gebhart/patrepeval huggingface dataset:
[18F]ALX5406: A Brain-Penetrating Prodrug for GlyT1-Specific PET Imaging (2021)

Selective inhibition of glycine transporter 1 (GlyT1) has emerged as a potential approach to alleviate <i>N</i>-methyl-d-aspartate receptor (NMDAR) hypofunction in patients with schizophrenia and cognitive decline. ALX5407 is a potent and selective inhibitor of GlyT1 derived from the metabolic intermediate sarcosine (<i>N</i>-methylglycine) that showed antipsychotic potential in a number of animal models. Whereas clinical application of ALX5407 is limited by adverse effects on motor performance and respiratory function, a suitably radiolabeled drug could represent a promising PET tracer for the visualization of GlyT1 in the brain. Herein, [<sup>18</sup>F]ALX5407 and the corresponding methyl ester, [<sup>18</sup>F]ALX5406, were prepared by alcohol-enhanced copper mediated radiofluorination and studied <i>in vitro</i> in rat brain slices and <i>in vivo</i> in normal rats. [<sup>18</sup>F]ALX5407 demonstrated accumulation consistent with the distribution of GlyT1 in <i>in vitro</i> autoradiographic studies but no brain uptake in μPET experiments in naı̈ve rats. In contrast, the methyl ester [<sup>18</sup>F]ALX5406 rapidly entered the brain and was enzymatically transformed into [<sup>18</sup>F]ALX5407, resulting in a regional accumulation pattern consistent with GlyT1 specific binding. We conclude that [<sup>18</sup>F]ALX5406 is a promising and easily accessible PET probe for preclinical <i>in vivo</i> imaging of GlyT1 in the brain.
Stable Shortest Horizon FCS-MPC Output Voltage Control in Non-Minimum Phase Boost-Type Converters Based on Input-State Linearization (2021)

Finite Control Set Model Predictive Control (FCS-MPC) is an alternative to conventional linear controllers in power converters due to its attractive properties such as its conceptual simplicity, flexibility, direct consideration of non linearities as well as constraints, and fast control response. This last feature imposes computational constraints and short prediction horizons are therefore needed. In fact, in many applications an horizon one FCS-MPC controller is used. However, using FCS-MPC with a short prediction horizon in topologies that exhibit non-minimum phase behavior such as active-front-end rectifiers, dc-dc boost converters, and Z-source converters, among others, may lead to control issues. This work studies the origin of these control issues using nonlinear control theory considering a dc-dc boost converter as a case study. It is shown that the difficulty to directly control the converter output voltage using short horizon FCS-MPC is the resulting unstable internal dynamic, as the short horizon FCS-MPC controller acts like an input-output linearizing controller. To solve the problem of the unstable internal dynamic, a short horizon FCS-MPC controller based on input-state linearization is proposed allowing correct operation of the system. Experimental results show the feasibility of the proposal.
Synthese d'hydrates de carbone branches en vue de leur utilisation a l'elaboration de molecules d'interet biologique (1990)

Cette these expose differents projets de recherche a partir d'hydrates de carbone. Le premier chapitre decrit une tentative de synthese de la thienamycine substituee en cinq alpha par un groupe methyle a partir du d-mannose. La difficulte synthetique rencontree concerne la creation d'une liaison carbone-carbone en alpha d'un carbone quaternaire. Differentes methodes ont ete tentees et en particulier la formation intermediaire d'une cyanhydrine suivie de sa desoxygenation radicalaire. Cette derniere methode a ete effectuee sur plusieurs hexopyranosides. Le second chapitre presente un projet de synthese du c-disaccharide de l'avermectine b1a par couplage de deux derives de l'oleandrose. Au cours de ce travail, la formation d'aldehydes alpha, beta insatures par traitement acide d'ethers d'enol alpha alkoxy substitues est decrite: ceux-ci se sont reveles des precurseurs d'un type nouveau de dienopyranosides. Le troisieme chapitre concerne l'etude de la diastereoselectivite faciale de la reaction de diels-alder sur ces dienopyranosides avec differents dienophiles mais egalement l'etude de la stereoselectivite de la version intramoleculaire de cette reaction a partir de trienohexopyranosides
Supplementary Video Legend from Targeted Anti–Vascular Endothelial Growth Factor Receptor-2 Therapy Leads to Short-term and Long-term Impairment of Vascular Function and Increase in Tumor Hypoxia (2023)

Supplementary Video Legend from Targeted Anti–Vascular Endothelial Growth Factor Receptor-2 Therapy Leads to Short-term and Long-term Impairment of Vascular Function and Increase in Tumor Hypoxia
Threshold based selective survivability for optical WDM mesh networks (2004)

This paper presents survivability mechanisms that attempt to improve the overall restoration efficiency of dynamic link restoration in optical WDM mesh networks. The proposed mechanisms make use of network state information such as link load in order to identify critical network sections (such as links or segments) that are subsequently protected by selectively assigning backup capacity ahead of failures. The first approach, termed "threshold based selective link restoration", utilizes existing link load information to identify critical links, and the second approach, termed "threshold based selective segment restoration", employs data-analysis techniques to identify critical segments. The overall goal of the proposed algorithms is to improve the restoration efficiency by providing a trade-off between proactive protection and reactive restoration. The experimental results indicate that under high loads, the proposed approaches maintain a consistent restoration efficiency that is at least 10% when compared to dynamic restoration.
High-Performance a-IGZO Thin Film Diode as Selector for Cross-Point Memory Application (2014)

We present amorphous indium-gallium-zinc oxide Schottky diodes with unprecedented current densities of 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">4</sup> and 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">5</sup> A/cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> at forward biases of 1.5 and 5 V, respectively. The diode presents a high rectification ratio of 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">10</sup> at ±2 V, which is essential for suppressing the sneak current of not-selected cells in the memory array. In addition, we show that the diode complies with the demanding performance of memory applications. The device degradation, given by a 30% reduction of its forward current after 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">4</sup> s of continuous bias stress or 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">9</sup> pulses cycles, was studied via I-V and C-V measurements and can be attributed to trapping of electrons at deep acceptor levels, which increases the diode built-in potential. Finally, we show that the device is stable upon thermal stress at 300 °C for 1 h, which opens the possibility of further processing and integration with the memory cell.
Toward energy-efficient content dissemination (2011)

A major role of today's Internet is to provide efficient content dissemination among users, such as distributing multimedia content and sharing user generated data. To meet the ever increasing demands, the Internet has been rapidly growing, and it now includes a web of tens of millions of networked devices ranging from content servers to core and edge routers to home gateways. Due to the sheer numbers, however, it is reported that these devices, such as those used for content delivery, consume a considerable amount of energy. While optimizing the energy efficiency of data centers is well studied in the literature, understanding the energy efficiency of various content dissemination strategies has received comparatively little attention thus far. In this article we review existing content dissemination architectures and survey the energy efficiency of various network devices used for content delivery. The energy efficiency comparison using simple trace-based simulations reveals that a change from a host-oriented to a content-centric networking model can substantially improve energy efficiency of content dissemination. Our preliminary results are encouraging and will stimulate further research in this direction.
Effects of SO2 and I2 on the Photoluminescence of Oxidized Porous Silicon (1997)

The photoinduced visible light emission from lightly oxidized porous silicon can be reversibly quenched by both sulfur dioxide molecules and iodine molecules. Possible mechanisms for these processes are compared to the better understood mechanism for Brönsted base quenching of porous silicon photoemission. Supporting evidence was obtained through infrared spectroscopy, electron paramagnetic resonance spectroscopy, and surface chemistry. The feasibility of fashioning a SO2 sensor using oxidized porous silicon is also discussed.
Clinical Performance of a Durasul Highly Cross-Linked Polyethylene Acetabular Liner for Total Hip Arthroplasty at Five Years (2005)

While the qualitative wear pattern of the highly cross-linked polyethylene liner was the same as that of the conventional polyethylene liner, the annual linear wear rate was 45% of that seen with the conventional polyethylene liner. Therefore, we believe that these early data support the continued use of this highly cross-linked polyethylene liner for total hip arthroplasty.
Interframe estimation and video coding (1996)

This thesis consists of two parts: the first part addresses least-squares optimal backward and forward motion-compensated interframe estimation. The second part is devoted to the development of two applications of interframe estimation: backward multiresolution video coding and coding of MRI volumetric data.
We propose an operator-based paradigm for backward motion estimation. It is shown that the backward motion-compensated estimation problem, in a sampled environment, naturally decomposes into a discrete search and a continuous optimization problem. Solution strategies for each of the problems are individually explored, and a fast recursive least squares (RLS) algorithm for the solution of the optimization problem is proposed. We explore a dual operator space that offers potential computational advantages compared to the primary operators, and extend the operator method to higher dimensional spaces.
Two predominant motion estimation methods, known as warping and overlapped-block matching, are studied. We compute optimal interpolation kernels for warping, based on video sequence statistics. Optimal interpolation kernels for typical sequences are far from the usual bilinear or affine kernels, and offer significant improvements in MSE performance.
Warping and overlapped-block methods are very different in their approach to addressing motion field ambiguities (ambiguities arise from a subsampled motion field). Each of them is best suited to certain motion scenarios. Noting that these scenarios often coexist in video, we motivate a joint warping/overlapped-block methodology. Through a generalization of the techniques developed in optimal warping, optimal joint warping/overlapped-block kernels are computed.
The problem of backward coding in a multiresolution environment is analyzed. It is shown that a direct band-to-band estimation of coefficients in a maximally subsampled (wavelet) multiresolution framework is generally not possible, due to aliasing effects. A method is proposed to circumvent the aliasing problem, and a coding scheme is built around it. Quantization of estimation errors (residues) is performed through zerotree wavelet coding. Because of interdependencies in the quantization of estimation error at a given resolution and motion estimation at higher resolutions, true zerotrees are not computable, thus we construct a substitute zerotree. The resulting coder has a rate-distortion performance comparable to that provided by a typical MPEG coder.
Finally, interframe coding of volumetric MRI data is considered. For the first time, this work reports coding gain (over intraframe coding) for interframe coding of MRI data. The interframe estimator used in this coder addresses the volumetric nature of the data by using a warping estimator and the high-variance noise of MRI through in-loop filtering. Quantization of estimation errors is performed through a zerotree wavelet coder.
Structure-Guided Design of Aminopyrimidine Amides as Potent, Selective Inhibitors of Lymphocyte Specific Kinase: Synthesis, Structure–Activity Relationships, and Inhibition of in Vivo T Cell Activation (2008)

The lymphocyte-specific kinase (Lck), a member of the Src family of cytoplasmic tyrosine kinases, is expressed in T cells and natural killer (NK) cells. Genetic evidence, including knockout mice and human mutations, demonstrates that Lck kinase activity is critical for normal T cell development, activation, and signaling. Selective inhibition of Lck is expected to offer a new therapy for the treatment of T-cell-mediated autoimmune and inflammatory disease. With the aid of X-ray structure-based analysis, aminopyrimidine amides 2 and 3 were designed from aminoquinazolines 1, which had previously been demonstrated to exhibit potent inhibition of Lck and T cell proliferation. In this report, we describe the synthesis and structure-activity relationships of a series of novel aminopyrimidine amides 3 possessing improved cellular potency and selectivity profiles relative to their aminoquinazoline predecessors 1. Orally bioavailable compound 13b inhibited the anti-CD3-induced production of interleukin-2 (IL-2) in mice in a dose-dependent manner (ED 50 = 9.4 mg/kg).
SEAR: towards a mobile and context-sensitive speech-enabled augmented reality (2002)

A maintenance engineer who talks to pumps and pipes may not seem like the ideal person to entrust with keeping a factory running smoothly, but we hope that our mobile speech-enabled augmented reality (SEAR) framework will enable such behavior in the future to be anything but suspicious. We describe how the SEAR framework uses our flexible and scalable vision-based localization techniques to offer the engineer a seamless multi-modal user interface. This interface juxtaposes a graphical augmented reality view with a context-sensitive speech dialog concerning the industrial equipment located in the immediate vicinity.
Hepatic expression of the woodchuck hepatitis virus X-antigen during acute and chronic infection and detection of a woodchuck hepatitis virus X-antigen antibody response (1997)

The expression and localization of the woodchuck hepatitis virus X-antigen (WHxAg) was examined and compared with other markers of a woodchuck hepatitis virus (WHV) infection using rabbit antisera generated against recombinant WHxAg produced in bacteria. Cellular fractionation studies showed that WHxAg was localized to the soluble and cytoskeletal fractions of the cell when assayed by immunoprecipitation of [35S]-met-cys labeled extracts derived from primary cultures of acute WHV-infected hepatocytes. Immunohistochemical examination of liver from chronic WHV-infected animals showed WHV core antigen (WHcAg) and WHxAg expression in non-neoplastic tissue. The WHxAg was found localized to the cytoplasm of infected cells, similar to WHcAg. WHxAg expression was diminished in the foci of altered hepatocytes and in hepatocellular adenomas but was found in only 1 of 11 hepatocellular carcinomas (HCC). Hepatic biopsies from woodchucks experimentally inoculated with WHV were examined during the acute phase of infection and during convalescence for WHcAg and WHxAg expression by immunohistochemistry. Concurrent expression of WHcAg and WHxAg was observed during the viremic phase of infection. The two antigens exhibited similar localization to the cell cytoplasm, similar distribution within the liver lobule, and similar patterns of clearance during convalescence. An immune response to WHxAg was documented in some woodchucks following acute WHV infection. These studies further define the woodchuck model of HBV infection and should allow for the investigation of the role of hepadnaviral X-antigen expression in the pathogenesis of chronic hepatitis and HCC.
Impedance Measurement on Inductive Power Transfer Systems (2019)

Inductive charging of electric vehicles requires that the vehicle and ground systems work together for power transfer from grid to the vehicle battery. In order to qualify if the vehicle system is compatible with the ground system, the presented impedance of the vehicle to the ground system can be used for characterization. However, there are no commercially available systems existing that are able to measure the impedance precisely while power transfer. For this reason, we developed a device that can be applied to characterize the presented impedance of vehicle systems. We will present first measurement results that were obtained with the device and discuss the main challenges in impedance measurements during power transfer.
Pharmacokinetic/Pharmacodynamic Modeling of Renin Biomarkers in Subjects Treated With the Renin Inhibitor Aliskiren (2008)

A semimechanistic pharmacokinetic/pharmacodynamic (PK/PD) model was developed to evaluate the effects of aliskiren on the renin-angiotensin system (RAS) in humans. Mean data were extracted from a three-way crossover, placebo-controlled study. Outcome measures included the time-course of plasma renin activity (PRA) and plasma concentrations of aliskiren, active renin (AR), angiotensin I (ANG I), and angiotensin II (ANG II). The disposition of aliskiren may be best described as a two-compartment model with nonlinear elimination and distribution. The four biomarkers of RAS inhibition were co-modeled, and the AR showed a dose-dependent increase after the administration of aliskiren. This effect was described in terms of an indirect stimulatory response model in conjunction with an empirical submodel of functional adaptation. The estimated concentration of aliskiren necessary for producing 50% inhibition of PRA is 0.66 ng/ml, which is similar to in vitro estimates (0.33 ng/ml) after correction for plasma protein binding. The final and reduced models test the current hypothesis that RAS is inhibited by direct renin antagonism, and also provide suitable platforms for future clinical study design and analysis.
Vortex fluidic entrapment of functional microalgal cells in a magnetic polymer matrix (2013)

Composite materials based on superparamagnetic magnetite nanoparticles embedded in polyvinylpyrrolidone (PVP) are generated in a continuous flow vortex fluidic device (VFD). The same device is effective in entrapping microalgal cells within this material, such that the functional cells can be retrieved from aqueous dispersions using an external magnet.
Giant, unconventional anomalous Hall effect in the metallic frustrated magnet candidate, KV 3 Sb 5 (2020)

The anomalous Hall effect (AHE) is one of the most fundamental phenomena in physics. In the highly conductive regime, ferromagnetic metals have been the focus of past research. Here, we report a giant extrinsic AHE in KV<sub>3</sub>Sb<sub>5</sub>, an exfoliable, highly conductive semimetal with Dirac quasiparticles and a vanadium Kagome net. Even without report of long range magnetic order, the anomalous Hall conductivity reaches 15,507 Ω<sup>-1</sup> cm<sup>-1</sup> with an anomalous Hall ratio of ≈ 1.8%; an order of magnitude larger than Fe. Defying theoretical expectations, KV<sub>3</sub>Sb<sub>5</sub> shows enhanced skew scattering that scales quadratically, not linearly, with the longitudinal conductivity, possibly arising from the combination of highly conductive Dirac quasiparticles with a frustrated magnetic sublattice. This allows the possibility of reaching an anomalous Hall angle of 90° in metals. This observation raises fundamental questions about AHEs and opens new frontiers for AHE and spin Hall effect exploration, particularly in metallic frustrated magnets.
Effect of Copper Addition on Electromigration Behavior of Silver Metallization (2009)

This study investigates the effect of Cu alloying on electromigration behavior of Ag metallization. Electromigration tests are performed on pure Ag and Ag (1.5% Cu) samples deposited by e-beam evaporation. The experiments show that Ag (Cu) alloy interconnect has superior elctromigration resistance compared to pure Ag interconnect. X-ray diffraction, four point probe measurements and electron microscopy were used to investigate the test structures and corresponding thin film samples. The Cu improves the lifetime of interconnect test structures by hindering Ag diffusion and increasing 111 texture of Ag. Also, Cu addition seemingly reduces the agglomeration in Ag.
1223: Hydrogen Peroxide Induces Bladder Overactivity Via Sensitization of C-Fiber Afferent Pathways Through Activation of Cyclooxygenase in Rats (2005)

You have accessJournal of UrologyDiscussed Poster, Tuesday, May 24, 2005, 1:00 - 5:00 pm1 Apr 20051223: Hydrogen Peroxide Induces Bladder Overactivity Via Sensitization of C-Fiber Afferent Pathways Through Activation of Cyclooxygenase in Rats Hitoshi Masuda, Kazunori Kihara, Michael B. Chancellor, and Naoki Yoshimura Hitoshi MasudaHitoshi Masuda More articles by this author , Kazunori KiharaKazunori Kihara More articles by this author , Michael B. ChancellorMichael B. Chancellor More articles by this author , and Naoki YoshimuraNaoki Yoshimura More articles by this author View All Author Informationhttps://doi.org/10.1016/S0022-5347(18)35368-0AboutPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail "1223: Hydrogen Peroxide Induces Bladder Overactivity Via Sensitization of C-Fiber Afferent Pathways Through Activation of Cyclooxygenase in Rats." The Journal of Urology, 173(4S), p. 332 © 2016 by American Urological AssociationFiguresReferencesRelatedDetails Volume 173Issue 4SApril 2005Page: 332 Advertisement Copyright & Permissions© 2016 by American Urological AssociationMetricsAuthor Information Hitoshi Masuda More articles by this author Kazunori Kihara More articles by this author Michael B. Chancellor More articles by this author Naoki Yoshimura More articles by this author Expand All Advertisement PDF downloadLoading ...
Pharmacokinetics and Pharmacodynamics of the Urotensin‐II Receptor Antagonist Palosuran in Healthy Male Subjects (2009)

Palosuran is a new potent and specific antagonist of the human urotensin II (U-II) receptor (UT receptor). This entry-into-humans study evaluated the tolerability and safety, pharmacokinetics, and pharmacodynamics of palosuran in a double-blind, placebo-controlled, single ascending-dose design. Oral doses of 5 to 2000 mg were given to 9 sequential groups of 8 healthy young men (6 on active drug, 2 on placebo) each. At regular intervals, tolerability and safety parameters and plasma levels of palosuran and U-II were determined. Urine was collected to determine excretion of sodium, potassium, creatinine, and palosuran. In this study, palosuran was well tolerated. No serious adverse events or dose-related adverse events were reported. No treatment-related pattern was detected for vital signs, clinical laboratory parameters, or electrocardiography parameters. After rapid absorption, palosuran displayed a plasma concentration-time profile characterized by 2 peaks at approximately 1 and 4 hours after drug administration. The apparent terminal elimination half-life was approximately 20 hours. AUC and C(max) values increased proportionally with doses up to 500 mg. Excretion of unchanged palosuran in urine was limited. No consistent effect was found on any of the pharmacodynamic variables measured. The results of this entry-into-humans study warrant further investigation of the therapeutic potential of palosuran.