gebhart/patrepeval huggingface dataset:
The mechanism of action and pharmacological specificity of the anticonvulsant NMDA antagonist MK‐801: a voltage clamp study on neuronal cells in culture (1989)

1. Some possible molecular mechanisms of action of the anxiolytic, anticonvulsant and neuroprotective agent MK-801 have been examined in 'whole-cell' voltage clamp recordings performed on rat hippocampal and cortical neurones, bovine adrenomedullary chromaffin cells and N1E-115 neuroblastoma cells maintained in cell culture. 2. Transmembrane currents recorded from rat hippocampal and cortical neurones in response to locally applied N-methyl-D-aspartate (NMDA) were antagonized by MK-801 (0.1-3.0 microM). Blockade was use-dependent, and little influenced by transmembrane potential. MK-801 (3 microM) had no effect on currents evoked by kainate (100 microM). 3. The antagonism of NMDA-induced currents by MK-801 was only slowly and incompletely reversed when the cell membrane potential was clamped at -60 mV during washout. Prolonged applications of NMDA at +40, but not -60 mV during washout, markedly accelerated recovery from block. 4. In contrast to MK-801, ketamine (10 microM) blocked NMDA-induced currents in a voltage-dependent manner. Blockade increased with membrane hyperpolarization and was completely reversible upon washout. 5. MK-801 (1-10 microM) produced a voltage- and concentration-dependent block of membrane currents elicited by ionophoretically applied acetylcholine (ACh) recorded from bovine chromaffin cells. The block was readily reversible upon washout. 6. gamma-Aminobutyric acidA (GABAA) receptor-mediated chloride currents of chromaffin cells were unaffected by MK-801 (1-100 microM). In contrast, such currents were potentiated by diazepam (1 microM). MK-801 (100 microM) had no effect on currents evoked by GABA on hippocampal neurones. 7. MK-801 (10 microM) had little effect on membrane currents recorded from N1E-115 neuroblastoma cells in response to ionophoretically applied 5-hydroxytryptamine (5-HT). Such currents were antagonized by the 5-HT3 receptor antagonist GR 38032F (1 nM) and also by MK-801 at high concentration (100 microM). 8. Voltage-activated, tetrodotoxin-sensitive, sodium currents of chromaffin cells were unaffected by 10 microM MK-801. However, at a relatively high concentration (100 microM), MK-801 reduced the amplitude of such currents to approximately 77% of control. 9. The relevance of the present results to the central actions of MK-801 is discussed.
[Inhibitory effects of human bone marrow mesenchymal stem cells and cord blood mononuclear cells on mixed lymphocyte response and PHA induction transformation]. (2004)

To study and compare the immunomodulatory functions of human bone marrow mesenchymal stem cell (MSC) and cord blood mononuclear cell (CBMNC) in vitro, human bone marrow MSC were separated with Percoll (1.073 g/L) and cultured in low-glucose DMEM, and cord blood mononuclear cells were isolated with Ficoll (1.077 g/L). These two kinds of cells were added to mixed lymphocyte cultures and PHA induction transformation cultures with various concentrations. The proliferation of lymphocytes was measured by MTT method, effects of MSC and CBMNC on mixed lymphocyte response and PHA-induced lymphocyte transformation were investigated. The results showed that both 5 x 10(4), 1 x 10(4) MSC and 2 x 10(5) CBMNC could inhibit the mixed lymphocyte response (MLR) and PHA induced transformation. But with lower concentrations (MSC < or = 1 x 10(3), CBMNC < or = 1 x 10(5)), the inhibition effects of MSC and CBMNC were less consistent. 1 x 10(2) MSC and 1 x 10(4) CBMNC mainly increased the lymphocyte activation. In addition, the inhibition ratio of 5 x 10(4) MSC (MLC 65.3%, PHA 79.1%) was higher than that of 2 x 10(5) CBMNC (MLC 8.6%, PHA 37.3%). It is concluded that larger numbers of both MSC and CBMNC showed negative immunomodulatory functions and inhibited the mixed lymphocyte response and induction of transformation in vitro. Moreover, the inhibitory effect of MSC was much stronger than that of CBMNC.
InGaAs monolithic photoreceiver integrating PIN/JFET with diffused junctions and a resistor (1988)

Monolithic InGaAs PIN/FETs are considered as competitors to APDs for high-speed long-haul optical transmissions at 1.3–1.6 μm.1,2 However, high- performance photodiodes and transistors call for conflicting requirements in terms of active layer thicknesses and doping levels; this incompatibility has so far hampered development of a high-sensitivity high-speed PIN/FET.
How Melting Points of AKD, the Corresponding Ketone and Their Mixtures Affect Spreading Behaviour (2001)

The redistribution of Alkylketene dimmers (AKD) on fibre surfaces during curing plays an important role in the sizing efficiency of paper with AKD. Good surface coverage of AKD is a prerequisite for achieving a good sizing effect. It is a common observation that ketone (hydrolysed AKD) does not provide the same level of sizing of cellulose fibres and paper as does AKD under the same sizing conditions, despite the fact that ketones are more hydrophobic than AKD. This has generally been thought to be due to the fact that a ketone is unable to form a covalent β-ketoester bond with OH groups on the surface of cellulose fibres. Recent work in our laboratory has concentrated on comparing interactions between a glass surface (model surface chosen for cellulose fibres) and AKD and ketones. Our measurements show that both AKD and the corresponding ketones exhibit similar strength in their interaction with a glass surface. This result suggests that there may be other reasons why ketones have poorer ability in sizing cellulose fibres. In this study the weak sizing ability of ketones was investigated by taking a different approach. Special attention was given to the spreading behaviour of AKD and their corresponding ketones. We focused on the melting points of AKD, their corresponding ketones and mixtures of AKD and ketones. Our results show that the melting point of the AKD wax studied (52 C) was markedly lower than that of the ketone wax ( 80 C) which was produced by hydrolysing the AKD. The much higher melting point of the latter has a strong negative impact on its spreading ability, contributing to its sizing performance being much worse than that of AKD. A tentative explanation of this phenomenon is given based on molecular interactions.
Status of the U.S. Department of Energy's Advanced Hydropower Turbine Systems Program (2001)

No abstract prepared.
Technology Mapping for FPGA Using GeneralizedFunctional Decomposition (1994)

In this paper, we address the technology mapping for RAM‐based FPGA. Functional decomposition is applied to decompose a large function into a set of smaller subfunctions such that each subfunction can be implemented using a single logic cell. Our system is mainly divided into two parts. The first part is designed specifically for totally symmetric functions. A Fast-Decompose algorithm based on weight dependency is proposed. The second part deals with general functions. We consider some techniques such as output partition, variable partition, don′t care assignment and encoding to minimize the number of subfunctions derived. Using these techniques together, our tool, Fun-Map , improves the mapping results compared with other tools in terms of area and delay.
Optimized Organometal Halide Perovskite Planar Hybrid Solar Cells via Control of Solvent Evaporation Rate (2014)

Organometallic halide perovskite-based solar cells have exhibited rapidly increasing efficiencies through the use of mesoporous composites. The addition of materials used in organic solar cells to perovskite-based solar cells (PSCs) enables the fabrication of low-cost, flexible, low-temperature, solution-processed PSCs. However, obtaining sufficient coverage of the organic layer, usually poly(3,4-ethylenedioxythiophene)–poly(styrenesulfonate) (PEDOT:PSS), with CH3NH3PbI3–xClx films remains difficult in spite of the advances. In this study, we investigated the influence of controlling the solvent evaporation rate on the degree of PEDOT:PSS surface coverage by CH3NH3PbI3–xClx. We determined that an adequately fast spinning speed, drying at room temperature, and stepwise ramp annealing are critical for obtaining optimized planar hybrid perovskite solar cells with an ITO/PEDOT:PSS/CH3NH3PbI3–xClx/PCBM/Al structure and efficiencies of up to 11.8%.
Abusing File Processing in Malware Detectors for Fun and Profit (2012)

We systematically describe two classes of evasion exploits against automated malware detectors. Chameleon attacks confuse the detectors' file-type inference heuristics, while werewolf attacks exploit discrepancies in format-specific file parsing between the detectors and actual operating systems and applications. These attacks do not rely on obfuscation, metamorphism, binary packing, or any other changes to malicious code. Because they enable even the simplest, easily detectable viruses to evade detection, we argue that file processing has become the weakest link of malware defense. Using a combination of manual analysis and black-box differential fuzzing, we discovered 45 new evasion exploits and tested them against 36 popular antivirus scanners, all of which proved vulnerable to various chameleon and werewolf attacks.
Effects of Halothane Anesthesia on Vasoconstrictor Response to NG-Nitro-L-Arginine Methyl Ester, an Inhibitor of Nitric Oxide Synthesis, in Sheep (1993)

This study tests the hypothesis that halothane-induced inhibition of the endothelium-derived relaxing factor/nitric oxide (EDRF/NO) pathway significantly contributes to cardiovascular performance and thus reduces the vasoconstrictor response to NO synthesis inhibitors in vivo. We determined the effects of the administration of the NO synthesis inhibitor NG-nitro-L-arginine methyl ester (L-NAME) in chronically instrumented, halothane-anesthetized sheep and in awake control animals. Six sheep underwent halothane anesthesia (1.5 vol%) with mechanical ventilation. Five sheep were studied in the awake state with spontaneous breathing. Both groups received a bolus of L-NAME (25 mg/kg), followed 4 h later by L-arginine (300 mg/kg) to reverse the effects of L-NAME. L-NAME administration caused a significant increase in pulmonary and systemic vascular resistance (P < 0.05) in both groups. However, L-NAME produced a sharp increase in mean arterial and pulmonary artery pressures only in the control group, whereas the pressor response in the halothane group was attenuated. Cardiac output, which was significantly lower after L-NAME administration in both groups, increased after L-arginine. The results suggest that halothane does not significantly alter the EDRF/NO-mediated effects on the vasculature but potentiates the cardiac depressant effect of L-NAME.
Doxorubicin Disaccharide Analogue: Apoptosis-Related Improvement of Efficacy In Vivo (1997)

The high antitumor activity of MEN 10755 in human tumor xenografts, including doxorubicin-resistant xenografts, and its unique pharmacologic and biologic properties make this disaccharide analogue a promising candidate for clinical evaluation.
Glibenclamide improves postischemic recovery of myocardial contractile function in trained and sedentary rats (2001)

In this study, we sought to determine whether there was any evidence for the idea that cardiac ATP-sensitive K+ (K(ATP)) channels play a role in the training-induced increase in the resistance of the heart to ischemia-reperfusion (I/R) injury. To do so, the effects of training and an K(ATP) channel blocker, glibenclamide (Glib), on the recovery of left ventricular (LV) contractile function after 45 min of ischemia and 45 min of reperfusion were examined. Female Sprague-Dawley rats were sedentary (Sed; n = 18) or were trained (Tr; n = 17) for >20 wk by treadmill running, and the hearts from these animals used in a Langendorff-perfused isovolumic LV preparation to assess contractile function. A significant increase in the amount of 72-kDa class of heat shock protein was observed in hearts isolated from Tr rats. The I/R protocol elicited significant and substantial decrements in LV developed pressure (LVDP), minimum pressure (MP), rate of pressure development, and rate of pressure decline and elevations in myocardial Ca(2+) content in both Sed and Tr hearts. In addition, I/R elicited a significant increase in LV diastolic stiffness in Sed, but not Tr, hearts. When administered in the perfusate, Glib (1 microM) elicited a normalization of all indexes of LV contractile function and reductions in myocardial Ca(2+) content in both Sed and Tr hearts. Training increased the functional sensitivity of the heart to Glib because LVDP and MP values normalized more quickly with Glib treatment in the Tr than the Sed group. The increased sensitivity of Tr hearts to Glib is a novel finding that may implicate a role for cardiac K(ATP) channels in the training-induced protection of the heart from I/R injury.
Ultrafast optical manipulation of magnetic order (2010)

The interaction of subpicosecond laser pulses with magnetically ordered materials has developed into a fascinating research topic in modern magnetism. From the discovery of subpicosecond demagnetization over a decade ago to the recent demonstration of magnetization reversal by a single $40\phantom{\rule{0.3em}{0ex}}\mathrm{fs}$ laser pulse, the manipulation of magnetic order by ultrashort laser pulses has become a fundamentally challenging topic with a potentially high impact for future spintronics, data storage and manipulation, and quantum computation. Understanding the underlying mechanisms implies understanding the interaction of photons with charges, spins, and lattice, and the angular momentum transfer between them. This paper will review the progress in this field of laser manipulation of magnetic order in a systematic way. Starting with a historical introduction, the interaction of light with magnetically ordered matter is discussed. By investigating metals, semiconductors, and dielectrics, the roles of (nearly) free electrons, charge redistributions, and spin-orbit and spin-lattice interactions can partly be separated, and effects due to heating can be distinguished from those that are not. It will be shown that there is a fundamental distinction between processes that involve the actual absorption of photons and those that do not. It turns out that for the latter, the polarization of light plays an essential role in the manipulation of the magnetic moments at the femtosecond time scale. Thus, circularly and linearly polarized pulses are shown to act as strong transient magnetic field pulses originating from the nonabsorptive inverse Faraday and inverse Cotton-Mouton effects, respectively. The recent progress in the understanding of magneto-optical effects on the femtosecond time scale together with the mentioned inverse, optomagnetic effects promises a bright future for this field of ultrafast optical manipulation of magnetic order or femtomagnetism.
Iridium‐Catalyzed Regio‐ and Enantioselective Hydroarylation of Alkenyl Ethers by Olefin Isomerization (2017)

Iridium-catalyzed hydroarylation of alkenyl ethers, such as allylic and homoallylic ethers, by C-H bond activation gave high yields of the corresponding addition products, where the aryl groups were selectively installed at the α-carbon atom to the alkoxy group. The reaction involves an isomerization of the alkenyl ethers into the corresponding 1-alkenyl ethers, which then undergo the regio- and enantioselective hydroarylation.
Exchanges of Uranium(VI) Species in Amidoxime-Functionalized Sorbents (2009)

Amidoxime (AO)-functionalized polymer sorbents used in this study were prepared by two different routes involving UV grafting and electron-beam grafting of acrylonitrile (AN) into poly(propylene) fibrous and microporous sheets, and subsequent conversion of AN to AO groups by reacting the precursor sorbent with hydroxylamine. The values of self-diffusion coefficient (D(s)) of UO(2)(2+) in fibrous and sheet AO sorbents were found to be 1.1 x 10(-6) and 2.3 x 10(-10) cm(2) s(-1), respectively. The higher diffusion mobility of UO(2)(2+) in the fibrous AO sorbent was attributed to its higher free volume as observed in scanning electron microscopic studies. The water content was also found to be maximum in AO-fibrous sorbent (165-200 wt %) and minimum in AO-sheet sorbent (70 wt %). In fibrous AO sorbent, the values of D(s) for Na(+) and Sr(2+) were found to be comparable to their self-diffusion coefficients in the aqueous medium. This indicated that the retardation in diffusion mobility of the ions was a minimum in the fibrous AO sorbent. However, D(s) of UO(2)(2+) in the fibrous membrane was found to be significantly lower than that of Sr(2+), which has a self-diffusion coefficient comparable to that of UO(2)(2+) in aqueous medium. This could be attributed to stronger binding of UO(2)(2+) with AO groups as compared to Sr(2+). To understand the parameters affecting the U(VI) sorption from seawater, the U(VI) exchange rates between fibrous AO sorbent (S) and seawater (aq) involving (H(+)/Na(+))(S) right harpoon over left harpoon ([UO(2)(CO(3))(3)](4-))(aq) and (UO(2)(2+))(S) right harpoon over left harpoon ([UO(2)(CO(3))(3)](4-))(aq) systems were experimentally measured. The exchange profiles thus obtained were found to be non-Fickian and much slower than (H(+))(S) right harpoon over left harpoon (UO(2)(2+))(aq) and (UO(2)(2+))(S) right harpoon over left harpoon (UO(2)(2+))(aq) exchanges. This seems to suggest that the reaction kinetics involved in decomplexation of [UO(2)(CO(3))(3)](4-) into UO(2)(2+), which forms a complex with AO groups, is the rate-determining step in sorption of U(VI) from seawater. The kinetics of U(VI) sorption in AO-gel and AO-fibrous sorbents followed the pseudo-second-order rate equation. The density of AO groups in the sorbents and their conditioning were found to influence the U(VI) sorption from seawater.
Localization of the functional sites on the alpha chain of acetylcholine receptor. (1987)

A comprehensive synthetic approach, previously developed in this laboratory, has been applied to systematically screen the entire extracellular part (residues 1-210) of the alpha chain of the Torpedo californica acetylcholine receptor (AChR) for the profiles of the continuous regions that are recognized by antibodies against free, or membrane-sequestered, AChR; the regions recognized by AChR-primed T cells; the regions that bind alpha-bungarotoxin and cobratoxin; and an acetylcholine-binding region. Eight continuous antigenic sites were localized in this part of the alpha chain by all of the antisera tested. The sites were independent of the host species from which the antisera were obtained and were also similar to antisera against the isolated pentameric AChR or against the membrane-sequestered AChR. Six regions were found to stimulate AChR-primed T cells (T sites). Three of the T sites coincided with regions recognized by antibodies. At least two T sites had no detectable antibody responses directed to them. Five toxin-binding regions were localized, and may constitute distinct sites or, alternatively, different faces in one (or more) sites. Some of these regions coincided with regions recognized by anti-AChR antibodies. One of the toxin-binding regions bound acetylcholine, and immunization with this peptide induced experimental autoimmune myasthenia gravis.
Additive antileukemia effects by GFI1B- and BCR–ABL-specific siRNA in advanced phase chronic myeloid leukemic cells (2013)

Previous studies demonstrated selective inhibition of the BCR-ABL (breakpoint cluster region-Abelson murine leukemia oncogene) tyrosine kinase by RNA interference in leukemic cells. In this study, we evaluated the effect of BCR-ABL small interfering RNA (siRNA) and GFI1B siRNA silencing on chronic myeloid leukemia (CML) cells in myeloid blast crises. The GFI1B gene was mapped to chromosome 9 and is, therefore, located downstream of the BCR-ABL translocation in CML cells. Co-transfection of BCR-ABL siRNA and GFI1B siRNA dramatically decreased cell viability and significantly induced apoptosis and inhibited proliferation in K562 cells (P<0.0001) and primary advanced phase CML cells (P<0.0001) versus controls. Furthermore, combining of BCR-ABL siRNA and GFI1B siRNA significantly modified the expression of several relevant genes including Myc, MDR1, MRP1 and tyrosyl-phosphoproteins in primary CML cells. Our data suggest that silencing of both BCR-ABL siRNA and GFI1B siRNA is associated with an additive antileukemic effect against K562 cells and primary advanced CML cells, further validating these genes as attractive therapeutic targets.
Analysis of a ripple-free input-current boost converter with discontinuous conduction characteristics (1997)

Coupled inductor techniques supply a method to reduce the power converter size and weight and achieve ripple-free current. The boost power converter is a very popular topology in industry. However, the input-current ripple hinders efforts to meet electromagnetic interference (EMI) requirements. In particular, the input current becomes discontinuous and pulsating when the conventional boost power converter operates in the discontinuous inductor-current mode. This paper describes a boost power converter which has the same discontinuous properties as the conventional boost power converter. However, the proposed boost topology has continuous or ripple-free input current when it operates with discontinuous inductor-current. The proposed topology is compared with traditional converter topologies, such as the Sepic and Cuk power converters. Simulation results are presented. The prototype is built to demonstrate the theoretical prediction. The proposed boost topology is simple, with straightforward control ~the same as pulse-width modulation (PWM)\.
Anticancer Drugs, Ionophoric Peptides, and Steroids as Substrates of the Yeast Multidrug Transporter Pdr5p (1996)

Pdr5p is the yeast Saccharomyces cerevisiae ATP-binding cassette transporter conferring resistance to several unrelated drugs. Its high overproduction in Pdr1p transcription factor mutants allows us to study the molecular mechanism of multidrug transport and substrate specificity. We have developed new in vivo and in vitro assays of Pdr5p-mediated drug transport. We show that in spite of little sequence homology, and inverted topology in respect to that of mammalian P-glycoproteins, Pdr5p shares with them common substrates. Pdr5p extrudes rhodamines 6G and 123, from intact yeast cells in an energy-dependent manner. Plasma membrane preparations from a Pdr5p-overproducing strain exhibit ATP hydrolysis-dependent, osmotically sensitive rhodamine 6G fluorescence quenching. The quenching is competitively inhibited by micromolar concentrations of many anticancer drugs, such as vinblastine, vincristine, taxol, and verapamil, and of ionophoric peptides as well as steroids. In contrast, other anticancer drugs, like colchicine and some multidrug resistance modifiers, such as quinidine, exert noncompetitive inhibition. Our experimental system opens new possibilities for the analysis of structure-function relationship of multidrug transporter substrates and inhibitors.