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Showing 1-30 of 144 results for "d9766" within Papers
John J Sunderland et al.
Journal of nuclear cardiology : official publication of the American Society of Nuclear Cardiology, 22(1), 72-84 (2014-10-09)
Recent technological improvements to PET imaging equipment combined with the availability of software optimized to calculate regional myocardial blood flow (MBF) and myocardial flow reserve (MFR) create a paradigm shifting opportunity to provide new clinically relevant quantitative information to cardiologists.
Lihong Zhang et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(48), 19023-19028 (2007-11-21)
Autophagy is a lysosome-dependent cellular catabolic mechanism mediating the turnover of intracellular organelles and long-lived proteins. Reduction of autophagy activity has been shown to lead to the accumulation of misfolded proteins in neurons and may be involved in chronic neurodegenerative
Hui Quan et al.
PloS one, 10(5), e0127885-e0127885 (2015-05-29)
Recent studies have suggested that 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR) increases macrophage phagocytosis through adenosine monophosphate-activated protein kinase (AMPK). However, little information is available on the effects of AICAR on the clearance of apoptotic cells by macrophages, known as efferocytosis, which is essential
Damir Elmar Zecevic et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 87(2), 264-270 (2014-04-29)
Many upcoming drug candidates are pH-dependent poorly soluble weak bases in the pH range of the gastrointestinal tract. This often leads to a high in vivo variability and bioavailability issues. Aiming to overcome these limitations, the design of solid dispersions
Pavla Plačková et al.
Journal of enzyme inhibition and medicinal chemistry, 30(1), 57-62 (2014-04-01)
6-Chloropurines substituted at the position 9 with variously modified bicyclic skeletons represent promising antiviral and anticancer agents. This work aimed to investigate the transport mechanisms of 9-[(1R*,2R*,4S*)-bicyclo[2.2.1]hept-2-yl]-6-chloro-9H-purine (9-norbornyl-6-chloropurine, NCP) and their relationship to the metabolism and biological activity of the
Xiu-Jun Liu et al.
PloS one, 9(12), e115790-e115790 (2014-12-23)
The tumor microenvironment plays a crucial role during tumor development. Integrated combination of drugs that target tumor microenvironment is a promising approach to anticancer therapy. Here, we report a multifunctional combination of low-cytotoxic drugs composed of dipyridamole, bestatin and dexamethasone
Subrata Chakrabarti et al.
Vascular pharmacology, 48(4-6), 143-149 (2008-03-18)
Stroke is a leading cause of morbidity and mortality and the most common cause of neurological disability in older individuals. Prevention of recurrent stroke includes risk factor modification as well as the use of therapies that inhibit platelet activation. One
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
David T Manallack et al.
Journal of medicinal chemistry, 48(10), 3449-3462 (2005-05-13)
Dimitrios Psachoulias et al.
Pharmaceutical research, 29(12), 3486-3498 (2012-08-15)
To develop an in vitro methodology for prediction of concentrations and potential precipitation of highly permeable, lipophilic weak bases in fasted upper small intestine based on ketoconazole and dipyridamole luminal data. Evaluate usefulness of methodology in predicting luminal precipitation of
Lourdes Santana et al.
Journal of medicinal chemistry, 51(21), 6740-6751 (2008-10-07)
The work provides a new model for the prediction of the MAO-A and -B inhibitor activity by the use of combined complex networks and QSAR methodologies. On the basis of the obtained model, we prepared and assayed 33 coumarin derivatives
Eva Estébanez-Perpiñá et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(41), 16074-16079 (2007-10-04)
Current approaches to inhibit nuclear receptor (NR) activity target the hormone binding pocket but face limitations. We have proposed that inhibitors, which bind to nuclear receptor surfaces that mediate assembly of the receptor's binding partners, might overcome some of these
Jonas Borregaard Eriksen et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 154, 105532-105532 (2020-09-02)
It is our hypothesis that the presence of an absorptive sink for in-vitro dissolution experiments is decisive to predict extent and duration of super-saturation of low soluble drugs in formulations expected to increase oral absorption, often called enabling formulations. Combined
Evan R Abt et al.
Cell chemical biology, 27(2), 197-205 (2019-11-18)
Biosynthesis of the pyrimidine nucleotide uridine monophosphate (UMP) is essential for cell proliferation and is achieved by the activity of convergent de novo and salvage metabolic pathways. Here we report the development and application of a cell-based metabolic modifier screening
Giovanni Cianchetta et al.
Journal of medicinal chemistry, 48(8), 2927-2935 (2005-04-15)
Trying to understand the complex interactions that substrates and inhibitors have with the efflux transporter P-glycoprotein has been the subject of various publications. In this work, we have confined our study to substrates by picking a diverse set of 129
Valeria Caso et al.
European journal of internal medicine, 23(7), 580-585 (2012-09-04)
Stroke is a leading cause of death worldwide and the first cause of disability in the Western world. Over the last 20 years, antiplatelet agents have reduced overall stroke rates in primary and secondary prevention in men. However, this has
Derek B J Bone et al.
Microvascular research, 95, 68-75 (2014-07-01)
Purine nucleosides and nucleobases play key roles in the physiological response to vascular ischemia/reperfusion events. The intra- and extracellular concentrations of these compounds are controlled, in part, by equilibrative nucleoside transporter subtype 1 (ENT1; SLC29A1) and by equilibrative nucleobase transporter
Hyung-Hwan Kim et al.
Arteriosclerosis, thrombosis, and vascular biology, 28(3), s39-s42 (2008-01-05)
Dipyridamole (DP) is a phosphodiesterase inhibitor that increases the intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanine monophosphate (cGMP) by preventing their conversion to AMP and GMP, respectively. By increasing cAMP and cGMP levels in platelets, DP reversibly
Branden S Moriarity et al.
PloS one, 9(5), e96114-e96114 (2014-05-07)
The advent of Transcription Activator-Like Effector Nucleases (TALENs), and similar technologies such as CRISPR, provide a straightforward and cost effective option for targeted gene knockout (KO). Yet, there is still a need for methods that allow for enrichment and isolation
S M Yvonne Zuurbier et al.
Nederlands tijdschrift voor geneeskunde, 157(25), A5836-A5836 (2013-06-20)
In patients with TIA or stroke of arterial origin various antiplatelet agents, or combinations of these, have been found to be effective to reduce the risk of new vascular complications. International guidelines currently recommend three treatment strategies with antiplatelet agents
Michael A Zimmerman et al.
Hepatology (Baltimore, Md.), 58(5), 1766-1778 (2013-05-25)
Ischemia and reperfusion-elicited tissue injury contributes to morbidity and mortality of hepatic surgery and during liver transplantation. Previous studies implicated extracellular adenosine signaling in liver protection. Based on the notion that extracellular adenosine signaling is terminated by uptake from the
Extracellular Degradation into Adenosine and the Activities of Adenosine Kinase and AMPK Mediate Extracellular NAD+-produced increases in the Adenylate Pool of BV2 Microglia under Basal Conditions
Zhang J, et al.
Frontiers in Cellular Neuroscience, 12 (2018)
Djeven P Deva et al.
Cardiology in the young, 24(5), 822-830 (2013-09-21)
Vasodilator stress perfusion cardiovascular magnetic resonance imaging is a clinically useful tool for detection of clinically significant myocardial ischaemia in adults. We report our 5-year retrospective experience with perfusion cardiovascular magnetic resonance in a large, quarternary adult congenital heart disease
J A Thorn et al.
General pharmacology, 27(4), 613-620 (1996-06-01)
1. In mammals, nucleoside transport is an important determinant of the pharmacokinetics, plasma and tissue concentration, disposition and in vivo biological activity of adenosine as well as nucleoside analogues used in antiviral and anticancer therapies. 2. Two broad types of
Yajie Yu et al.
Cell death & disease, 12(9), 821-821 (2021-09-01)
Metabolic reprogramming is an integral part of the growth-promoting program driven by the MYC family of oncogenes. However, this reprogramming also imposes metabolic dependencies that could be exploited therapeutically. Here we report that the pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH)
Yingqiu Liu et al.
Biochemical pharmacology, 86(7), 914-925 (2013-07-24)
AMP-activated protein kinase (AMPK) activates endothelial nitric oxide synthase (eNOS) via phosphorylation at the activating site. The eNOS-nitric oxide (NO)/soluble guanylate cyclase (sGC)-cGMP/cGMP-dependent protein kinase (PKG) signaling axis is a major antiaggregatory mechanism residing in platelets. Based on the hypothesis
Kelly D Flemming et al.
Journal of neurosurgery, 118(1), 43-46 (2012-09-25)
The goal of this study was to determine the risk of using antithrombotic agents in patients with established intracerebral cavernous malformations (ICMs). From a previously described cohort of 292 patients with radiographically defined ICMs, 40 required an antithrombotic after the
Alison Atterbury et al.
The Journal of physiology, 587(Pt 18), 4497-4508 (2009-08-05)
The purine adenosine is an extracellular signalling molecule involved in a large number of physiological and pathological conditions throughout the mammalian brain. However little is known about how adenosine release and its subsequent clearance change during brain development. We have
Tochukwu C Okwuosa et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 118, 134-143 (2018-03-16)
A method for the production of liquid capsules with the potential of modifying drug dose and release is presented. For the first time, the co-ordinated use of fused deposition modelling (FDM), 3D printing and liquid dispensing to fabricate individualised dosage
Andrew S Weyrich et al.
American journal of therapeutics, 16(2), 164-170 (2009-03-21)
The recognition that stroke and other ischemic events are manifestations of chronic progressive inflammation has had a great impact on the development of prevention strategies. The most recent American Heart Association guidelines recommend combination aspirin and extended-release dipyridamole over aspirin
Jing Yuan et al.
Nature chemical biology, 5(10), 765-771 (2009-09-08)
Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened seven parasite lines for differences in responses to 1,279 bioactive chemicals. Hundreds of compounds were
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