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91.
Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH‐102
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Dr. Isabell Haym Dr. Tri H. V. Huynh Dr. Stinne W. Hansen Dr. Martin H. F. Pedersen Dr. Josep A. Ruiz Dr. Mette N. Erichsen Dr. Mikko Gynther Walden E. Bjørn‐Yoshimoto Dr. Bjarke Abrahamsen Dr. Jesper F. Bastlund Dr. Christoffer Bundgaard Anette L. Eriksen Prof. Anders A. Jensen Prof. Lennart Bunch 《ChemMedChem》2016,11(4):403-419
Although the selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor UCPH‐101 has become a standard pharmacological tool compound for in vitro and ex vivo studies in the EAAT research field, its inability to penetrate the blood–brain barrier makes it unsuitable for in vivo studies. In the present study, per os (p.o.) administration (40 mg kg?1) of the closely related analogue UCPH‐102 in rats yielded respective plasma and brain concentrations of 10.5 and 6.67 μm after 1 h. Three analogue series were designed and synthesized to improve the bioavailability profile of UCPH‐102, but none displayed substantially improved properties in this respect. In vitro profiling of UCPH‐102 (10 μm ) at 51 central nervous system targets in radioligand binding assays strongly suggests that the compound is completely selective for EAAT1. Finally, in a rodent locomotor model, p.o. administration of UCPH‐102 (20 mg kg?1) did not induce acute effects or any visible changes in behavior. 相似文献
92.
93.
After hydrothermal pretreatment and enzymatic hydrolysis of wheat straw, a slurry rich in lignin but with a high content of inorganic substances, especially silica, and residual carbohydrates is produced. This slurry was used to develop an ethanol organosolv separation method to produce silica-free lignin fractions. The addition of para toluene sulphonic acid (PTSA) and the use of two alternative long-chain alcohols, oleyl alcohol or nonylphenol, were tested. In every reaction, two lignin fractions were produced and their molecular size and elemental composition were characterized. The yield of each fraction and the change in MWD were studied as a function of temperature and solid to liquid ratio. At 100, 150, and 200°C and with the use of PTSA, high-purity lignin fractions were obtained. After lignin fractionation with nonylphenol, a liquid silica-free product with high lignin content was obtained in yields between 17 and 72%. 相似文献
94.
Scheidler Stefan Anders Birte Regli Christian Bolay Stephan Huggenberger Peter 《Grundwasser》2019,24(4):277-286
Grundwasser - Topographically induced Alpine regional groundwater flow systems below the unconsolidated valley fillings constitute a substantial unused geothermal resource. Within the... 相似文献
95.
Ho Sn Lam G. Zimmermann G. Anders G. Bach D. Rennecke W. Zychlinski 《Advanced Synthesis \u0026amp; Catalysis》1985,327(5):759-766
Studies on Thermal Conversion of Phenyleyclopentane, -hexane, -heptane, and -octane in the Gas Phase The title compounds were pyrolyzed from 700 to 780°C in a metallic laboratory tubular reactor in the presence of steam. The reaction products were analyzed by gas chromatography and by a combination of gas chromatography and mass spectrometry. From the phenylcyclanes tested, more than 65 hydrocarbons could be detected in the liquids, besides gaseous reaction products. In most cases unambiguous structures could be derived by using different analytical methods. As typical initial-step products phenylcyclenes, ω-phenyl-1-alkenes and 1-phenyl-1-alkenes are formed by dehydrogenation and isomerization of the title compounds. The detection of phenylalkenes corresponds well with the isomerization of unsubstituted cyclanes to the corresponding α-olefines described in former papers. 相似文献
96.
Tingting Gu Jesper Just Katrine Tang Stenz Yan Yan Peter Sieljacks Jakob Wang Thomas Skjaerlund Groennebaek Jesper Emil Jakobsgaard Emil Rindom Jon Herskind Anders Gravholt Thomas Ravn Lassen Mathias Jrgensen Rikke Bk Eugenio Gutirrez-Jimnez Nina Kerting Iversen Peter Mondrup Rasmussen Jens Randel Nyengaard Malene Mller Jrgensen Frank de Paoli Hans Erik Btker Jrgen Kjems Kristian Vissing Kim Ryun Drasbek 《International journal of molecular sciences》2022,23(6)
Ischemic conditioning and exercise have been suggested for protecting against brain ischemia-reperfusion injury. However, the endogenous protective mechanisms stimulated by these interventions remain unclear. Here, in a comprehensive translational study, we investigated the protective role of extracellular vesicles (EVs) released after remote ischemic conditioning (RIC), blood flow restricted resistance exercise (BFRRE), or high-load resistance exercise (HLRE). Blood samples were collected from human participants before and at serial time points after intervention. RIC and BFRRE plasma EVs released early after stimulation improved viability of endothelial cells subjected to oxygen-glucose deprivation. Furthermore, post-RIC EVs accumulated in the ischemic area of a stroke mouse model, and a mean decrease in infarct volume was observed for post-RIC EVs, although not reaching statistical significance. Thus, circulating EVs induced by RIC and BFRRE can mediate protection, but the in vivo and translational effects of conditioned EVs require further experimental verification. 相似文献
97.
Analyses of samples of bed ash from a stationary fluidized bed boiler show the presence of calcium sulphide. In some samples, half of the total sulphur was present as sulphide. The samples containing CaS were obtained under unstaged conditions and with a high excess air ratio, 1.3 to 1.4. The samples were taken after a stop in the limestone addition, i.e. at high SO2 emissions of about 1000 mL/m3 (ppm). No CaS was found during limestone addition when the SO2 emission was 300–400 mL/m3. This indicates that formation of large amounts of CaS may be initiated as the SO2 concentration exceeds some critical level. 相似文献
98.
Anna Andersson Anders Magnusson Suzanne Troedsson Stefan Lundmark Frans H. J. Maurer 《应用聚合物科学杂志》2008,109(4):2269-2274
A combination of intumescent components was evaluated as a novel flame retardant system in a flexible polyurethane foam, and the incorporation of these components gave rise to a significant enhancement of the flame retardant properties of the foam. The heat release rate was lowered at an early stage as well as throughout the fire, the total heat production was decreased and the time to ignition was prolonged. Mechanical measurements of the foam revealed enhanced properties in terms of stiffness accompanied by a large decrease in elongation at break as compared with a reference foam. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008 相似文献
99.
Sigrid Lædre Ole Edvard Kongstein Anders Oedegaard Frode Seland Håvard Karoliussen 《International Journal of Hydrogen Energy》2012
Stainless steel is attractive as material for bipolar plates in proton exchange membrane fuel cells, due to its high electrical conductivity, high mechanical strength and relatively low material and processing cost. Potentiostatic and potentiodynamic tests were performed in H2SO4 solutions on AISI 316L stainless steel bipolar plates with etched flow fields. The effect of pH and presence of small amounts of fluoride and chloride on the corrosion rate and interfacial contact resistance of the stainless steel bipolar plate were investigated. The tests performed in electrolytes with various pH values revealed that the oxide layer was thinner and more prone to corrosion at pH values significantly lower than the pH one expects the bipolar plate to experience in an operating proton exchange membrane fuel cells. The use of solutions with very low pH in such measurements is thus probably not the best way of accelerating the corrosion rate of stainless steel bipolar plates. By use of strongly acidic solutions the composition and thickness of the oxide layer on the stainless steel is probably altered in a way that might never have happened in an operating proton exchange membrane fuel cell. Additions of fluoride and chloride in the amounts expected in an operating fuel cell (2 ppm F− and 10 ppm Cl−) did not cause significant changes for neither the polarization- nor the contact resistance measurements. However, by increasing the amount of Cl− to 100 ppm, pitting was initiated on the stainless steel surface. 相似文献
100.
This paper presents a fully automatic system intended to detect leaks of dielectric fluid in underground high-pressure, fluid-filled (HPFF) cables. The system combines a number of artificial intelligence (AI) and data processing techniques to achieve high detection capabilities for various rates of leaks, including leaks as small as 15 l per hour. The system achieves this level of precision mainly thanks to a novel auto-tuning procedure, enabling learning of the Bayesian network – the decision-making component of the system – using simulated leaks of various rates. Significant new developments extending the capabilities of the original leak detection system described in [1] and [2] form the basis of this paper. Tests conducted on the real-life HPFF cable system in New York City are also discussed. 相似文献