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https://www.readbyqxmd.com/read/27919660/a-comparison-of-vasodilation-mode-among-selexipag-ns-304-2-4-5-6-diphenylpyrazin-2-yl-isopropyl-amino-butoxy-n-methylsulfonyl-acetamide-its-active-metabolite-mre-269-and-various-prostacyclin-receptor-agonists-in-rat-porcine-and-human-pulmonary-arteries
#1
Chiaki Fuchikami, Kohji Murakami, Koyuki Tajima, Junko Homan, Keiji Kosugi, Kazuya Kuramoto, Michiko Oka, Keiichi Kuwano
Selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N- (methylsulfonyl)acetamide]) is a novel, orally available non-prostanoid prostacyclin receptor (IP receptor) agonist that has recently been approved for the treatment of pulmonary arterial hypertension (PAH). We examined the effect of the active metabolite of selexipag, MRE-269, and IP receptor agonists that are currently available as PAH therapeutic drugs on the relaxation of rat, porcine and human pulmonary artery. cAMP formation in human pulmonary artery smooth muscle cells was induced by all test compounds (MRE-269, epoprostenol, iloprost, treprostinil and beraprost sodium) and suppressed by IP receptor antagonists (CAY10441 and 2-[4-(1H-indol-4-yloxymethyl)-benzyloxycarbonylamino]-3-phenyl-propionic acid)...
December 2, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27913583/epigenetic-control-of-microsomal-prostaglandin-e-synthase-1-by-hdac-mediated-recruitment-of-p300
#2
Christian Fork, Andrea E Vasconez, Patrick Janetzko, Carlo Angioni, Yannick Schreiber, Nerea Ferreiros, Gerd Geisslinger, Matthias S Leisegang, Dieter Steinhilber, Ralf P Brandes
: Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely used medicine to treat pain, fever, inflammation and to inhibit platelet function. Understanding the expression regulation of enzymes of the prostanoid pathway is of great medical relevance. Histone acetylation crucially controls gene expression. We set out to identify the impact of histone deacetylases (HDACs) on the generation of prostanoids and examine the consequences on vascular function. Inhibition of HDACs (HDACi) with the pan HDAC inhibitor SAHA attenuated prostaglandin E2 (PGE2) generation in the murine vasculature and in human vascular smooth muscle cells...
December 2, 2016: Journal of Lipid Research
https://www.readbyqxmd.com/read/27903663/beyond-a-single-pathway-combination-therapy-in-pulmonary-arterial-hypertension
#3
REVIEW
Olivier Sitbon, Sean Gaine
There is a strong rationale for combining therapies to simultaneously target three of the key pathways implicated in the pathogenesis of pulmonary arterial hypertension (PAH). Evidence to support this strategy is growing, and a number of studies have demonstrated that combination therapy, administered as either a sequential or an initial regimen, can improve long-term outcomes in PAH. Dual combination therapy with a phosphodiesterase-5 inhibitor and an endothelin receptor antagonist is the most widely utilised combination regimen...
December 2016: European Respiratory Review: An Official Journal of the European Respiratory Society
https://www.readbyqxmd.com/read/27895464/selexipag-in-the-treatment-of-pulmonary-arterial-hypertension-design-development-and-therapy
#4
REVIEW
Elizabeth Ashley Hardin, Kelly M Chin
Pulmonary arterial hypertension is characterized by abnormalities in the small pulmonary arteries including increased vasoconstriction, vascular remodeling, proliferation of smooth muscle cells, and in situ thrombosis. Selexipag, a novel, oral prostacyclin receptor agonist, has been shown to improve hemodynamics in a phase II clinical trial and reduce clinical worsening in a large phase III clinical trial involving patients with pulmonary arterial hypertension. In this paper, we describe the prostacyclin signaling pathway, currently available oral prostanoid medications, and the development and clinical use of selexipag...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27882058/cyclooxygenase-2-a-role-in-cancer-stem-cell-survival-and-repopulation-of-cancer-cells-during-therapy
#5
REVIEW
Lisa Y Pang, Emma A Hurst, David J Argyle
Cyclooxygenase-2 (COX-2) is an inducible form of the enzyme that catalyses the synthesis of prostanoids, including prostaglandin E2 (PGE2), a major mediator of inflammation and angiogenesis. COX-2 is overexpressed in cancer cells and is associated with progressive tumour growth, as well as resistance of cancer cells to conventional chemotherapy and radiotherapy. These therapies are often delivered in multiple doses, which are spaced out to allow the recovery of normal tissues between treatments. However, surviving cancer cells also proliferate during treatment intervals, leading to repopulation of the tumour and limiting the effectiveness of the treatment...
2016: Stem Cells International
https://www.readbyqxmd.com/read/27872515/therapeutic-treatment-of-arthritic-mice-with-15-deoxy-%C3%AE-12-14-prostaglandin-j2-15d-pgj2-ameliorates-disease-through-the-suppression-of-th17-cells-and-the-induction-of-cd4-cd25-foxp3-cells
#6
Vanessa Carregaro, Marcelo H Napimoga, Raphael S Peres, Luciana Benevides, Laís Amorim Sacramento, Larissa G Pinto, Renata Grespan, Thiago M Cunha, João Santana da Silva, Fernando Q Cunha
The prostaglandin, 15-deoxy Δ(12,14)-prostaglandin J2 (15d-PGJ2), is a lipid mediator that plays an important role in the control of chronic inflammatory disease. However, the role of prostanoid in rheumatoid arthritis (RA) is not well determined. We demonstrated the therapeutic effect of 15d-PGJ2 in an experimental model of arthritis. Daily administration of 15d-PGJ2 attenuated the severity of CIA, reducing the clinical score, pain, and edema. 15d-PGJ2 treatment was associated with a marked reduction in joint levels of proinflammatory cytokines...
2016: Mediators of Inflammation
https://www.readbyqxmd.com/read/27872513/vaginal-lactoferrin-modulates-pge2-mmp-9-mmp-2-and-timp-1-amniotic-fluid-concentrations
#7
Alessandro Trentini, Martina Maritati, Carlo Cervellati, Maria C Manfrinato, Arianna Gonelli, Carlo A Volta, Fortunato Vesce, Pantaleo Greco, Franco Dallocchio, Tiziana Bellini, Carlo Contini
Inflammation plays an important role in pregnancy, and cytokine and matrix metalloproteases (MMPs) imbalance has been associated with premature rupture of membranes and increased risk of preterm delivery. Previous studies have demonstrated that lactoferrin (LF), an iron-binding protein with anti-inflammatory properties, is able to decrease amniotic fluid (AF) levels of IL-6. Therefore, we aimed to evaluate the effect of vaginal LF administration on amniotic fluid PGE2 level and MMP-TIMP system in women undergoing genetic amniocentesis...
2016: Mediators of Inflammation
https://www.readbyqxmd.com/read/27871289/inhibition-of-stat3-and-mapk-dependent-pge2-synthesis-ameliorates-phagocytosis-of-fibrillar-%C3%AE-amyloid-peptide-1-42-via-ep2-receptor-in-emf-stimulated-n9-microglial-cells
#8
Gen-Lin He, Zhen Luo, Ting-Ting Shen, Ping Li, Ju Yang, Xue Luo, Chun-Hai Chen, Peng Gao, Xue-Sen Yang
BACKGROUND: Prostaglandin E2 (PGE2)-involved neuroinflammatory processes are prevalent in several neurological conditions and diseases. Amyloid burden is correlated with the activation of E-prostanoid (EP) 2 receptors by PGE2 in Alzheimer's disease. We previously demonstrated that electromagnetic field (EMF) exposure can induce pro-inflammatory responses and the depression of phagocytosis in microglial cells, but the signaling pathways involved in phagocytosis of fibrillar β-amyloid (fAβ) in microglial cells exposed to EMF are poorly understood...
November 21, 2016: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/27865847/functional-characterisation-and-application-of-an-ex-vivo-perfusion-superfusion-system-in-murine-airways
#9
Esther Y Cheah, Tracy S Mann, Philip C Burcham, Peter J Henry
INTRODUCTION: The aim of this study was to develop two dynamic ex vivo airway explant systems, a perfusion-superfusion system and a ventilation-superfusion system, for the study of toxic airborne substances, such as the prevalent smoke constituent acrolein. METHODS: Mouse isolated tracheal segments were perfused with physiological media or ventilated with humidified air at 37°C to mimic dynamic flow conditions, and superfused with media over the exterior surface...
November 16, 2016: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/27865703/discovery-of-2-2-chloro-6-fluorophenyl-amino-n-3-fluoro-5-trifluoromethyl-phenyl-1-methyl-7-8-dihydro-1h-1-4-dioxino-2-3-3-4-benzo-1-2-d-imidazole-5-carboxamide-as-potent-selective-and-efficacious-microsomal-prostaglandin-e2-synthase-1-mpges-1-inhibitor
#10
Nagarajan Muthukaman, Sanjay Deshmukh, Neelam Sarode, Shital Tondlekar, Macchindra Tambe, Dnyandeo Pisal, Mahamadhanif Shaikh, Vidya G Kattige, Srinivasa Honnegowda, Vikas Karande, Abhay Kulkarni, Satyawan B Jadhav, Mahamad Yunnus A Mahat, Girish S Gudi, Neelima Khairatkar-Joshi, Laxmikant A Gharat
The discovery and SAR of potent, selective dioxane-fused tricyclic benz[d]imidazole derivatives as mPGES-1 inhibitor are herein described. Various amide modifications in this series afforded many potent mPGES-1 inhibitors, of which 17d proved to be suitable for further profiling in vivo. Compound 17d {2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2',3':3,4]benzo[1,2-d]imidazole-5-carboxamide} exhibited excellent mPGES-1 enzyme (IC50: 8nM), cell (A549 IC50: 16...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27818253/vasodilator-activity-of-hydrogen-sulfide-h2s-in-human-mesenteric-arteries
#11
Serena Materazzi, Giovanni Zagli, Romina Nassini, Ilenia Bartolini, Stefano Romagnoli, Cosimo Chelazzi, Silvia Benemei, Andrea Coratti, Angelo Raffaele De Gaudio, Riccardo Patacchini
The role of endogenous H2S has been highlighted as a gaseous transmitter. The vascular smooth muscle inhibitory effects of H2S have been characterized in isolated aorta and mesenteric arteries in rats and mice. Our study was aimed at investigating the vascular effects of H2S on human isolated mesenteric arteries and examining the underlying mechanisms involved. All experiments were performed on rings (4-8mm long) of human mesenteric arteries obtained from patients undergoing abdominal surgery. Ethical approval was obtained from the Ethics Committee of the University Hospital of the University of Florence (app...
November 3, 2016: Microvascular Research
https://www.readbyqxmd.com/read/27815021/interleukin-1%C3%AE-induces-sleep-independent-of-prostaglandin-d2-in-rats-and-mice
#12
Bin-Jia Zhang, Shu-Rong Shao, Kosuke Aritake, Atsuko Takeuchi, Yoshihiro Urade, Zhi-Li Huang, Michael Lazarus, Wei-Min Qu
Interleukin-1β (IL-1β) and prostaglandin (PG) D2 are endogenous sleep-promoting substances. Since it was reported that a highly selective cyclooxygenase-2 (COX-2) inhibitor, NS398, completely inhibited IL-1β-induced sleep in rats, IL-1β-induced sleep had been believed to be mediated by prostanoids, most probably PGD2. However, in the present study, pretreatment of rats with NS398 (3mg/kg) did not suppress the 64.2% increased non-rapid eye movement (non-REM, NREM) sleep during infusion of IL-1β (10ng) for 6h in the nocturnal (active) period between 23:00 and 5:00 into the subarachnoid space of the PGD2-sensitive sleep-promoting zone of the basal forebrain...
November 2, 2016: Neuroscience
https://www.readbyqxmd.com/read/27785045/buerger-s-disease-providing-integrated-care
#13
REVIEW
Peter Klein-Weigel, Theresa Sophie Volz, Leonora Zange, Jutta Richter
Buerger's disease, also known as thromboangiitis obliterans (TAO), is a segmental inflammatory disease affecting small- and medium-sized vessels, which is strongly associated with tobacco use. Although the etiology is still unknown, recent studies suggest an immunopathogenesis. Diagnosis is based on clinical and angiomorphologic criteria, including age, history of smoking, clinical presentation with distal extremity ischemia, and the absence of other risk factors for atherosclerosis, autoimmune disease, hypercoagulable states, or embolic disease...
2016: Journal of Multidisciplinary Healthcare
https://www.readbyqxmd.com/read/27771466/gender-related-differences-in-pulmonary-arterial-hypertension-targeted-drugs-administration
#14
REVIEW
Alberto M Marra, Nicola Benjamin, Christina Eichstaedt, Andrea Salzano, Michele Arcopinto, Luna Gargani, Michele D Alto, Paola Argiento, Lorenzo Falsetti, Paolo Di Giosia, Andrea M Isidori, Francesco Ferrara, Eduardo Bossone, Antonio Cittadini, Ekkehard Grünig
During the last 15 years, a real "paradigm-shift" occurred, due to the development of PAH-targeted drugs, leading to crucial improvements in symptoms, exercise capacity, hemodynamics and outcome of PAH patients. In order to describe differences regarding epidemiology and therapy in PAH according to gender, we performed a review of the available literature in "PubMed" and "Web of Science" databases. In order to find relevant articles, we combined each of the following the keywords "pulmonary arterial hypertension", "gender", "sex", "men", "woman", "male", "female", "phosphodiesterase inhibitors", "endothelin receptor antagonists", "prostanoids"...
October 19, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27770021/in-vivo-studies-validating-multitargeting-of-prostanoid-receptors-for-achieving-superior-anti-inflammatory-effects
#15
David F Woodward, Jenny W Wang, Ming Ni, Alex Bauer, Jose L Martos, Robert W Carling, Neil J Poloso
The purpose of these studies was to test the hypothesis that a selected polypharmacological approach for treating the prostanoid-mediated component of inflammatory diseases would produce a therapeutic effect superior to global inhibition of prostaglandin (PG) biosynthesis by aspirin-like drugs. The compound studied was AGN 211377, which had been previously shown to produce a superior effect on cytokine release from human macrophages compared with cyclooxygenase (COX) inhibitors. AGN 211377 antagonizes prostanoid prostaglandin D2 (DP)1, DP2, prostaglandin E2 (EP)1, EP4, prostaglandin F2α, and thromboxane A2 receptors but not anti-inflammatory EP2, prostaglandin I2, or EP3 receptors...
October 21, 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27768866/adding-lyso-lipids-to-arachidonate-metabolism-sets-the-stage-for-new-biology
#16
James A Shayman
Prostaglandins have been characterized as the metabolic products of arachidonic acid released from glycerophospholipids following hydrolysis by phospholipase A2s and enzymatic oxidation by the COX1 and COX2. In this issue of Cell Chemical Biology, Liu et al. (2016) examine the metabolism of 2-arachidonoyl-lyso-phosphatidylcholine and 2-arachidonoyl-lyso-phosphatidylethanolamine by COX2 and conversion to glycerolipid linked prostanoids, raising a series of interesting and important questions.
October 20, 2016: Cell Chemical Biology
https://www.readbyqxmd.com/read/27765359/cardioprotective-actions-of-curcumin-on-the-pathogenic-nfat-cox-2-prostaglandin-e2-pathway-induced-during-trypanosoma-cruzi-infection
#17
Matías Hernández, Susana Wicz, Ricardo S Corral
BACKGROUND: Diverse cardiovascular signaling routes have been considered critical for Chagas cardiomyopathy caused by the protozoan parasite Trypanosoma cruzi. Along this line, T. cruzi infection and endothelin-1 (ET-1) have been shown to cooperatively activate the Ca(2+)/NFAT cascade in cardiomyocytes, leading to cyclooxygenase type 2 (COX-2) induction and increased release of prostanoids and prohypertrophic peptides. PURPOSE: To determine whether the well-known cardioprotective and anti-inflammatory effects of curcumin (Cur) could be helpful to interfere with this key machinery for pathogenesis of Chagas myocarditis...
November 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27763812/prostanoid-receptor-antagonist-effects-on-intraocular-pressure-supported-by-ocular-biodisposition-experiments
#18
David F Woodward, Stacey L Wenthur, Tara L Rudebush, Shan Fan, Carol B Toris
PURPOSE: Since all prostanoid receptors affect intraocular pressure (IOP) and endogenous prostanoids are found in ocular tissues, the pressor effects of prostanoid antagonists were comprehensively evaluated. The absence of effects of most of these antagonists was not entirely anticipated. To ensure no false-negative results, ocular biodisposition studies were conducted. METHODS: Monkeys with laser-induced ocular hypertension were used to study antagonist effects on IOP...
October 20, 2016: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27760451/-pulmonary-hypertension-due-to-chronic-lung-disease-recommendations-of-the-cologne-consensus-conference-2016
#19
H Olschewski, J Behr, H Bremer, M Claussen, P Douschan, M Halank, M Held, M M Hoeper, S Holt, H Klose, S Krüger, T J Lange, F Reichenberger, D Skowasch, S Ulrich, H Wilkens, W Seeger
The 2015 European Guidelines on Pulmonary Hypertension did not cover only pulmonary arterial hypertension (PAH) but also some aspects of pulmonary hypertension (PH) associated with chronic lung disease. The European Guidelines point out that the drugs currently used to treat patients with PAH (prostanoids, endothelin receptor antagonists, phosphodiesterase-5 inhibitors, sGC stimulators) have not been sufficiently investigated in other forms of PH. Therefore, the European Guidelines do not recommend the use of these drugs in patients with chronic lung disease and PH...
October 2016: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/27756404/local-intra-uterine-ang-1-7-infusion-attenuates-pge2-and-6-keto-pgf1%C3%AE-in-decidualized-uterus-of-pseudopregnant-rats
#20
K Bridget Brosnihan, Victor M Pulgar, Manish S Bharadwaj, Liomar A A Neves, Liliya M Yamaleyeva
BACKGROUND: Cyclooxygenase (COX)-derived prostanoids (PGE2, PGI2) are important contributors to the process of decidualization. Previous studies showed the presence of Ang-(1-7) in the primary and secondary decidualized zones of the implantation site at early pregnancy. Decreased concentrations of Ang-(1-7) were found in the decidualized uterus compared to the non-decidualized uterus of pseudopregnant rats, suggesting that low levels of Ang-(1-7) are required for successful decidualization at early pregnancy...
October 18, 2016: Reproductive Biology and Endocrinology: RB&E
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