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https://www.readbyqxmd.com/read/28520337/pde-5-inhibitors-should-be-used-post-radical-prostatectomy-as-erection-function-rehabilitation-opinion-no
#1
EDITORIAL
Jonathan Clavell-Hernández, Run Wang
No abstract text is available yet for this article.
May 2017: International Braz J Urol: Official Journal of the Brazilian Society of Urology
https://www.readbyqxmd.com/read/28520336/pde-5-inhibitors-should-be-used-post-radical-prostatectomy-as-erection-function-rehabilitation-opinion-yes
#2
EDITORIAL
Laith M Alzweri, Arthur L Burnett
No abstract text is available yet for this article.
May 2017: International Braz J Urol: Official Journal of the Brazilian Society of Urology
https://www.readbyqxmd.com/read/28515693/rolipram-improves-outcome-in-a-rat-model-of-infant-sepsis-induced-cardiorenal-syndrome
#3
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/28507431/targeted-drugs-for-pulmonary-arterial-hypertension-a-network-meta-analysis-of-32-randomized-clinical-trials
#4
Xiao-Fei Gao, Jun-Jie Zhang, Xiao-Min Jiang, Zhen Ge, Zhi-Mei Wang, Bing Li, Wen-Xing Mao, Shao-Liang Chen
BACKGROUND: Pulmonary arterial hypertension (PAH) is a devastating disease and ultimately leads to right heart failure and premature death. A total of four classical targeted drugs, prostanoids, endothelin receptor antagonists (ERAs), phosphodiesterase 5 inhibitors (PDE-5Is), and soluble guanylate cyclase stimulator (sGCS), have been proved to improve exercise capacity and hemodynamics compared to placebo; however, direct head-to-head comparisons of these drugs are lacking. This network meta-analysis was conducted to comprehensively compare the efficacy of these targeted drugs for PAH...
2017: Patient Preference and Adherence
https://www.readbyqxmd.com/read/28494463/plasma-drug-concentrations-in-patients-with-pulmonary-arterial-hypertension-on-combination-treatment
#5
Ekkehard Grünig, Johanna Ohnesorge, Nicola Benjamin, Jürgen Burhenne, Yeliz Enderle, Benjamin Egenlauf, Christine Fischer, Satenik Harutyunova, Andrea Huppertz, Hans Klose, Walter E Haefeli
BACKGROUND: Combination therapy with the phosphodiesterase type 5 inhibitors (PDE-5i) sildenafil or tadalafil and the endothelin receptor antagonists (ERA) bosentan, ambrisentan, or macitentan may cause mutual pharmacokinetic interactions in patients with pulmonary arterial hypertension (PAH). OBJECTIVE: The objective of this study was to analyze plasma drug concentrations in PAH patients receiving different combination treatments. METHODS: PAH patients receiving a stable combination treatment with ERA and PDE-5i with targeted dosage for at least 1 month were routinely assessed, including clinical parameters and plasma drug concentrations...
May 12, 2017: Respiration; International Review of Thoracic Diseases
https://www.readbyqxmd.com/read/28486684/superior-vasodilation-of-human-pulmonary-vessels-by-vardenafil-compared-with-tadalafil-and-sildenafil-additive-effects-of-bosentan%C3%A2
#6
Michael Ried, Reiner Neu, Karla Lehle, Christian Großer, Tamas Szöke, Gunter Lang, Hans-Stefan Hofmann, Markus Hoenicka
OBJECTIVES: Pulmonary arterial hypertension is characterized by pulmonary vascular proliferation and remodelling, leading to a progressive increase in pulmonary arterial resistance. Vasodilator properties of 3 different phosphodiesterase (PDE)-5 inhibitors alone and in combination with an endothelin (ET) receptor antagonist were compared in an ex vivo model. METHODS: Segments of human pulmonary arteries (PAs) and pulmonary veins (PVs) were harvested from lobectomy specimens...
May 9, 2017: Interactive Cardiovascular and Thoracic Surgery
https://www.readbyqxmd.com/read/28485811/the-effects-of-second-messenger-camp-and-its-relative-components-on-the-contraction-of-uterine-smooth-muscle-of-rat
#7
S-J Shu, X-G Lei, J-H Liang, Y-H Song, Q Xu, X-D Chen, L-G Mao, Z-G Li
OBJECTIVE: To investigate the effect of second messenger pathways on the uterine smooth muscle contraction and their associated mechanisms, and compare the evaluation methods. MATERIALS AND METHODS: Preparation of uterine smooth muscle strips from healthy pregnant 18-21 d SD and non-pregnant rats. When the contraction of muscle strips was stable, we conducted gradient administration: PDE4 inhibitors (Z90), prostaglandin PGE2, adenylate cyclase inhibitor (SQ 22,530), cAMP analogs (dbcAMP) and AMPK agonists (AICAR), solvent dimethyl sulfoxide (DMSO) as controlled...
April 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28477148/a-low-ca-2-i-induced-enhancement-of-camp-activated-ciliary-beating-by-pde1a-inhibition-in-mouse-airway-cilia
#8
Haruka Kogiso, Shigekuni Hosogi, Yukiko Ikeuchi, Saori Tanaka, Chikao Shimamoto, Hitoshi Matsumura, Takashi Nakano, Koh-Ichi Sano, Toshio Inui, Yoshinori Marunaka, Takashi Nakahari
This study demonstrated that PDE1 (phosphodiesterase 1) existing in the ciliary beat frequency (CBF)-regulating metabolon regulates CBF in procaterol-stimulated lung airway ciliary cells of mouse. Procaterol (an β2-agonist) increased the ciliary bend angle (CBA) and CBF via cAMP accumulation in the ciliary cells of mice: interestingly, the time course of CBF increase was slower than that of CBA increase. However, IBMX (3-isobutyl-1-methylxanthine, an inhibitor of PDE) increased CBA and CBF in an identical time course...
May 5, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28474020/characterization-of-the-structure-dynamics-and-allosteric-pathways-of-human-npp1-in-its-free-form-and-substrate-bound-complex-from-molecular-modeling
#9
Xavier Barbeau, Patrick Mathieu, Jean-François Paquin, Patrick Lagüe
The ectonucleotide phosphodiesterase/pyrophosphatase-1 (NPP1) is a type II transmembrane glycoprotein that regulates extracellular inorganic purine nucleotide and inorganic diphosphate levels through the hydrolysis of ATP into AMP and diphosphate. NPP1 is a promising drug target as it plays a role in several disorders. In the present work, we report the 3D structure modeling and extensive molecular dynamics simulations of NPP1-h, both in its free and ATP-bound forms. We identified the key residues involved in the binding of the ATP and the binding modes...
May 5, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28462841/design-and-optimization-of-purine-derivatives-as-in-vivo-active-pde10a-inhibitors
#10
Liu Chen, Danqi Chen, Le Tang, Jing Ren, Jiaojiao Chen, Xuechu Zhen, Yu-Chih Liu, Chenhua Zhang, Haibin Luo, Jingkang Shen, Bing Xiong
Phosphodiesterases are important enzymes regulating signal transduction mediated by second messenger molecules cAMP or cGMP. PDE10A is a unique member in the PDE family because of its selective expression in medium spiny neurons. It is recognized as anti-psychotic drug target. Based on the structural similarity between our previous chemistry work on 8-aminoimidazo[1,2-a]pyrazines and the PDE10A inhibitors reported by Bartolome-Nebreda et al., we initialized a project for developing PDE10A inhibitors. After several rounds of optimization, we were able to obtain a few compounds with good PDE10A enzymatic activity...
April 13, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28453742/blinded-contractility-analysis-in-hipsc-cardiomyocytes-in-engineered-heart-tissue-format-comparison-with-human-atrial-trabeculae
#11
Ingra Mannhardt, Alexandra Eder, Berengere Dumotier, Maksymilian Prondzynski, Elisabeth Krämer, Martin Traebert, Klaus-Dieter Söhren, Frederik Flenner, Konstantina Stathopoulou, Marc D Lemoine, Lucie Carrier, Torsten Christ, Thomas Eschenhagen, Arne Hansen
Objective: Human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CM) may serve as a new assay for drug testing in a human context, but their validity particularly for the evaluation of inotropic drug effects remains unclear. In this blinded analysis, we compared the effects of 10 indicator compounds with known inotropic effects in electrically stimulated (1.5 Hz) hiPSC-CM-derived 3 dimensional engineered heart tissue (EHT) and human atrial trabeculae (hAT). Methods and results: Human EHTs were prepared from iCell® hiPSC-CM, hAT obtained at routine heart surgery...
April 27, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28451983/therapeutic-targeting-of-pdes-and-pi3k-in-heart-failure-with-preserved-ejection-fraction-hfpef
#12
REVIEW
Valentina Sala, Jean Piero Margaria, Alessandra Murabito, Fulvio Morello, Alessandra Ghigo, Emilio Hirsch
PURPOSE OF REVIEW: Heart Failure with preserved Ejection Fraction (HFpEF) is a prevalent disease with considerable individual and societal burden. HFpEF patients often suffer from multiple pathological conditions thatcomplicate management and adversely affect outcome, including pulmonary hypertension and chronic obstructive pulmonary disease (COPD). To date, no treatment proved to be fully effective in reducing morbidity and mortality in HFpEF, possibly due to an incomplete understanding of the underlying molecular mechanisms...
April 27, 2017: Current Heart Failure Reports
https://www.readbyqxmd.com/read/28448580/sildenafil-normalizes-bowel-transit-in-preclinical-models-of-constipation
#13
Sarah K Sharman, Bianca N Islam, Yali Hou, Margaux Usry, Allison Bridges, Nagendra Singh, Subbaramiah Sridhar, Satish Rao, Darren D Browning
Guanylyl cyclase-C (GC-C) agonists increase cGMP levels in the intestinal epithelium to promote secretion. This process underlies the utility of exogenous GC-C agonists such as linaclotide for the treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). Because GC-C agonists have limited use in pediatric patients, there is a need for alternative cGMP-elevating agents that are effective in the intestine. The present study aimed to determine whether the PDE-5 inhibitor sildenafil has similar effects as linaclotide on preclinical models of constipation...
2017: PloS One
https://www.readbyqxmd.com/read/28443667/identification-of-a-phosphodiesterase-inhibiting-fraction-from-roasted-coffee-coffea-arabica-through-activity-guided-fractionation
#14
Teresa Röhrig, David Liesenfeld, Elke Richling
Recent reports that coffee can significantly inhibit cAMP phosphodiesterases (PDEs) in vitro, as well as in vivo, have described another beneficial effect of coffee consumption. However, the PDE-inhibiting substances remain mostly unknown. We chose activity-guided fractionation and an in vitro test system to identify the coffee components that are responsible for PDE inhibition. This approach indicated that a fraction of melanoidins reveals strong PDE-inhibiting potential (IC50 = 130 ± 42 μg/mL). These melanoidins were characterized as water-soluble, low-molecular weight melanoidins (<3 kDa) with a nitrogen content of 4...
May 8, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28424739/rapid-screening-of-potential-phosphodiesterase-inhibitors-from-the-roots-of-ilex-pubescens-hook-et-arn-using-a-combination-of-ultrafiltration-and-lc-ms
#15
Zichen Liu, Zongtao Lin, Shizhong Chen, Lingjun Wang, Shaoxiang Xian
The cyclic nucleotide phosphodiesterase (PDE) plays an important role in regulating the levels of second messenger molecules cAMP and cGMP. Various PDE inhibitors have been successfully developed into drugs for targeted diseases. In addition, PDE inhibitors can also be found in different foods and natural medicines. In this study, ultrafiltration liquid chromatography-diode-array detector-electrospray ionization-ion-trap-time-of-flight-mass spectrometry (ultrafiltration LC-DAD-ESI-IT-TOF-MS) was applied to screen PDE inhibitors from the roots of Ilex pubescens Hook...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28421158/cytotoxicity-of-zardaverine-in-embryonal-rhabdomyosarcoma-from-a-costello-syndrome-patient
#16
Donna M Cartledge, Katherine M Robbins, Katherine M Drake, Rachel Sternberg, Deborah L Stabley, Karen W Gripp, E Anders Kolb, Katia Sol-Church, Andrew D Napper
Costello syndrome (CS) patients suffer from a very high 10% incidence of embryonal rhabdomyosarcoma (ERMS). As tools to discover targeted therapeutic leads, we used a CS patient-derived ERMS cell line (CS242 ERMS) harboring a homozygous p.G12A mutation in HRAS, and a control cell line derived from the same patient comprising non-malignant CS242 fibroblasts with a heterozygous p.G12A HRAS mutation. A library of 2,000 compounds with known pharmacological activities was screened for their effect on CS242 ERMS cell viability...
2017: Frontiers in Oncology
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
#17
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/28406621/discovery-of-selective-phosphodiesterase-1-inhibitors-with-memory-enhancing-properties
#18
Brian Dyck, Bryan Branstetter, Tawfik Gharbaoui, Andrew R Hudson, J Guy Breitenbucher, Laurent Gomez, Iriny Botrous, Tami Marrone, Richard Barido, Charles K Allerston, E Peder Cedervall, Rui Xu, Vandana Sridhar, Ryan Barker, Kathleen Aertgeerts, Kara Schmelzer, David Neul, Dong Lee, Mark Eben Massari, Carsten B Andersen, Kristen Sebring, Xianbo Zhou, Robert Petroski, James Limberis, Martin Augustin, Lawrence E Chun, Thomas E Edwards, Marco Peters, Ali Tabatabaei
A series of potent thienotriazolopyrimidinone-based PDE1 inhibitors was discovered. X-ray crystal structures of example compounds from this series in complex with the catalytic domain of PDE1B and PDE10A were determined, allowing optimization of PDE1B potency and PDE selectivity. Reduction of hERG affinity led to greater than a 3000-fold selectivity for PDE1B over hERG. 6-(4-Methoxybenzyl)-9-((tetrahydro-2H-pyran-4-yl)methyl)-8,9,10,11-tetrahydropyrido[4',3':4,5]thieno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one was identified as an orally bioavailable and brain penetrating PDE1B enzyme inhibitor with potent memory-enhancing effects in a rat model of object recognition memory...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28394532/-phosphodiesterase-type-5-inhibitors-in-the-treatment-of-erectile-dysfunction-past-present-and-future
#19
S I Gamidov, R I Ovchinnikov, A Yu Popova, S Kh Izhbaev
This review article describes the differences in efficacy and side effects between available phosphodiesterase type 5 (PDE-5) inhibitors used for treating erectile dysfunction. The most studied PDE-5 inhibitor is sildenafil.
April 2017: Urologii︠a︡
https://www.readbyqxmd.com/read/28382232/resveratrol-enhances-the-inotropic-effect-but-inhibits-the-proarrhythmic-effect-of-sympathomimetic-agents-in-rat-myocardium
#20
Jesús Hernandez-Cascales
BACKGROUND: Resveratrol is a cardioprotective agent with known antiarrhythmic effects that has recently been shown to inhibit phosphodiesterase (PDE) enzyme activity. Thus, it is possible that resveratrol increases the inotropic effect of sympathomimetic agents, as PDE inhibitors do but, unlike other PDE inhibitors, its effect may not be accompanied by proarrhythmia due to its antiarrhythmic action. This work is aimed to test this hypothesis. METHODS: This is an "in vitro" concentration-response relationship study...
2017: PeerJ
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