gebhart/patrepeval huggingface dataset:
Urinary Recovery of <i>N</i> -Formimidoyl Thienamycin (MK0787) as Affected by Coadministration of <i>N</i> -Formimidoyl Thienamycin Dehydropeptidase Inhibitors (1983)

N-Formimidoyl thienamycin (MK0787) undergoes renal metabolism by a dipeptidase, dehydropeptidase I, located on the brush border of the proximal tubular cells. The effects of two inhibitors (MK-789 and MK-791) of dehydropeptidase I on the pharmacokinetics of N-formimidoyl thienamycin were studied in 41 healthy subjects receiving various combinations of N-formimidoyl thienamycin and MK-789 or MK-791. Both inhibitors affected the plasma kinetics of N-formimidoyl thienamycin only to a small extent. Plasma concentrations and the area under the plasma concentration curve increased about 20% with a proportional decrease in plasma clearance. Plasma half-life was not altered significantly. Coadministration of MK-789 or MK-791 resulted in uniform and marked increases in urinary recovery and renal clearance of N-formimidoyl thienamycin. Thus, at an N-formimidoyl thienamycin/MK-791 ratio of 1:0.25 or higher, the urinary recovery was about 72% in all subjects, whereas it varied between 7.7 and 43% when N-formimidoyl thienamycin was given alone. The ratio of the N-formimidoyl thienamycin and MK-791 doses affected response. At relatively higher doses of MK-791, significant increases of N-formimidoyl thienamycin urinary recovery, renal clearance, and urine concentrations occurred during the later part of the 10-h observation period after each administration. At a 1:1 ratio of the two drugs, the inhibition of renal metabolism of N-formimidoyl thienamycin was maintained for at least 8 h, whereas renal clearance declined as soon as 4 h after the administration of a 1:0.25 ratio. The results indicated that MK-789 and MK-791 alter the renal excretion of N-formimidoyl thienamycin from glomerular filtration plus tubular secretion to glomerular filtration only, possibly by competitively inhibiting the penetration of N-formimidoyl thienamycin into the proximal tubular cells.
Chronic Iron Deposition following Acute Hemorrhagic Myocardial Infarction: A Cardiovascular Magnetic Resonance Study (2012)

Introduction - Intramyocardial hemorrhage frequently occurs in large reperfused myocardial infarctions (MI). However, its long-term fate remains unexplored.

Hypothesis - We hypothesize that intramyocardial hemorrhage, secondary to reperfused MI, results in chronic iron deposition within infarcted territories.

Methods - We studied 15 patients by Cardiovascular Magnetic Resonance (CMR) T2* mapping (1.5T) on day 3 and 6 months after successful percutaneous coronary intervention for first STEMI. Using the same CMR protocol, we also studied 20 canines, on days 3 and 56 post ischemia-reperfusion injury, of which 3 animals received sham procedures. Subsequently, canine hearts were explanted, imaged ex-vivo, and samples of hemorrhagic infarcts (Hemo+), non-hemorrhagic infarcts (Hemo-), remote and sham myocardium were isolated, sectioned and mass spectrometry was performed.

Results - Eleven patients had Hemo+ (verified by T2* CMR on day 3) and their scar tissue T2* values remained significantly lower after 6 months, when compared to Hemo- and remote myocardium (Fig 1; p<0.001). In canines, Hemo+ territories showed a significant T2* reduction compared to the other groups (Fig 2; p<0.001). Mean iron content ([Fe]) of Hemo+ on day 56 was 10-fold greater than that observed in control groups (p<0.001), while no differences were observed among the control groups (p=0.14). A strong linear relationship was observed between log(T2*) and -log([Fe]) (R2 = 0.74; p<0.001) on day 56. Conclusion - Hemorrhagic MI leads to chronic iron depositions within the infarct zones. Consequences of chronic iron deposition within the scar tissue remain to be investigated.
A Method to Generate Propulsor Side Forces (2010)

A computational study was performed to investigate a method to generate vehicle maneuvering forces from a propulsor alone. A ducted, preswirl propulsor was configured with an upstream stator row and downstream rotor. During normal operation, the upstream stator blades are all situated at the same pitch angle and preswirl the flow into the propulsor while generating a roll moment to counter the moment produced by the rotor. By varying the pitch angles of the stator blade about the circumference, it is possible to both generate a mean stator side force and subsequently vary the axial velocity and swirl that is ingested into the propulsor. The rotor then generates a side force in response to the inflow. Both potential flow and fully viscous 3D Reynolds averaged Navier–Stokes (RANS) computations were used to predict the stator forces, velocity field, and rotor response. Potential flow methods were used for initial examination of a wide variety of stator configurations. The most promising were then modeled using RANS. The RANS inflow was then computed and used as velocity boundary conditions during rotor blade design using potential flow methods. Blade parameters including blade number, rake, skew, and a combination of the two were varied to characterize their effects. RANS was used to then validate the final propulsor design. Computations demonstrated that total side force coefficients on the order of 0.1 and moment coefficients about the stator leading edge of 0.066 could be generated by the propulsor alone. This translates to an additional 50% control authority at 3 kn for current Navy 21″ unmanned undersea vehicles.
Investigation of Liquid Metal Ohmic Contacts for Graphene Photonic Devices (2015)

We demonstrate the first contact resistance measurements of graphene–galinstan (g-g) ohmic contacts in an effort to improve the performance of graphene photonic devices. The nobility of carbon materials provide an interesting graphene sensor application to explore an oxidation free liquid metal - semimetal interface that can be used to lower contact resistance at source/drain terminals of a standard graphene phototransistor. Our methods utilize photopolymerization of the reactive monomer Trimethlylolpropane Triacrylate (TMPTA) in order to fabricate micro structures necessary to overlay liquid metal contacts on graphene. With the use of an industry standard transfer length method (TLM), a contact resistance of −124±28Ω was measured at both standard temperature and pressure. The results from our study suggest that liquid metals such as galinstan are comparable alternatives to rigid semiconductor interfaces and demonstrates interesting boundary characteristics that may lead to heavy chemical doping and associated low resistance contacts that are required to increase sensitivity in graphene photonic devices.
Differential Rate Assay of Human Pancreatic and Salivary α-Amylases in Serum Using Two Coupled Enzymes (1986)

p-Nitrophenyl O-6-deoxy-6-[(2-pyridyl)amino]-alpha-D-glucopyranosyl-(1----4)-O-alpha- D-glucopyranosyl-(1----4)-O-alpha-D-glucopyranosyl-(1----4)-O-alpha-D- glucopyranosyl-(1----4)-alpha-D-glucopyranoside (FG5P) is hydrolyzed by human pancreatic a-amylase (HPA) or salivary alpha-amylase (HSA) to O-6-deoxy-6-[(2-pyridyl)amino]-alpha-D- glucopyranosyl-(1----4)-O-alpha-D-glucopyranosyl-(1----4)-D-glucose (FG3) and p-nitrophenyl alpha-maltoside or to O-6-deoxy-6-[(2-pyridyl)amino]-alpha-D-glucopyranosyl-(1----4)-O-alpha- D-glucopyranosyl-(1----4)-O-alpha-D-glucopyranosyl-(1----4)-D-glucose (FG4) and p-nitrophenyl alpha-glucoside. The use of alpha-D-glucosidase (maltase) [EC 3.2.1.20] of Saccharomyces carlsbergensis and oligo-1,6-glucosidase (isomaltase) [EC 3.2.1.10] of bakers' yeast as coupled enzymes differentiates between the two reactions, because alpha-D-glucosidase liberates p-nitrophenol from both p-nitrophenyl alpha-glucoside and p-nitrophenyl alpha-maltoside, but oligo-1,6-glucosidase liberates it only from p-nitrophenyl alpha-glucoside. HPA produces more FG4 and p-nitrophenyl alpha-glucoside than HSA. Taking advantage of the differences in the action of the two amylases and in the substrate specificity of the coupled enzymes, we have developed a new colorimetric differential rate assay of alpha-amylases in human serum.
Specificity of the high-mannose recognition site between Enterobacter cloacae pili adhesin and HT-29 cell membranes (1997)

Enterobacter cloacae has been implicated as one of the causative agents in neonatal infection and causes a septicemia thought to be initiated via the gastrointestinal tract. The adhesion of radiolabeled E. cloacae to HT-29 cells was concentration and temperature dependent and was effectively blocked by unlabeled bacteria or by millimolar concentrations of alpha-mannosides and micromolar concentrations of high-mannose oligosaccharides. A variety of well-characterized mannose oligosaccharides were tested as inhibitors of adhesion. The best inhibitor was the Man9(GlcNAc)2-tyrosinamide, which was considerably better than other tyrosinamide-linked oligosaccharides such as Man7(GlcNAc)2, Man6(GlcNAc)2 or Man5(GlcNAc)2. Further evidence that the bacteria preferred Man9(GlcNAc)2 structures was obtained by growing HT-29 cells in the presence of glycoprotein processing inhibitors that block mannosidase I and increase the amount of protein-bound Man9(GlcNAc)2 at the cell surface. Such cells bound 1.5- to 2-fold more bacteria than did control cells. The adhesin involved in binding to high-mannose structures was purified from isolated pili. On sodium dodecyl sulfate-gels, a 35-kDa protein was identified by its specific binding to a mannose-containing biotinylated albumin. The amino acid sequences of several peptides from the 35-kDa subunit showed over 85% identity to FimH, the mannose-specific adhesin of Salmonella typhimurium. Pili were labeled with 125I and examined for the ability to bind to HT-29 cells. Binding showed saturation kinetics and was inhibited by the addition of Man9(GlcNAc)2-tyrosinamide but not by oligosaccharides with fewer mannose residues. Polyclonal antibody against this 35-kDa protein also effectively blocked adhesion of pili or E. cloacae, but no effect was observed with nonspecific antibody. These studies demonstrate that the 35-kDa pilus subunit is a lectin whose specificity is directed toward Man, (GlcNAc)2 oligosaccharides.
Analytics-Based Solutions for Improving Alert Management Service for Enterprise Systems (2013)

Today's enterprise systems are continuously monitored for timely detection of behavioral anomalies. The tools for monitoring these systems generate alerts on observing abnormal conditions. These alerts are then acted upon by the service desk personnel for timely resolution of the problems. However, there are several drawbacks in today's alert management service for alert generation and resolution. Present approach of generating and analyzing alerts is highly manual, ad-hoc, and intuition-driven. The fixes are often temporary and ineffective thereby making the system unstable. We propose to replace this manual and intuition-based approach with an automated and analytics led approach. We present algorithms to detect duplicate alerts, infer inter-alert relationships, and derive temporal signature of alerts. We validate the proposed ideas by presenting a real-world case-study.
Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors (2004)

Several 1-aryl-4-(2-arylethyl)piperazine derivatives were synthesized and tested in-vitro for their binding affinity for 5-HT(7) and 5-HT(1A) receptors. These compounds displayed 5-HT(7 )receptor affinity ranging between K(i) = 474 nM and K(i) = 8.2 nM, besides high affinity for the 5-HT(1A) receptor. Intrinsic activity of the most potent compounds was assessed. 4-[2-(3-Methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine (16) and 1-(1,2-benzisoxazol-3-yl)-4-[2-(3-methoxyphenyl)ethyl]piperazine (20) (K(i) = 24.5 and 8.2 nM, respectively) behaved as partial agonist and full agonist, respectively, when tested for 5-HT(7) receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction.
Acid ceramidase is a novel factor required for early embryo survival (2007)

Recent studies suggest that the lipid, ceramide, induces the default apoptosis process in eggs. Yet, it is obscure how newly formed embryos overcome this fate. Acid ceramidase (AC) is a key regulatory enzyme involved in ceramide metabolism, and mutations in the AC gene (Asah1) result in Farber Lipogranulomatosis, a fatal human genetic disorder. Our previous studies revealed that AC knockout (Asah1-/-) mice had a lethal phenotype, and herein we reveal the mechanism underlying this observation. A single-cell, polymerase chain reaction (PCR) genotyping method was developed to analyze individual embryos from Asah1 +/- intercrosses. Combined with Annexin V staining, this genotype analysis demonstrated that Asah1-/- embryos could not survive beyond the 2-cell stage, and underwent apoptotic death. Notably, sphingosine-1-phosphate (S1P) treatment of early 2-cell embryos from the Asah1 +/- intercrosses rescued Asah1-/- embryos, and enabled their progression from the 2-cell to 4-8-cell stage. Quantitative PCR also revealed that expression of the Asah1 gene in healthy embryos was initiated at the 2-cell stage, coincident with embryonic genome activation (EGA). AC activity and Western blot analyses further demonstrated high expression and activity of the enzyme in normal, unfertilized eggs, which likely provide the protein to newly formed embryos prior to EGA. Based on these observations, we suggest that AC is an essential factor required for embryo survival that functions by removing ceramide from the newly formed embryos, thus inhibiting the default apoptosis pathway.
Automatic Real-Time Reconstruction of Patient-Specific 3D Knee Model Using Ultrasound RF Data (2012)

Introduction In this work, we present the first real-time fully automatic system for reconstruction of patient-specific 3D knee bones models using ultrasound raw RF data. The system was experimented on two cadaveric knees, and reconstruction accuracy of 2 mm was achieved. Methods To use the highest available contrast and spatial resolution in the ultrasound data, the raw RF signals were used directly to automatically extract the bone contours from the ultrasound scans. Figure 1 shows a sample ultrasound B-mode image for cadaver9s distal femur, showing some of the scan lines raw RF signals as well as the final extracted contour using our method. An ultrasound machine (SonixRP, Ultrasonix Inc) was used to scan the knee joint and the RF data of the scans are acquired by custom-built (using Visual C++) software running on the ultrasound machine. An optical tracker (Polaris Spectra, Northern Digital Inc) was attached to the ultrasound probe to track its motion while being used in scanning. The scanning of the knee was performed at two flexion angles (full extension, and deep knee bend). At each position, the knee was fixed in order to collect scans that represent a partial surface of the bone (which will be later mutually registered to represent the whole bone9s surface). Figure 4 shows fluoroscopy images of a patient9s knee, showing the different articulating surfaces of the knee bones visible to the ultrasound at different flexion angles. Figure 5 shows a dissected cadaver9s knee showing the articulating surfaces visible to ultrasound at 90 degrees flexion. The custom-built software collects the RF data synchronized with the probe tracking data for each ultrasound frame. Each frame of the RF data is then processed to extract the bone contour. The bone contours are automatically extracted from the RF data frame with frame rate of 25 frames per second. Figure 2 shows a flowchart for the contour extraction process. The extracted bone contours were then used by the our software, along with the ultrasound probe9s tracking data, to reconstruct point clouds representing the bones9 surfaces. These point clouds were then aligned to the mean model of the bone9s atlas using ICP and integrated together to form 3D point cloud of the bone9s surface. A 3D model of the bone is then reconstructed by morphing the mean model to match the point cloud. Figure 3 shows a flowchart for the point cloud and 3D model reconstruction process. Results The developed system was tested on two cadavers9 knees. The cadavers9 knees were CT-scanned and manually segmented. The reconstructed models using ultrasound were then compared to the segmented models. An average error of 2 mm was achieved. Figure 6 shows sample ultrasound RF signals, and their processed version and the extracted bone echoes. Figure 7 shows sample ultrasound frames and the extracted bone contours from them. Figure 8 shows the reconstructed point clouds and 3D models for two distal femurs and a proximal tibia.
Synthesis of novel 1,2,3,4‐tetrahydrobenzo[<i>c</i>]‐1,5‐naphthyridines from pyrrolo[1,2‐<i>b</i>]isoquinolines (1987)

Abstract 1,2,3,4‐Tetrahydrobenzo[ c ]‐1,5‐naphthyridine ( 5a ) was prepared by a novel synthetic route involving the rearrangement of (±)‐( Z )‐1,10a‐dihydropyrrolo[1,2‐ b ]isoquinoline‐3,10(2 H ,5 H )‐dione oxime to afford 1,4‐dihydrobenzo[ c ]‐1,5‐naphthyridin‐2(3 H )‐one, which was reduced to 5a. The cholinomimetic activity observed with 5a prompted the synthesis and biological evaluation of additional analogues.
Electrically small particles for harvesting and channeling infrared energy (2014)

We present a novel structure composed of an ensemble of electrically small resonators for harvesting infrared energy. A flower-like structure composed of electrically small split-ring resonators, each of whose greatest length is less than λ/21, is proven to achieve more than 85% power harvesting efficiency at 0.348 THz.
The Compatibility of a Boron-Based Anion Receptor with the Carbon Anode in Lithium-Ion Batteries (2003)

The electrochemical stability of the boron anion receptor, tris(pentafluorophenyl) borane (TPFPB), on a carbonaceous mesocarbon microbeads (MCMB) electrode and its compatibility with the passivated solid electrolyte interphase (SEI) layer on the carbon anode were investigated. Comparison of the irreversible capacity loss of the MCMB electrode during initial galvanostatic cycling using electrolyte with and without the TPFPB additive indicates excellent electrochemical stability of TPFPB on the carbonaceous electrode. Cyclic voltammetry studies show that the SEI layer on the surface of the carbon electrode can be formed through the decomposition of ethylene carbonate in the presence of TPFPB. Prolonged cycling test verifies the long-term stability of the SEI layer on carbon in the presence of the TPFPB additive. The SEI layer is not dissolved by TPFPB even after heat-treatment under conditions which dissolve LiF salt. This suggested a cross-linked structure for the SEI layer on carbon electrode. A Li-ion cell using an electrolyte containing TPFPB displays better cycling performance than a cell without TPFPB under the same conditions. © 2003 The Electrochemical Society. All rights reserved.
<title>Acousto-optic processor for carrier frequency and envelope modulation analysis</title> (1992)

An acousto-optic processor capable of analyzing signals consisting of a high frequency carrier modulated by an envelope signal is described. Space-integrating spectral analysis is used to channelize signals by carrier frequency. Time-integrating spectral analysis is used to characterize the envelope signal that modulates each carrier frequency. The output is a two- dimensional display with carrier frequency along one axis and envelope frequency along the orthogonal axis. Several advantages of the processor are explained and proof-of-concept experimental results are presented. One possible application of the processor is to the automatic separation and determination of the carrier frequencies and pulse repetition frequencies of multiple received radar signals.
: Isolation and structure of halistatin 1 from the eastern Indian Ocean marine sponge Phakellia carteri (1993)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT: Isolation and structure of halistatin 1 from the eastern Indian Ocean marine sponge Phakellia carteriGeorge R. Pettit, Rui Tan, Feng Gao, Michael D. Williams, Dennis L. Doubek, Michael R. Boyd, Jean M. Schmidt, Jean Charles Chapuis, Ernest Hamel, and Cite this: J. Org. Chem. 1993, 58, 9, 2538–2543Publication Date (Print):April 1, 1993Publication History Published online1 May 2002Published inissue 1 April 1993https://pubs.acs.org/doi/10.1021/jo00061a030https://doi.org/10.1021/jo00061a030research-articleACS PublicationsRequest reuse permissionsArticle Views454Altmetric-Citations95LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
Optimization of Cr Content in High Cr Heat Resistant Steels on the Basis of Long Term Creep Strength (2002)

There have been many investigations to improve creep strengths of 9-12% Cr ferritic steels, aiming to increase the efficiency of power generation and to reduce CO2 emission to the global environment. We have tried to develop a heat resistant ferritic steel for a steam turbine rotor which would be tolerable even in the ultra super critical condition (e.g., steam temperatures of 620 to 650°C). In the beginning of alloy design, the Cr content was increased to strengthen the average chemical bond between the atoms in steel, which resulted in high creep strength in the test for a short term under the condition of large applied stresses. However, it was found from the creep test for a longer term under the condition of 650°C, 157MPa that a 10% Cr steel was much superior in creep strength to an 11.5% Cr steel, contrary to the results obtained from the creep test for a short term. Thus a series of creep tests was performed with six ferritic steels varying in Cr content in the range of 8.5 to 11.5%. As a result, it was found that an excess amount of Cr had a detrimental effect on the long-term creep strength, because it acted in some ways to promote the recovery and the softening of the martensitic microstructure in the steels. By this effect, a 9% Cr steel exhibited the highest creep strength among the six steels under the very long-term creep condition of 650°C, 98MPa.Thus the developing of advanced ferritic steels necessitates the optimization of the Cr content.
Thermocapillary flow and natural convection in a melt column with an unknown melt/solid interface (1991)

Abstract A vertical melt column set up between an upper heating rod and a lower sample rod, i.e. the so‐called halfzone system, is a convenient experimental tool for studying convection in the melt in floating‐zone crystal growth. In order to help understand the convection observed in the melt column, a computer model has been developed to describe steady state, axisymmetrical thermocapillary flow and natural convection in the melt. The governing equations and boundary conditions are expressed in general non‐orthogonal curvilinear co‐ordinates in order to accurately treat the unknown melt/solid interface as well as all other physical boundaries in the system. The effects of key dimensionless variables on the following items are discussed: (1)convection and temperature distribution in the melt; (2) the shape of the melt/solid interface; (3) the height of the melt column. These dimensionless variables are the Grashof, Marangoni and Prandtl numbers.