gebhart/patrepeval huggingface dataset:
A novel series of selective, non-peptide inhibitors of angiotensin II binding to the AT2 site (1993)

The availability of peptide and non-peptide Ang II receptor antagonists has permitted the study of Ang II receptor heterogeneity. It is now widely recognized that there are at least two distinct Ang II receptor subtypes. AT1 receptors are selective in their recognition of agents such as losartan, DuP 532, L-158,809, SK&F108566, and similar non-peptides. To date, all of the well-known actions of Ang II in mammals are blocked by the AT1 selective antagonists such as losartan and are thus designated as being mediated by the AT1 receptor. Although there have been reports of functional activity mediated through AT2 sites, the pharmacological role for the AT2 receptor has not yet been elucidated. Herein, we report the chemistry and SAR on a novel series of 1,2,3,4-tetrahydrosioquinoline-3-carboxylic acids which have selective affinity for AT2 receptors. The most potent of which (19) has an IC50 of 30 nM for the AT2 receptor in the rat adrenal radioligand binding assay.
M1 and M3 muscarinic antagonists inhibit human nasal glandular secretion in vitro (1992)

Mucus glycoproteins (MGP) are high-molecular-weight glycoconjugates that are released from submucosal glands and epithelial goblet cells in the respiratory tract. Muscarinic receptors have an important role in the regulation of human nasal glandular secretion and mucus production, but it is not known which of the five muscarinic receptor subtypes are involved. The effect of nonselective and M1-, M2-, and M3-selective muscarinic antagonists on methacholine (MCh)-induced MGP secretion from human nasal mucosal explants was tested in vitro. MGP was assayed by enzyme-linked immunosorbent assay using a specific anti-MGP monoclonal antibody (7F10). MCh (100 microM) induced MGP secretion up to 127% compared with controls. MCh-induced MGP release was significantly inhibited by atropine (100 microM), the M, receptor antagonist pirenzepine (10-100 microM), and the M3 receptor antagonist 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP; 1-100 microM). 4-DAMP significantly inhibited MCh-induced MGP release at a lower concentration (1 microM) than pirenzepine (10 microM). The M2 receptor antagonists AF-DX 116 and gallamine (both at 100 microM) had no effect. No antagonist alone had a significant effect on MGP release. These results indicate that the M1 and M3 muscarinic receptor subtypes regulate MGP secretion from human nasal mucosa and suggest that the M3 receptor has the predominant effect.
Design elements of binary joint transform correlation and selected optimization techniques (1992)

A new power spectrum binarization technique is introduced that eases experimental implementation while significantly improving binary joint transform correlation performance. Impacts of fundamental design parameters on correlator performance have been evaluated using computer simulations. Realistic images including multiple objects in challenging backgrounds were used to characterize the effects of parameter variations such as threshold levels and low-frequency blocks. The design aspects emphasized were those contributing to ease of experimental implementations, including practical dynamic range limitations and achievable threshold levels. Experimental results using the optimization techniques developed with simulations are given.
Lithium-ion batteries for aerospace (2004)

Under the Mars Surveyor Program (MSP01), lithium-ion batteries were developed by Lithion Inc. (Yardney Technical Products Inc.), each being 28 V, 25 Ah, 8-cells, 9 kg and fully qualified prior to mission cancellation. In addition to the requirement of being able to supply at least 90 cycles on the surface of Mars, the battery was demonstrated to be capable of operation (both charge and discharge) over a large temperature range (-20/spl deg/ to +40/spl deg/C), with tolerance to non-operational excursions to -30/spl deg/ and +50/spl deg/C. After mission cancellation, the batteries delivered to JPL were subjected to generic performance tests to demonstrate the applicability of the technology to meet future NASA aerospace applications. One of the two batteries currently being tested at JPL is undergoing testing according to anticipated performance requirements of future Mars Lander applications. The primary goal of this activity is to determine the performance capability to power surface operation on Mars for a prolonged period (> 3 years) after being subjected to a long cruise period. The second 25 AHr battery is being tested to determine the viability of using lithium-ion technology for future planetary orbiter applications. The test implemented consists of cycling the battery continuously under LEO conditions (30% DOD), while periodically checking the battery impedance and full capacity (100% DOD). Prior to initiating these tests, a number of characterization tests were performed to determine general performance attributes and battery health. In addition to presenting battery data, results obtained with individual cells will also be presented to further describe the capabilities of the technology to meet future applications.
ChemInform Abstract: DECARBOXYLATION OF ALKYLIDENE CYANO‐ESTERS (1979)

Abstract Unter Verwendung von Natrium Chlorid und Wasser in DMSQ erhält man aus Alkyliden‐cyanoestern wie (I) unter Hydrolyse und Decarboxylierung die ungesättigten Nitrile wie (II).
Target 2035 – an update on private sector contributions (2023)

Target 2035, an international federation of biomedical scientists from the public and private sectors, is leveraging 'open' principles to develop a pharmacological tool for every human protein. These tools are important reagents for scientists studying human health and disease and will facilitate the development of new medicines. It is therefore not surprising that pharmaceutical companies are joining Target 2035, contributing both knowledge and reagents to study novel proteins. Here, we present a brief progress update on Target 2035 and highlight some of industry's contributions.
Metabolism and murine pharmacokinetics of the 8-(N,N-dimethylcarboxamide) analogue of the experimental antitumor drug mitozolomide (NSC353451). (1989)

The in vitro cytotoxicity, stability, and metabolism of the 8-(N,N-dimethylcarboxamide) and 8-(N-methylcarboxamide) analogues of the experimental antitumor drug mitozolomide have been investigated in conjunction with their in vivo murine pharmacokinetics and metabolism. When tested against the TLX5 lymphoma in vitro the ID50 values for dimethylmitozolomide, methylmitozolomide, and mitozolomide were 14.6, 3.0, and 2.3 microM, respectively. The cytotoxicity of dimethylmitozolomide was dramatically increased when it was incubated with murine hepatic microsomes. There was no significant difference in the in vitro stabilities of dimethylmitozolomide and methylmitozolamide with half-lives of 43.5 and 45.8 min, respectively, in RPMI at 37 degrees C. The in vitro microsomal incubation of dimethylmitozolomide produced significant amounts of methylmitozolomide, which suggests that methylmitozolomide contributed to the cytotoxicity of dimethylmitozolomide in the presence of microsomes. The pharmacokinetics of both dimethylmitozolomide and methylmitozolomide, given i.p. at 10 mg/kg, were investigated in CBA/Ca mice bearing the s.c. solid TLX5 lymphoma. Methylmitozolomide was absorbed rapidly with maximum plasma and tumor concentrations of 10.66 mg/liter and 8.01 mg/kg, respectively, achieved 0.17 h following dosing. Dimethylmitozolomide was also rapidly absorbed with maximum plasma and tumor concentrations of 9.34 mg/liter and 5.00 mg/kg, respectively, achieved within 0.18 h of dosing. Following administration of dimethylmitozolomide, methylmitozolomide was found in both plasma and tumor tissue. The plasma and tumor area under the curves of methylmitozolomide were 87.7% and 120.8%, respectively, of those seen when mice were dosed with authentic methylmitozolomide. By comparison of the area under the curves and clearance values, it was demonstrated that 89% of the administered dimethylmitozolomide was metabolized via methylmitozolomide.
New Insights on End-Stage Renal Disease and Healthy Individual Gut Bacterial Translocation: Different Carbon Composition of Lipopolysaccharides and Different Impact on Monocyte Inflammatory Response (2021)

Chronic kidney disease induces disruption of the intestinal epithelial barrier, leading to gut bacterial translocation. Here, we appreciated bacterial translocation by analyzing circulating lipopolysaccharides (LPS) using two methods, one measuring only active free LPS, and the other quantifying total LPS as well as LPS lipid A carbon chain length. This was done in end-stage renal disease (ESRD) patients and healthy volunteers (HV). We observed both higher LPS concentration in healthy volunteers and significant differences in composition of translocated LPS based on lipid A carbon chain length. Lower LPS activity to mass ratio and higher concentration of high-density lipoproteins were found in HV, suggesting a better plasma capacity to neutralize LPS activity. Higher serum concentrations of soluble CD14 and pro-inflammatory cytokines in ESRD patients confirmed this hypothesis. To further explore whether chronic inflammation in ESRD patients could be more related to LPS composition rather than its quantity, we tested the effect of HV and patient sera on cytokine secretion in monocyte cultures. Sera with predominance of 14-carbon chain lipid A-LPS induced higher secretion of pro-inflammatory cytokines than those with predominance of 18-carbon chain lipid A-LPS. TLR4 or LPS antagonists decreased LPS-induced cytokine production by monocytes, demonstrating an LPS-specific effect. Thereby, septic inflammation observed in ESRD patients may be not related to higher bacterial translocation, but to reduced LPS neutralization capacity and differences in translocated LPS subtypes.
The slowly reacting mode of combustion of gaseous mixtures in spherical vessels. Part 2: Buoyancy-induced motion and its effect on the explosion limits (2016)

This paper investigates the effect of buoyancy-driven motion on the quasi-steady ‘slowly reacting’ mode of combustion and on its thermal-explosion limits, for gaseous mixtures enclosed in a spherical vessel with a constant wall temperature. Following Frank-Kamenetskii's seminal analysis of this problem, the strong temperature dependence of the effective overall reaction rate is taken into account by using a single-reaction model with an Arrhenius rate having a large activation energy, resulting in a critical value of the vessel radius above which the slowly reacting mode of combustion no longer exists. In his contant-density, convection-free analysis, the critical conditions were found to depend on the value of a Damköhler number, defined as the ratio of the time for the heat released by the reaction to be conducted to the wall, to the homogeneous explosion time evaluated at the wall temperature. For gaseous mixtures under normal gravity, the critical Damköhler number increases through the effect of buoyancy-induced motion on the rate of heat conduction to the wall, measured by an appropriate Rayleigh number . In the present analysis, for small values of , the temperature is given in the first approximation by the spherically symmetric Frank-Kamenetskii solution, used to calculate the accompanying gas motion, an axisymmetric annular vortex determined at leading order by the balance between viscous and buoyancy forces, which we call the Frank-Kamenetskii vortex. This flow is used in the equation for conservation of energy to evaluate the influence of convection on explosion limits for small , resulting in predicted critical Damköhler numbers that are accurate up to values of on the order of a few hundred.
Digestibility of fatty acid monomers, dimers and polymers in the rat (1992)

This study was designed to determine digestibilities of fatty acid monomers, dimers and polymers as components of diets containing thermally oxidized oils. Male Wistar rats were fed semipurified diets supplemented with unheated, heated and a 1:1 mixture of unheated/heated olive oils at 6, 12 and 20% w/w of diet. In a 14‐d experimental period, fecal lipids were extracted and analyzed by a combination of adsorption and high‐performance size‐exclusion chromatographies. Thus, it was possible to separate and quantitate five groups of fatty acids—nonpolar monomers, oxidized monomers, nonpolar dimers, oxidized dimers and polymers. Nonpolar fatty acid monomers showed high digestibilities, although significantly influenced by the alteration level of the dietary oil. The apparent absorption of oxidized fatty acid monomers averaged 76.6%. Among polymeric fatty acids, the lowest digestibilities were found for nonpolar dimers (10.9% on average), whereas oxidized dimers and polymers possessed higher apparent absorbability than expected, ranging from 22.7% to 49.6%. Chemical modifications prior to absorption, leading to less complex products, may have contributed to enhanced digestibility of polymers.
On-Chip Group Velocity Dispersion Compensation using Coupled Chirped Vertical Gratings (2009)

Coupled chirped vertical gratings are proposed for on-chip group velocity dispersion compensation. The device is studied using finite-difference time domain simulations and fabricated. The device circumvents the need for directional couplers to redirect compensated data.
UV scanning for SOI defectivity monitoring (2006)

This paper shows how a new generation of inspection system enables us to monitor SOI as requested in the ITRS roadmaps; it shows also the large amount of key information we can collect, giving us important feedback on the SOI process.
Schizosaccharomyces pombe Carboxyl-terminal Domain (CTD) Phosphatase Fcp1 (2004)

Schizosaccharomyces pombe Fcp1 is an essential protein serine phosphatase that preferentially dephosphorylates Ser(2) of the RNA polymerase II C-terminal domain (CTD) heptad repeat Y(1)S(2)P(3)T(4)S(5)P(6)S(7). Here we show that: (i) Fcp1 acts distributively during the hydrolysis of substrates containing tandem Ser(2)-PO(4) heptads; (ii) the minimal optimal CTD substrate for Fcp1 is a single heptad of phasing S(5)P(6)S(7)Y(1)S(2)P(3)T(4); and (iii) single alanine mutations of flanking residues Tyr(1) or Pro(3) result in 6-fold decrements in CTD phosphatase activity. Fcp1 belongs to the DXDX(T/V) family of phosphotransferases that act via an acyl-phosphoenzyme intermediate. An alanine scan of 11 conserved positions of S. pombe Fcp1 identifies Thr(174), Tyr(237), Thr(243), and Tyr(249) as important for phosphatase activity. Structure-activity relationships at these positions were determined by introducing conservative substitutions. Our results, together with previous mutational studies, highlight a constellation of 11 amino acids that are conserved in all Fcp1 orthologs and likely comprise the active site.
Quantitative Determination of Loadings and Oxidation Products of Polystyrene-Bound Phosphines Using <sup>31</sup>P MAS NMR (2003)

The use of (31)P magic angle spinning (MAS) NMR for the quantitative determination of resin loadings and the building up of oxidation products was investigated. Loadings of polystyrene-bound phosphines were evaluated via addition of triphenyl phosphate as reference compound. Results for a series of phosphines are consistent with those obtained from well-established analytical methods. The compounds were also investigated with (13)C MAS NMR, and the individual oxidation stabilities were monitored under oxygen atmosphere.
Influence of trace erythromycin and erythromycin-H2O on carbon and nutrients removal and on resistance selection in sequencing batch reactors (SBRs) (2009)

Three sequencing batch reactors (SBRs) were operated in parallel to study the effects of trace erythromycin (ERY) and ERY-H2O on the treatment of a synthetic wastewater. Through monitoring (1) daily effluents and (2) concentrations of nitrogen (N) and phosphorous (P) in certain batch cycles of the three reactors operated from transient to steady states, the removal of carbon, N, and P was affected negligibly by ERY (100 microg/L) or ERY-H2O (50 microg/L) when compared with the control reactor. However, through analyzing microbial communities of the three steady state SBRs on high-density microarrays (Phylo-Chip), ERY, and ERY-H2O had pronounced effects on the community composition of bacteria related to N and P removal, leading to diversity loss and abundance change. The above observations indicated that resistant bacteria were selected upon exposure to ERY or ERY-H2O. Shortterm batch experiments further proved the resistance and demonstrated that ammonium oxidation (56-95%) was inhibited more significantly than nitrite oxidation (18-61%) in the presence of ERY (100, 400, or 800 microg/L). Therefore, the presence of ERY or ERY-H2O (at microg/L levels) shifted the microbial community and selected resistant bacteria, which may account for the negligible influence of the antibiotic ERY or its derivative ERY-H2O (at microg/L levels) on carbon, N, and P removal in the SBRs.
Erratum: ‘‘The generation of noise in impinging vortex motion past a step’’ [Phys. Fluids <b>2</b> <b>8</b>, 3004 (1985)] (1986)

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Large-area low-noise flexible organic photodiodes for detecting faint visible light (2020)

Silicon photodiodes are the foundation of light-detection technology; yet their rigid structure and limited area scaling at low cost hamper their use in several emerging applications. A detailed methodology for the characterization of organic photodiodes based on polymeric bulk heterojunctions reveals the influence that charge-collecting electrodes have on the electronic noise at low frequency. The performance of optimized organic photodiodes is found to rival that of low-noise silicon photodiodes in all metrics within the visible spectral range, except response time, which is still video-rate compatible. Solution-processed organic photodiodes offer several design opportunities exemplified in a biometric monitoring application that uses ring-shaped, large-area, flexible, organic photodiodes with silicon-level performance.
A Study of Precoding for LTE TDD Using Cell Specific Reference Signals (2010)

We investigate non-codebook-based multiple-input multiple-output (MIMO) precoding schemes for the time division duplex (TDD) mode of LTE where channel reciprocity could be exploited. Previously proposed non-codebook-based precoding schemes typically use UE specific reference signals for demodulation. Cell specific reference signals are however still transmitted for the transmission of common control signaling, mobility measurements and downlink channel quality measurements. In order to save the resources occupied by UE specific reference signals, and to simplify UE implementation, a non-codebook-based precoding scheme using cell-specific reference signals is considered. Link throughput simulations indicate that such scheme outperforms the scheme using UE specific reference signals in the scenario with high transmit antenna correlation and low UE velocity.
Enhanced cognitive demodulation with artificial intelligence (2020)

The low-cost 'THz Torch' wireless link technology is still in its infancy. Until very recently, inherent limitations with available hardware has resulted in a modest operational figure of merit performance (Range [Formula: see text] Bit Rate). However, a breakthrough was reported here by the authors, with the introduction of 'Cognitive Demodulation'. This bypassed the thermal time constant constraints normally associated with both the thermal emitter and sensor; allowing step-change increases in both Range and Bit Rate with direct electronic modulation. This paper concentrates on advancements to the bit error rate (BER) performance. Here, separate techniques are introduced to the demodulation software that, when combined, result in enhanced Cognitive Demodulation. A factor of more than 100 improvement in BER was demonstrated within the laboratory and approximately a 60-fold improvement in a non-laboratory environment; both at the maximum Range and Bit Rate of 2 m and 125 bps, respectively, demonstrated recently. Moreover, demodulation speed is increased by almost a factor of 10,000; allowing for real-time demodulation while easing future computational hardware requirements. In addition to these software advancements, the paper demonstrates important improvements in hardware that has brought the technology out of the laboratory, with field trials being performed within an office corridor.
What do thiobarbituric acid and hemoglobin-methylene blue tests evaluate in the endogenous lipid peroxidation of rat liver? (1989)

To detect the endogenous lipid peroxides in rat liver, the thiobarbituric acid (TBA) and hemoglobin-methylene blue (HMB) tests were used. The endogenous lipid peroxidation in rat liver was induced by peroxidative drugs, and then these tests were carried out. When CCl4, paraquat or phenobarbital was intraperitoneally injected, the HMB values were significantly increased only at the early period after the doses (1h), whereas two peaks of TBA value were observed at 1h and around 24h after the doses. When peroxidation was induced by thiopental or alcohol, the TBA value also gave two peaks. It was suggested that the agreement between detections by both HMB and TBA (the early peak) indicated the peroxide formation, and that the independent increase in TBA value (second peak) the accumulation of aldehydes in the liver. The life span of HMB-reactive substances was short in vivo compared with that of the TBA-reactive substances. It is considered that the TBA test was useful to detect the endogenous lipid peroxidation under the conditions that TBA test could detect aldehydes originating from lipid peroxidation because lipid peroxides were unstable in vivo.
S2CMAF: Multi-Method Assessment Fusion for Scan-to-CAD Methods (2022)

Scan-to-CAD-based 3D reconstruction of indoor environments has become increasingly more popular in recent years. The inherent structure of Scan-to-CAD consists of object detection, model retrieval, and alignment. Therefore, a variety of metrics are required to assess these three aspects. This can lead to ambiguous evaluation results and incorrect quality assumptions. To impede the problem of incorrect evaluation, we introduce S2CMAF, a multi-method assessment fusion approach for Scan-to-CAD pipelines. S2CMAF merges several metrics used in evaluating these pipelines into one unique quality score. We show that S2CMAF significantly improves the correlation between Scan-to-CAD results and the ground truth, compared to the conventionally used Scan2CAD benchmark. Additionally, we train S2CMAF using different optimization techniques and demonstrate the advantages of our approach on real-world data.
An Unusually Shallow Distance-Dependence for Triplet-Energy Transfer (2000)

Long-range interactions over 50 Å allow electron exchange to proceed in a series of conformationally constrained Ru/Os polypyridine complexes (see picture). The dynamics of the intramolecular electron exchange indicate that the connecting 1,4-diethynylated-2,5-dialkoxybenzene units act independently as superexchange mediators. Even with five such units linked together there is no indication for the population of a connector-based triplet state.
Measurement of digital noise in mixed-signal integrated circuits (1995)

This paper proposes a method of measuring the influence of digital noise on analog circuits using wide-band voltage comparators as noise detectors. Noise amplitude and r.m.s voltage are successfully measured by this method. A test chip is fabricated to measure the digital noise influence. From the experimental results, it is shown that the digital noise influence can be considerably reduced by using a differential configuration in analog circuits for mixed-signal IC's. The digital noise influence can be further reduced by lowering the digital supply voltage. These results show that the voltage-comparator-based measuring method is effective in measuring the influence of digital noise on analog circuits.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>