gebhart/patrepeval huggingface dataset:
Long-acting dihydropyridine calcium antagonists. 6. Structure-activity relationships around 4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-2-[(2-hydroxyethoxy)methyl]-5-(methoxycarbonyl)-6-methyl-1,4-dihydropyridine (1991)

The preparation of 4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-2-[(2-hydroxyethoxy)methyl]-5- (methoxycarbonyl)-6-methyl-1,4-dihydropyridine (2) is described, and its potent calcium antagonist activity on rat aorta (IC50 = 4 x 10(-9) M) and marked tissue selectivity in vitro for vascular smooth muscle over cardiac smooth muscle are established. In order to exploit the excellent in vitro profile of compound 2, a range of analogues were prepared but none were found to have superior calcium antagonist potency and tissue selectivity. Compound 2 has excellent in vivo activity in the anesthetized dog (ED50 = 12 micrograms/kg for reduction of CVR) and a plasma half-life in the conscious dog of 7.2 h. The pharmacokinetic parameters of 2 are compared to those determined for the structurally related compounds amlodipine and felodipine. The plasma clearance for 2 (9.6 mL/min/kg) is similar to that of amlodipine and is consistent with the extended 2-substituent hindering approach to the cytochrome P-450 enzyme responsible for oxidation of the DHP ring to the corresponding pyridine.
The drug-eluting stent: is it the Holy Grail? (2001)

Although the restenosis rate of coronary stenting is generally 10% to 20%, it can go as high as 60% in patients with diabetes or complex lesions. Currently, the only effective treatment for restenosis is brachytherapy. Drug-eluting stents may be the way to prevent restenosis that cardiologists have been seeking: the drug-coated stents are simple to use and help prevent negative remodeling and the intimal hyperplasia caused by stenting. In studies comparing sirolimus-coated and bare-metal stents, the sirolimus-coated stents resulted in less smooth muscle cell colonization, minimal intimal hyperplasia, and no edge effect; moreover, no adverse clinical events were reported. Currently ongoing, multicenter clinical trials of drug-eluting stents may soon come up with the answers that cardiologists have been hoping for.
Effect of spectral envelope smearing on speech reception. I (1992)

The effect of reduced spectral contrast on the speech-reception threshold (SRT) for sentences in noise and on phoneme identification, was investigated with 16 normal-hearing subjects. Signal processing was performed by smoothing the envelope of the squared short-time fast Fourier transform (FFT) by convolving it with a Gaussian-shaped filter, and overlapping additions to reconstruct a continuous signal. Spectral energy in the frequency region from 100 to 8000 Hz was smeared over bandwidths of 1/8, 1/4, 1/3, 1/2, 1, 2, and 4 oct for the SRT experiment. Vowel and consonant identification was studied for smearing bandwidths of 1/8, 1/2, and 2 oct. Results showed the SRT in noise to increase as the spectral energy was smeared over bandwidths exceeding the ear's critical bandwidth. Vowel identification suffered more from this type of processing than consonant identification. Vowels were primarily confused with the back vowels /c,u/, and consonants were confused where place of articulation is concerned.
Malaria: toxins, cytokines and disease (1995)

In this review the old concept of severe malaria as a toxic disease is re-examined in the light of recent discoveries in the field of cytokines. Animal studies suggest that the induction of TNF by parasite-derived molecules may be partly responsible for cerebral malaria and anemia, while hypoglycaemia may be due to direct effects of similar molecules on glucose metabolism. These molecules appear to be phospholipids and we suggest that when fully characterized they might form the basis of antitoxic therapy for malaria.
Synthesis and Preliminary Characterization of Some Polyester Rotaxanes (1995)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and Preliminary Characterization of Some Polyester RotaxanesHarry W. Gibson, Shu Liu, Pierre Lecavalier, Charles Wu, and Ya Xi ShenCite this: J. Am. Chem. Soc. 1995, 117, 3, 852–874Publication Date (Print):January 1, 1995Publication History Published online1 May 2002Published inissue 1 January 1995https://pubs.acs.org/doi/10.1021/ja00108a002https://doi.org/10.1021/ja00108a002research-articleACS PublicationsRequest reuse permissionsArticle Views685Altmetric-Citations131LEARN 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-Alertsclose Get e-Alerts
Receptor‐mediated phagocytosis of rat macrophages is regulated differentially for opsonized particles and non‐opsonized particles containing β‐glucan (2001)

Summary Experiments were conducted to test the hypothesis that opsonic and non‐opsonic phagocytic capacities are differentially regulated by resting and wound‐derived macrophages. Furthermore, the phagocytosis of non‐opsonized zymosan and β‐glucan particles was quantified to determine whether cells differentially regulate non‐opsonic lectinophagocytosis in accordance with the carbohydrate composition of the ligand. In that regard, wound macrophages exhibited profound differential regulation in lectinophagocytosis with a seven‐fold increase in phagocytosis of β‐glucan particles following overnight culture but with a relatively modest increase in internalization of mannan‐containing zymosan. Cultured peritoneal macrophages increased uptake of both particles similarly. Upon activation with interferon‐γ/lipopolysaccharide (IFN‐γ/LPS), wound macrophages selectively suppressed β‐glucan ingestion, while phagocytosis of zymosan particles was unaffected. Lectinophagocytosis was decreased in activated peritoneal macrophages regardless of particle composition and was due in part to a nitric oxide‐dependent mechanism which was without a role in regulation of wound macrophage lectinophagocytosis. Overnight culture of wound macrophages suppressed their capacity for opsonic‐dependent phagocytosis independently of activation, whereas suppression of phagocytosis by peritoneal macrophages was activation‐dependent. Regulation of all three phagocytic pathways was achieved distinctly by peritoneal and wound‐derived macrophages, with changes found in the percentage of resident peritoneal macrophages capable of phagocytosis, whereas the phagocytic capacity of wound macrophages was primarily affected by the number of particles ingested by individual cells. Taken together, these findings demonstrate that the differential regulation of phagocytic pathways encompasses the nature of the phagocytic particle, the site from which macrophages are obtained, their response to activating agents and the mechanism through which the cell population alters its phagocytic potential.
Controlling the near-field excitation of nano-antennas with phase-change materials (2013)

By utilizing the strongly induced plasmon coupling between discrete nano-antennas and quantitatively controlling the crystalline proportions of an underlying Ge2Sb2Te5 (GST) phase-change thin layer, we show that nanoscale light localizations in the immediate proximity of plasmonic nano-antennas can be spatially positioned. Isolated energy hot-spots at a subwavelength scale can be created and adjusted across the landscape of the plasmonic system at a step resolution of λ/20. These findings introduce a new approach for nano-circuitry, bio-assay addressing and imaging applications.
A novel autonomous taxi model for smart cities (2018)

Autonomous taxies are in high demand for smart city scenario. Such taxies have a well specified path to travel. Therefore, these vehicles only required two important parameters. One is detection parameter and other is control parameter. Further, detection parameters require turn detection and obstacle detection. The control parameters contain steering control and speed control. In this paper a novel autonomous taxi model has been proposed for smart city scenario. Deep learning has been used to model the human driver capabilities for the autonomous taxi. A hierarchical Deep Neural Network (DNN) architecture has been utilized to train various driving aspects. In first level, the proposed DNN architecture classifies the straight and turning of road. A parallel DNN is used to detect obstacle at level one. In second level, the DNN discriminates the turning i.e. left or right for steering and speed controls. Two multi layered DNNs have been used on Nvidia Tesla K 40 GPU based system with Core i-7 processor. The mean squared error (MSE) for the detection parameters viz. speed and steering angle were 0.018 and 0.0248 percent, respectively, with 15 milli seconds of real-time response delay.
A low noise single-transistor transimpedance preamplifier for Fourier-transform mass spectrometry using a T feedback network (2012)

A novel single-transistor transimpedance preamplifier has been introduced for improving performance in Fourier-transform ion cyclotron resonance (FT-ICR) mass spectrometry. A low noise junction field-effect transistor (JFET), BF862, is used as the main amplification stage of this trans-impedance preamplifier, and a T-shaped feedback network is introduced as both the feedback and the gate biasing solutions. The T feedback network has been studied using an operational amplifier (Op Amp), AD8099. Such a feedback system allows ~100-fold less feedback resistance at a given transimpedance, hence preserving bandwidth, which is beneficial to applications demanding high gain. The single-transistor preamplifier yields a tested transimpedance of ~10(4) Ω (80 dBΩ) in the frequency range between 1 kHz and 1 MHz (mass-to-charge ratio, m/z, of around 180-180k for a 12-T FT-ICR system), with a low power consumption of ~6 mW, which implies that this preamplifier is well suited to a 12-T FT-ICR mass spectrometer. In trading noise performance for higher trans-impedance, an alternative preamplifier design, an AD8099 preamplifier with the T feedback network, has also been studied with a capability of ~10(6) Ω (120 dBΩ) transimpedance in the same frequency range. The resistive components in the T feedback network reported here can be replaced by complex impedances, which allows adaptation of this feedback system to other frequency, transimpedance, and noise characteristics for applications not only in other mass spectrometers, such as Orbitrap, time-of-flight (TOF), and ion trap systems, but also in other charge/current detecting systems such as spectroscopy systems, microscopy systems, optical communication systems, or charge-coupled devices (CCDs).
Unraveling the Mechanisms of Endocrine Resistance in Breast Cancer: New Therapeutic Opportunities (2007)

Two thirds of breast cancers express the estrogen receptor (ER), which contributes to tumor development and progression. ER-targeted therapy is therefore widely used in breast cancer to inhibit signaling through ER and disrupt breast cancer growth. This therapeutic strategy, particularly using the antiestrogen tamoxifen, is proven to increase the cure rates in early breast cancer, improve patient outcomes in advanced disease, and reduce breast cancer incidence in the prevention setting. Despite the recent integration of more powerful endocrine agents into breast cancer care, resistance to all forms of endocrine therapy remains a major problem. New insight into ER biology and progress in understanding resistance mechanisms, mediated by molecular crosstalk between ER and various growth factor signaling pathways, are generating tremendous promise for new therapeutic opportunities to target resistance and improve breast cancer disease outcomes.
Measurement of the Rate of Myofibrillar Protein Degradation Using the Arteriovenous Difference in Plasma 3-Methylhistidine Concentration of Rats (2009)

There are several methods for measuring the rate of myofibrillar protein degradation using 3-methylhistidine (3-MeHis) levels in urine, plasma and isolated muscle. However, these methods lack the accuracy of rate measurements. Therefore, it is necessary to develop a new method for determining the rate of myofibrillar protein degradation. We characterized an arteriovenous difference method using 3-MeHis plasma concentration. Rats were fasted overnight and subsequently administered leucine (135 mg/100 g BW) or fed a 20% casein diet. The rate of myofibrillar protein degradation was calculated by multiplying the femoral artery blood flow rate by the arteriovenous difference in 3-MeHis concentrations (vein-artery). The blood was collected from the femoral vein and abdominal aorta. The release of 3-MeHis from hindlimb muscle was significantly suppressed (p<0.05) in rats fed leucine or the 20% casein diet, indicating that myofibrillar protein degradation was suppressed. These results suggest that the evaluation of the rate of myofibrillar protein degradation using the arteriovenous difference method reflects nutritional conditions in a more physiological manner.
An analysis of psychophysical tuning curves in normal and pathological ears (1983)

Simultaneous psychophysical tuning curves were obtained from normal-hearing and hearing-impaired listeners, using probe tones that were either at similar sound pressure levels or at similar sensation levels for the two types of listeners. Tuning curves from the hearing-impaired listeners were flat, erratic, broad, and/or inverted, depending upon the frequency region of the probe tone and the frequency characteristics of the hearing loss. Tuning curves from the normal-hearing listeners at low-SPL's were sharp as expected; tuning curves at high-SPL's were discontinuous. An analysis of high-SPL tuning curves suggests that tuning curves from normal-hearing listeners reflect low-pass filter characteristics instead of the sharp bandpass filter characteristics seen with low-SPL probe tones. Tuning curves from hearing-impaired listeners at high-SPL probe levels appear to reflect similar low-pass filter characteristics, but with much more gradual high-frequency slopes than in the normal ear. This appeared as abnormal downward spread of masking. Relatively good temporal resolution and broader tuning mechanisms were proposed to explain inverted tuning curves in the hearing-impaired listeners.
Carousel interferometer (1995)

A new type of a swinging interferometer, the carousel interferometer, is presented, and its properties are studied and compared with other swinging interferometers. The new interferometer is built with five plane mirrors. The optical path difference is accomplished by rotation of a system that consists of four mirrors. The modulation is almost independent of the scanning of the interferometer. It is not sensitive to external perturbations such as bending or other deformations of the mount. The construction is very compact. Because of its stability and low cost it is very applicable to small Fourier-transform spectrometers for any wave-number region from the far infrared down to the ultraviolet.
Constitutive transcription of the human interleukin-6 gene by rheumatoid synoviocytes: spontaneous activation of NF-kappaB and CBF1. (1998)

The involvement of IL-6 in the pathogenesis of rheumatoid arthritis (RA) has been recently demonstrated. In the present study, we investigated the cellular and molecular mechanisms involved in the spontaneous IL-6 production by the fibroblast-like synoviocytes (FLSs) obtained from patients with RA. Cloned FLSs were established from the bulk cultures of FLSs by the limiting dilution method. Some FLS clones spontaneously produced large amounts of IL-6, whereas others produced low amounts of it. Neither anti-human TNF-alpha nor IL-1 antibody affected spontaneous IL-6 production of these FLS clones, suggesting that IL-6 production of the FLSs was endogenously up-regulated. A luciferase reporter plasmid containing the human IL-6 promoter region was significantly transcribed when transfected into the IL-6 high-producing clones, indicating that the rheumatoid FLSs retained constitutive transcriptional activity of the IL-6 gene. Electrophoretic mobility shift assays revealed that the binding activity of p50 and p65 NF-kappaB subunits and CBF1 was significantly enhanced in the IL-6 high-producing clones compared with that of IL-6 low-producing clones and cultured sarcoma cells, suggesting that spontaneous activation of NF-kappaB and CBF1 may lead to the constitutive transcription of the IL-6 gene by rheumatoid FLSs.
General, Mild and Efficient Synthesis of β-Enaminones Catalyzed by Ceric Ammonium Nitrate (2007)

Corrected by: General, Mild and Efficient Synthesis of β-Enaminones Catalyzed by Ceric Ammonium NitrateSynlett 2007; 2007(08): 1330-1330DOI: 10.1055/s-2007-977447
Solvent effect in the photoreduction of decafluorobenzophenone by 2-propanol. Reinterpretation of the light-intensity effect in the benzophenone-2-propanol system (1973)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSolvent effect in the photoreduction of decafluorobenzophenone by 2-propanol. Reinterpretation of the light-intensity effect in the benzophenone-2-propanol systemJonas. DedinasCite this: J. Am. Chem. Soc. 1973, 95, 21, 7172–7174Publication Date (Print):October 1, 1973Publication History Published online1 May 2002Published inissue 1 October 1973https://pubs.acs.org/doi/10.1021/ja00802a054https://doi.org/10.1021/ja00802a054research-articleACS PublicationsRequest reuse permissionsArticle Views81Altmetric-Citations7LEARN 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-Alertsclose Get e-Alerts
Medium-Term Electric Load Forecasting Using Multivariable Linear and Non-Linear Regression (2011)

Medium-term forecasting is an important category of electric load forecasting that covers a time span of up to one year ahead. It suits outage and maintenance planning, as well as load switching operation. We propose a new methodol-ogy that uses hourly daily loads to predict the next year hourly loads, and hence predict the peak loads expected to be reached in the next coming year. The technique is based on implementing multivariable regression on previous year's hourly loads. Three regression models are investigated in this research: the linear, the polynomial, and the exponential power. The proposed models are applied to real loads of the Jordanian power system. Results obtained using the pro-posed methods showed that their performance is close and they outperform results obtained using the widely used ex-ponential regression technique. Moreover, peak load prediction has about 90% accuracy using the proposed method-ology. The methods are generic and simple and can be implemented to hourly loads of any power system. No extra in-formation other than the hourly loads is required.
Using NMR Decay-time Measurements to Monitor and Characterize DNAPL and Moisture in Subsurface Porous Media (2007)

Abstract Knowing how environmental properties affect dense nonaqueous phase liquid (DNAPL) solvent flow in the subsurface is essential for developing models of flow and transport in the vadose zone necessary for designing remediation and long-term stewardship strategies. For example, one must know if solvents are flowing in water-wetted or solvent-wetted environments, the pore-size distribution of the region containing DNAPLs, and the impact of contaminated plumes and their transport mechanisms in porous media. Our research investigates the capability and limitations of low-field proton nuclear magnetic resonance (NMR) relaxation decay-rate measurements for determining environmental properties affecting DNAPL solvent flow in the subsurface. The measurements that can be performed with the laboratory low-field system can also be performed in situ in the field with the current generation of commercial borehole logging tools. The oil and gas industry uses NMR measurements in deep subsurface, consolidated formations to determine porosity and hydrocarbon content and to estimate formation permeability. These determinations rely on the ability of NMR to distinguish between water and hydrocarbons in the pore space and to obtain the distribution of pore sizes from relaxation decay-rate distributions. In this paper, we will show how NMR measurement techniques can be used to characterize, monitor, and evaluate the dynamics of mixed fluids (water-DNAPL) in unconsolidated near-surface porous environments, and describe the use of proton NMR T2 (spin-spin relaxation time) measurements in unconsolidated sandy-soil samples to identify and characterize the presence of DNAPLs in these environments. The potential of NMR decay-rate distributions for characterizing DNAPL fluids in the subsurface and understanding their flow mechanisms has not previously been exploited; however, near-surface unsaturated vadose zone environments do provide unique challenges for using NMR measurements. These challenges are addressed through systematic laboratory experiments and a program of research to extend and adapt current field NMR measurements to near-surface environmental problems.