentofylline-phosphodiesterase-and-adenosine-reuptake-inhibitor-modulates-lymphocyte-subsets-and-lymphocyte-activity-after-in-vivo-administration-in-non-immunized-and-srbc-immunized-mice
#3
Marianna Szczypka, Magdalena Lis, Agnieszka Suszko-Pawłowska, Aleksandra Pawlak, Angelika Sysak, Bożena Obmińska-Mrukowicz
OBJECTIVES: The aim of the study was to investigate immunomodulatory effect of in-vivo administered propentofylline on the subsets and activity of murine lymphocytes. METHODS: Propentofylline (3 mg/kg) was administered orally to 8-week-old Balb/c mice, once or six times at 12-h intervals. The lymphocyte subsets, regulatory T cells, IL-5 and TNF levels were determined 12 h and 24 h after a single dose or after the sixth dose of the drug in non-immunized mice. Humoral immune response in sheep red blood cells (SRBC)-immunized mice was determined 4, 7 and 14 days after immunization...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28618988/synthesis-docking-and-anti-inflammatory-activity-of-triazole-amine-derivatives-as-potential-phosphodiesterase-4-inhibitors
#4
Ajmer Singh Grewal, Viney Lather, Deepti Pandita, Ruchi Dalal
BACKGROUND: Phosphodiesterase 4 (PDE4), one of the member of PDE superfamily catalyzes, the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate in pro-inflammatory and immunomodulatory cells leading to increased inflammatory processes. PDE4 has been reported as an attractive therapeutic target involved in various inflammatory disorders. OBJECTIVE: The present work was designed to synthesize and evaluate the anti-inflammatory activity of some new triazole amine derivatives as potential PDE4 inhibitors...
June 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28617319/pde4-inhibition-and-inflammatory-bowel-disease-a-novel-therapeutic-avenue
#5
REVIEW
Marco Spadaccini, Silvia D'Alessio, Laurent Peyrin-Biroulet, Silvio Danese
BACKGROUND: In the last few decades, a better knowledge of the inflammatory pathways involved in the pathogenesis of Inflammatory Bowel Disease (IBD) has promoted biological therapy as an important tool to treat IBD patients. However, in spite of a wider spectrum of biological drugs, a significant proportion of patients is unaffected by or lose their response to these compounds, along with increased risks of infections and malignancies. For these reasons there is an urgent need to look for new pharmacological targets...
June 15, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28613871/discovery-of-n-4-5-4-fluoro-phenyl-3-methyl-2-methylsulfanyl-3h-imidazol-4-yl-pyridin-2-yl-acetamide-cbs-3595-a-dual-p38%C3%AE-mapk-pde-4-inhibitor-with-activity-against-tnf%C3%AE-related-diseases
#6
Wolfgang Albrecht, Anke Unger, Silke M Bauer, Stefan A Laufer
The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 (PDE4) and the potential benefits arising from the blockage of both inflammation-related enzymes were thoroughly investigated. The most promising compound, CBS-3595 (1), was successively evaluated in in vitro experiments as well as in ex vivo and in vivo preclinical studies after administration of 1 to rodents, dogs and monkeys. The resulting data clearly indicated a potent suppression of tumor necrosis factor alpha (TNFα) release...
June 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28606099/pulmonary-hemodynamics-and-effects-of-phosphodiesterase-type-5-inhibition-in-heart-failure-a-meta-analysis-of-randomized-trials
#7
In-Chang Hwang, Yong-Jin Kim, Jun-Bean Park, Yeonyee E Yoon, Seung-Pyo Lee, Hyung-Kwan Kim, Goo-Yeong Cho, Dae-Won Sohn
BACKGROUND: Previous studies suggested that phosphodiesterase 5 inhibitors (PDE5i) have a beneficial effect in patients with heart failure (HF), although the results were inconsistent. We performed a meta-analysis to evaluate the effect of PDE5i in HF patients, and investigated the relationship between PDE5i effects and pulmonary hemodynamics. METHOD: We searched PubMed, EMBASE and the Cochrane Library for randomized controlled trials (RCTs) that compared PDE5i with placebo in HF with reduced ejection fraction (HFrEF) or HF with preserved EF (HFpEF)...
June 12, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28605578/roflupram-a-phosphodiesterase-4-inhibitior-suppresses-inflammasome-activation-through-autophagy-in-microglial-cells
#8
Tingting You, Yu-Fang Cheng, Jiahong Zhong, Bingtian Bi, Bingqing Zeng, Wenhua Zheng, Hai-Tao Wang, Jiang-Ping Xu
Inhibition of phosphodiesterase 4 (PDE4) suppressed the inflammatory responses in the brain. However, the underlying mechanisms are poorly understood. Roflupram (ROF) is a novel PDE4 inhibitor. In the present study, we found that ROF enhanced the level of microtubule-associated protein 1 light chain 3 II (LC3-II) and decreased p62 in microglial BV-2 cells. Enhanced fluorescent signals were observed in BV-2 cells treated with ROF by Lysotracker red and acridine orange staining. In addition, immunofluorescence indicated a significant increase in punctate LC3...
June 12, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28603838/compartmentalized-camp-responses-to-prostaglandin-ep2-receptor-activation-in-human-airway-smooth-muscle-cells
#9
Shailesh R Agarwal, Kathryn Miyashiro, Htun Latt, Rennolds S Ostrom, Robert D Harvey
BACKGROUND AND PURPOSE: Previous studies indicate that prostaglandin EP2 receptors (EP2 Rs) selectively couple to adenylyl cyclase type 2 (AC2) in non-lipid raft domains of airway smooth muscle (ASM) cells, where they regulate specific cAMP-dependent responses. The goal of the present study was to identify the cellular microdomains where EP2 Rs stimulate cAMP production. EXPERIMENTAL APPROACH: FRET-based cAMP biosensors were targeted to different subcellular locations of primary human ASM cells...
June 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28603047/tadalafil-induces-antiproliferation-apoptosis-and-phosphodiesterase-type-5-downregulation-in-idiopathic-pulmonary-arterial-hypertension-in-vitro
#10
Aya Yamamura, Eri Fujitomi, Naoki Ohara, Kikuo Tsukamoto, Motohiko Sato, Hisao Yamamura
Idiopathic pulmonary arterial hypertension (IPAH) is a fatal disease of the pulmonary artery resulting from a currently unidentified etiology. IPAH is pathologically characterized as sustained vasoconstriction and vascular remodeling of the pulmonary artery. Vascular remodeling is mediated by enhanced proliferation and reduced apoptosis in pulmonary arterial smooth muscle cells (PASMCs). Based on its pathological mechanism, specific phosphodiesterase type 5 (PDE5) inhibitors have been used in the treatment of IPAH...
June 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28597754/characteristics-of-pediatric-pulmonary-hypertension-trials-registered-on-clinicaltrials-gov
#11
Jordan D Awerbach, Richard A Krasuski, Kevin D Hill
The investigation of pediatric pulmonary hypertension (PH) drugs has been identified as a high priority by the United States National Institutes of Health (NIH). Studying pediatric PH is challenging due to the rare and heterogeneous nature of the disease. We sought to define the pediatric PH clinical trials landscape, to evaluate areas of trial success or failure, and to identify potential obstacles to the study of pediatric PH drugs. Interventional pediatric (ages 0-17 years) PH trials registered on ClinicalTrials...
April 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28597753/circulatory-power-and-ventilatory-power-over-time-under-goal-oriented-sequential-combination-therapy-for-pulmonary-arterial-hypertension
#12
Akihiro Hirashiki, Shiro Adachi, Yoshihisa Nakano, Yoshihiro Kamimura, Shigetake Shimokata, Kyosuke Takeshita, Atsuya Shimizu, Kenji Toba, Toyoaki Murohara, Takahisa Kondo
Many therapeutic options are available for patients with pulmonary arterial hypertension (PAH). However, little is known about the effects of sequential combination therapy on exercise capacity. Here we monitored exercise capacity by cardiopulmonary exercise testing (CPX) and observed the benefit of using a peak VO2 cutoff of 15 mL/kg/min to guide combination therapy. Thirty patients newly diagnosed with PAH were treated with goal-oriented sequential combination therapy. Endothelin receptor antagonists (ERA) were the first-line treatment, with phosphodiesterase type 5 inhibitors (PDE-5i) as the preferred combination partner...
April 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28597182/apremilast-a-novel-oral-treatment-for-psoriasis-and-psoriatic-arthritis
#13
REVIEW
Tiago Torres, Luis Puig
Psoriasis is a chronic immune-mediated disease associated with several co-morbidities and negative impacts on a patient's quality of life. Despite the advances in biologic therapy, there are still unmet needs in the treatment of psoriasis, as current treatments are limited in terms of long-term efficacy, tolerability, safety, route of administration, and cost. Apremilast is an oral, small-molecule phosphodiesterase 4 inhibitor that works intracellularly by blocking the degradation of cyclic adenosine 3',5'-monophosphate, resulting in increased intracellular cyclic adenosine 3',5'-monophosphate levels in phosphodiesterase 4-expressing cells...
June 8, 2017: American Journal of Clinical Dermatology
https://www.readbyqxmd.com/read/28594906/the-anti-inflammatory-and-immunomodulatory-potential-of-braylin-pharmacological-properties-and-mechanisms-by-in-silico-in-vitro-and-in-vivo-approaches
#14
Renan Fernandes Espírito-Santo, Cassio Santana Meira, Rafael Dos Santos Costa, Otávio Passos Souza Filho, Afranio Ferreira Evangelista, Gustavo Henrique Goulart Trossini, Glaucio Monteiro Ferreira, Eudes da Silva Velozo, Cristiane Flora Villarreal, Milena Botelho Pereira Soares
Braylin belongs to the group of natural coumarins, a group of compounds with a wide range of pharmacological properties. Here we characterized the pharmacological properties of braylin in vitro, in silico and in vivo in models of inflammatory/immune responses. In in vitro assays, braylin exhibited concentration-dependent suppressive activity on activated macrophages. Braylin (10-40 μM) reduced the production of nitrite, IL-1β, TNF-α and IL-6 by J774 cells or peritoneal exudate macrophages stimulated with LPS and IFN-γ...
2017: PloS One
https://www.readbyqxmd.com/read/28588484/akrinor-tm-a-cafedrine-theodrenaline-mixture-20-1-increases-force-of-contraction-of-human-atrial-myocardium-but-does-not-constrict-internal-mammary-artery-in-vitro
#15
Benjamin Kloth, Simon Pecha, Eileen Moritz, Yvonne Schneeberger, Klaus-Dieter Söhren, Edzard Schwedhelm, Hermann Reichenspurner, Thomas Eschenhagen, Rainer H Böger, Torsten Christ, Sebastian N Stehr
Background: Intraoperative hypotension is a common problem and direct or indirect sympathomimetic drugs are frequently needed to stabilize blood pressure. Akrinor(TM) consists of the direct and the indirect sympathomimetic noradrenaline and norephedrine. Both substances are covalently bound to the phosphodiesterase (PDE) inhibitor theophylline, yielding theodrenaline and cafedrine, respectively. We investigated pharmacodynamic effects of Akrinor(TM) and its constituents on contractile force and tension in human atrial trabeculae and internal A...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28587776/pharmacological-characterization-of-a-novel-potent-selective-and-orally-active-phosphodiesterase-2a-inhibitor-pdm-631
#16
Shunsuke Maehara, Keita Arakawa, Kotaro Hoshida, Hiroshi Nagasue, Noboru Chida, Kazunari Nakao, Shoji Furusako
Recently, we identified a novel phosphodiesterase 2A (PDE2A) inhibitor, PDM-631 ((S)-3-cyclopropyl-6-methyl-1-(1-(4-(trifluoromethoxy)phenyl)propan-2-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one). PDM-631 showed potent inhibitory activities for human and rat PDE2A with IC50 values of 1.5 and 4.2nM, respectively and more than 2000-fold selectivity against other phosphodiesterases. In rat studies, PDM-631 showed oral bioavailability and good brain penetration, and increased the cGMP levels in the cortex...
June 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28583339/off-label-use-of-phosphodiesterase-type-5-inhibitor-erectile-dysfunction-medication-to-enhance-sex-among-gay-and-bisexual-men-in-australia-results-from-the-flux-study
#17
Mohamed A Hammoud, Fengyi Jin, Toby Lea, Lisa Maher, Jeffrey Grierson, Garrett Prestage
BACKGROUND: Gay and bisexual men (GBM) use oral erectile dysfunction medications (EDMs) often with little evidence of medical indication necessitating their use. AIM: To investigate the prevalence, contexts, and motivations for oral EDM use and its relation to sexual risk behavior. METHODS: A total of 2,250 Australian GBM completed an online survey of licit and illicit drug use and their associated behaviors. Multivariate logistic regression analysis identified factors associated with use of EDMs in the previous 6 months and, for those who had used EDMs, factors associated with use on a weekly basis...
June 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/28580521/effects-of-nitrosyl-iron-complexes-with-thiocarbamide-and-its-aliphatic-derivatives-on-activities-of-ca-2-atpase-of-sarcoplasmic-reticulum-and-cgmp-phosphodiesterase
#18
L V Tatyanenko, N Yu Shmatko, N A Sanina, O V Dobrokhotova, I Yu Pikhteleva, A I Kotel'nikov, S M Aldoshin
We studied the effects of water-soluble cationic dinitrosyl iron complexes with thiocarbamide and its aliphatic derivatives, new synthetic analogs of natural NO donors, active centers of nitrosyl [1Fe-2S]proteins, on activities of Ca(2+)-ATPase of sarcoplasmic reticulum and cGMP phosphodiesterase. Nitrosyl iron complexes [Fe(C3N2H8S)Cl(NO)2](0)[Fe(NO)2(C3N2H8S)2](+)Cl(-) (I), [Fe(SC(N(CH3)2)2(NO)2]Cl (II), [Fe(SC(NH2)2)2(NO)2Cl×H2O (III), and [Fe(SC(NH2)2)2(NO)2]2SO4×H2O (IV) in a concentration of 10(-4) M completely inhibited the transporting and hydrolytic functions of Ca(2+)-ATPase...
June 5, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28565810/anti-atherogenic-properties-of-resveratrol-4-week-resveratrol-administration-associated-with-serum-concentrations-of-sirt1-adiponectin-s100a8-a9-and-vsmcs-contractility-in-a-rat-model
#19
Michał Wiciński, Bartosz Malinowski, Mateusz M Węclewicz, Elżbieta Grześk, Grzegorz Grześk
Resveratrol (3, 4', 5-trihydroxy-trans-stilbene) is a natural, non-flavonoid polyphenol that exerts protective properties against atherosclerosis-associated endothelial dysfunction and senescence. The present study aimed to assess the influence of resveratrol on vascular contractility and molecular factors including sirtuin-1 (SIRT1), adiponectin and calprotectin (S100A8/A9) that are considered to be important elements of atherogenesis. A total of 17 male rats were divided into a control and treatment group and administered resveratrol or a placebo...
May 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28560445/genistein-and-menaquinone-4-treatment-induced-alterations-in-the-expression-of-mrnas-and-their-products-are-beneficial-to-osteoblastic-mc3t3-e1-cell-functions
#20
Midori Katsuyama, Masashi Demura, Hironobu Katsuyama, Hideji Tanii, Kiyofumi Saijoh
The aim of the present study was to determine the molecular basis of the beneficial effects of genistein and/or menaquinone‑4 (MK‑4) on bone quality. Initially, 1 µM genistein was applied to MC3T3‑E1 cells for 24 h and the upregulated mRNAs that were detected by microarray were selected for further examination by reverse transcription‑quantitative‑polymerase chain reaction. Among them, alterations were observed in the level of GATA‑binding protein 6 (GATA6), Notch gene homolog 2 (NOTCH2), Wnt family member 5A (WNT5A), bone γ‑carboxyglutamate protein (BGLAP), chondroadherin (CHAD), dipeptidyl peptidase 4 (DPP4), ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2), alkaline phosphatase (ALP) 3 and ATPase phospholipid‑transporting 11A (ATP11A) in response to treatment with 0...
July 2017: Molecular Medicine Reports
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