gebhart/patrepeval huggingface dataset:
Highly selective .kappa.-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted cyclohexyl]arylacetamide derivatives (1990)

This paper describes the chemical synthesis, mu/kappa opioid receptor selectivity and analgesic activity of 14 novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted-cyclohexyl]arylacetamide derivatives. The prototype kappa-selective agonist, PD117302 (trans-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzo[b]thiophene-4- acetamide, 2) has been regio- and stereoselectively substituted in the C-4 and C-5 positions of the cyclohexyl ring with the methyl ether and spiro tetrahydrofuran groups. It is observed that optimal mu/kappa-receptor selectivity is obtained when the oxygen atom of the methyl ether or the tetrahydrofuran ring is joined to the equatorial C-4 position. Hence, (-)-(5 beta,7 beta,8 alpha)-N-methyl-N-[7-(1-pyrrolidinyl)-1- oxaspiro[4.5]dec-8-yl]benzo[b]furan-4-acetamide monohydrochloride (21) has exceptionally high kappa opioid receptor affinity and selectivity in vitro (kappa Ki = 0.83 nM, mu/kappa ratio = 1520) is the most potent kappa-selective analgesic ever reported. Compound 21 is 25 times more potent than morphine and 17 times more potent than U-62066 (spiradoline, 19) when assayed by the rat paw pressure test by intravenous administration (MPE50 = 0.024, 0.6, and 0.4 mg/kg, respectively).
Characteristics of the plasma impedance probe with constant bias (2005)

The impedance of a small spherical probe immersed in a uniform plasma is measured by recording the reflection coefficient of an applied signal using a network analyzer. This impedance has a resonance at the plasma frequency where the imaginary part goes to zero, a feature that has made this measurement a good way of determining electron density. When the plasma potential is positive with respect to the sphere—for example, if the sphere is electrically floating or grounded, a second resonance occurs at ω&amp;lt;ωpe due to the capacitance created by the depleted electron density in the sheath. A greatly increased power deposition occurs at this lower resonance, whose frequency can be controlled by applying a dc bias which changes the sheath width. As the bias is increased the value of this frequency becomes smaller until the resonance disappears completely at Vprobe=Vplasma. As the bias is further increased past the plasma potential, an electron sheath forms with its own resonance, which is at a lower frequency than the resonance associated with the ion sheath. The impedance of the electron sheath can be approximated using sheath transit time perturbation theory for a space charge limited diode. As with the ion sheath resonance, the largest energy deposition occurs at the lower of the two resonant frequencies.
Initial phase II experience of ipilimumab (IPI) alone and in combination with radiotherapy (XRT) in patients with metastatic castration-resistant prostate cancer (mCRPC) (2009)

5138 Background: IPI is a fully human, monoclonal anti-CTLA-4 antibody capable of enhancing anti-tumor immunity. In preclinical models, XRT releases tumor antigens and enhances anti-tumor activity of CTLA-4 blockade. In the dose escalation part of this Phase I/II trial 10 mg/kg dosing of IPI with or without prior priming by single fraction XRT was feasible. We now report initial phase II results. Methods: 45 patients (pts) with mCRPC and ECOG PS of 0–1 received 10 mg/kg q3 weeks (wks) X 4 of IPI in 3 groups: (1) IPI alone n=16, (2) IPI + XRT n=15 chemotherapy naïve (NoCHEMO), and (3) IPI + XRT n=14 chemotherapy experienced (CHEMO) pts. XRT (800 cGy) was given to up to 3 involved bony sites (GI tract sparing) just prior to starting IPI. PSA was monitored monthly, with scans q 3 months. Endpoints were to confirm safety and an initial assessment of activity. Results: 17 pts (38%) experienced 26 immune-related adverse events (irAEs) including diarrhea/colitis (12), rash/pruritus (6), hepatitis (4), endocrinopathy (4). 11 pts (24%) experienced 13 ≥ Grade 3 irAEs: GI (9; 20%) and hepatitis (4; 9%); all resolved with immunosuppression. 10 of 45 pts (22%; 95% CI 10–34%) had confirmed PSA declines ≥ 50% as follows in the table below. Median time to PSA decline was 5.7 wks (r 3 to 21 wks); median duration 23 wks (r 3 to 84+ wks). In one pt dosed with IPI alone, PSA ≤ 0.05 ng/ml, as well as a CR of bone, nodal and prostate lesions continue for 54+ and 84+ wks, respectively. Conclusions: irAEs in the 10 mg/kg cohorts are similar in type and rate to IPI in melanoma. irAEs and PSA declines occurred in chemotherapy naïve and post chemotherapy patients, and with or without XRT. Addition of XRT to 10 mg/kg is well tolerated. Time to response can be delayed, with a durable median response of 23 wks. Further study of IPI in mCRPC is warranted, with or without XRT as a potential immunosupportive maneuver to augment clinical responses to IPI. [Table: see text] [Table: see text]
On Learning From Others (2007)

Some people think that the practices of many courts in many countries, or in many relevant countries, offer helpful guidance to courts in other countries, when those courts are approaching hard or novel questions.'In their view, the practices of many courts create a body of law in which other courts should be highly interested.The obvious question is: Why?In The Law of Other States, 2 we attempt to make progress on this question.Our focus was not principally on the use of foreign precedents in the constitutional rulings of the U.S. Supreme Court.We meant to take that controversial and specialized problem as part of a much more general one, which involves courts in one jurisdiction using the decisions of courts in other jurisdictions.Within the United States, state courts frequently refer to the decisions of other state courts, even when construing state constitutions. 3 The high courts of many nations refer to the decisions of high courts of other nations. 4 The problem is that it is not self-evident that the practices of courts A-Y should be taken as valuable or informative for court Z. Exploration of that problem might also illuminate the question of whether and when a legislator or administrator in one state should attend to the decisions of legislators or administrators in other states.Our principal submission was that the problem is helpfully approached through the lens of the Condorcet Jury Theorem (CJT).If many people have (independently) decided that X is true, or that Y is good, the CJT gives us reason, under identifiable conditions, to believe that X is true and that Y is
A comparison of interfacial behaviours of pea (Pisum sativum L.) legumin and vicilin at air/water interface (1986)

Abstract The interfacial behaviours of the two main pea globulins (legumin and vicilin) at water/air interfaces were studied in order to improve the general knowledge concerning the physicochemical basis of the foaming and emulsifying properties of these proteins. The surface tension (γ) was monitored by the WILHELMY plate technique till it reaches a constant value. The final concentration c of the proteins injected in the subphase was comprised between 0.3. 10 −6 and 80. 10 −6 g/ml. The adsorption kinetics γ = f(t) were analyzed using different mathematical relations given in the literature. Different phases can be distinguished, corresponding to the diffusion, penetration and rearrangement of protein molecules at the interface, each phase being characterized by a rate constant and an energy barrier. The rate constants were generally higher in the case of vicilin; in consequence the equilibrium surface pressure π were reached more quickly. The isotherms π e = f (log c ) showed that the concentration needed to reach the plateau value of π e , were respectively about 11.7. 10 6 g/ml and 18.5. 10 −6 g/ml for vicilin and legumin air/water interface. The plateau value of π e , was about the same for both proteins at air/water interface (24.5 mN/m). For lower concentrations, vicilin gave higher values for ne. The areas per molecule in the adsorbed monolayer were about the same for vicilin (1.05 nm 2 ) and legumin (1.04 nm 2 ) at air/water interface. By studying the surface properties of vicilin/legumin mixtures it was observed that π e increased with increasing relative concentration of vicilin and that inhibiting interactions occured between the two globulins, legumin adsorption being more disturbed by vicilin than the opposite. According to these results, the differences between legumin and vicilin can be related to their molecular characteristics. Pea globulins and especially vicilin appeared to be efficient proteins as surface active agents.
Ultrasonic irradiation assisted efficient regioselective synthesis of CF3-containing pyrazoles catalyzed by Cu(OTf)2/Et3N (2013)

Cu(OTf)2/Et3N catalyst showed a great advantage over all the investigated catalysts, and the ultrasonic irradiation method offered high yields of pyrazoles in short reaction time compared with classical conditions. gHMBC spectra of the product were used to rationalize the observed regioselectivity.
Novel surface lipids of diapausing Manduca sexta pupae. Long chain oxoalcohol esters of acetoacetic, hydroxybutyric, and acetic acids. (1984)

Ester components in the surface wax from diapausing tobacco hornworm pupae, Manduca sexta L., were separated by thin layer chromatography and gas-liquid chromatography, and characterized by infrared spectroscopy and gas-liquid chromatography-mass spectrometry. Three groups of esters were identified as natural derivatives of acetic acid, acetoacetic acid, and 3-hydroxybutyric acid. The major ester fraction was identified as a mixture of C26 (10%), C27 (5%), and C28 (85%) oxoalcohol esters of acetoacetic acid. The major homolog consisted of equal amounts of 11-oxooctacosanyl 3-oxobutanoate and 12-oxooctacosanyl 3-oxobutanoate. Lesser amounts of 11- and 12-oxooctacosanyl and n-octacosanyl esters of acetic and 3-hydroxybutyric acids were also identified. The chain length distributions of these C26, C27, and C28 oxoalcohol and n-primary alcohol ester moieties, as well as the isomeric ratios for the 11- and 12-oxoalcohol isomers, were similar to the oxoaldehydes and unesterified oxoalcohols previously identified by Buckner et al (Buckner, J. S., Nelson, D. R., Haak, H., and Pomonis, J. G. (1984) J. Biol. Chem. 259, 8452-8470) as lipid components of the surface wax of M. sexta pupae.
Grapevine Rootstocks Differentially Affect the Rate of Ripening and Modulate Auxin-Related Genes in Cabernet Sauvignon Berries (2016)

In modern viticulture, grafting commercial grapevine varieties on interspecific rootstocks is a common practice required for conferring resistance to many biotic and abiotic stresses. Nevertheless, the use of rootstocks to gain these essential traits is also known to impact grape berry development and quality, although the underlying mechanisms are still poorly understood. In grape berries, the onset of ripening (véraison) is regulated by a complex network of mobile signals including hormones such as auxins, ethylene, abscisic acid, and brassinosteroids. Recently, a new rootstock, designated M4, was selected based on its enhanced tolerance to water stress and medium vigor. This study investigates the effect of M4 on Cabernet Sauvignon (CS) berry development in comparison to the commercial 1103P rootstock. Physical and biochemical parameters showed that the ripening rate of CS berries is faster when grafted onto M4. A multifactorial analysis performed on mRNA-Seq data obtained from skin and pulp of berries grown in both graft combinations revealed that genes controlling auxin action (ARF and Aux/IAA) represent one of main categories affected by the rootstock genotype. Considering that the level of auxin tightly regulates the transcription of these genes, we investigated the behavior of the main gene families involved in auxin biosynthesis and conjugation. Molecular and biochemical analyses confirmed a link between the rate of berry development and the modulation of auxin metabolism. Moreover, the data indicate that this phenomenon appears to be particularly pronounced in skin tissue in comparison to the flesh.
Human-Analytics in Information Systems Research and Applications in Personnel Selection (2018)

The human body provides a wealth of information that, when captured and analyzed, offers deep insight into the mind and its processes. At no other point in history has this information been as accessible as it is today. Using various sensor systems, researchers can now efficiently capture fine-grain behavioral data and leverage it for scientific insight. This dissertation begins by reviewing the capture and use of human-data from an information systems perspective in which the objective is to provide organizational value. The dissertation then proposes a scalable interview system for the collection and analysis of verbal and nonverbal human behaviors. Following design science principles, a proof-of-concept prototype system is created and evaluated in the context of personnel-selection. The prototype system comprises a highly structured interview paradigm and uses a standard web-camera to record interviewees. Experiment 1 evaluates the system’s ability to replicate subjective human judgements of source credibility. Experiment 2 then assesses the system’s ability to predict objective measures of general mental ability and job knowledge. During each experiment, study participants conduct mock job interviews using the prototype system. Participants respond to a series of interview questions related to a mock-job description. Behavioral features are extracted from facial displays, voice characteristics, and language usage captured by video recordings. In Experiment 1, participant performance is assessed using third-party raters. In Experiment 2, participants complete computerized assessments of general mental ability and job skills following the interview. Assessments and behavioral measures are then processed with predictive machine learning algorithms. The results indicate that subjective and objective measures of job performance can be inferred at rates considerably above chance using automated analysis of human behaviors. This research provides insight into the design principles that allow for human-analytics to become part of organizations’ day-to-day processes.
FEM based thermal model of an agrivoltaic system (2022)

This study aims at building a finite element model of an agrivoltaic system for thermal simulation. The system under consideration consists of an array of PV modules over a shadenet covering an array of plant crops. The plant crops are modelled as porous mediums for computing air flow. The solar radiative energy recieved by the various components of the system is computed using the surface to surface radiation equations. Heat loss in PV modules and plants by convection is modelled. This model also accounts for heat loss in plants through evaporative cooling. The physical properties of plants are assumed from literature. Properties that need experimental determination are treated as variable parameters.
Sex differences in antihypertensive treatment in France among 17 856 patients in a tertiary hypertension unit (2018)

Blood pressure control has greatly improved over the last 15 years in both men and women. Although the treatment choice remained strongly dependent on sex, this is not justified by a sex-related difference in cardiovascular benefit from antihypertensive treatment.
Synthesis and performance of ester quaternary biodegradable softeners (1994)

Abstract Reaction of hydroxyethylpiperazine with two moles of fatty acid, followed by quaternization with methyl chloride, methyl bromide or dimethyl sulfate, resulted in new quaternaries useful as biodegradable fabric softeners. Additional softeners were synthesized from hard tallow propane diamine by reaction with butyrolactone, followed by ethoxylation, esterification with one mole of fatty acid and quaternization.
Hybrid Modelling and Control of Obstacle-Aided Snake Robot Locomotion (2010)

A snake can traverse cluttered and irregular environments by using irregularities around its body as push points to aid the propulsion. This characteristic feature of biological snake locomotion, which is denoted as obstacle-aided locomotion, is investigated for snake robot locomotion purposes in this paper. The paper presents a hybrid model of the dynamics of a planar snake robot interacting with obstacles in its environment. Obstacle contact forces are calculated by formulating and solving a linear complementarity problem (LCP). The existence and uniqueness properties of the state evolution of the hybrid model are investigated. The paper also presents a hybrid control strategy employing measured contact forces to maintain propulsion while simultaneously preventing the snake robot from being jammed between obstacles in its path. The simulation results validate the hybrid modelling approach and the effectiveness of the proposed control strategy.
Benchmarking of triaxial failure criteria for composite laminates: Comparison between models of ‘Part (A)’ of ‘WWFE-II’ (2012)

As a part of the Second World-Wide Failure Exercise, the originators (or their collaborators) of three-dimensional failure theories applied their methods to 12 carefully selected challenging problems (test cases). In this article, the ‘blind’ theoretical predictions from 12 failure theories, making the backbone of Part (A) of the Second World-Wide Failure Exercise, are compiled in a structured manner. Key features in each theory are identified including: types of failure models employed, whether linear or nonlinear analysis was carried out, reliance on software and numerical methods, allowance for thermal stresses and identification of modes of failure. The results (failure envelopes and stress–strain curves) have been superimposed to show similarities and differences between the predictions of the various theories. In addition, bar charts have been constructed to demonstrate the levels of agreement between the predicted failure stresses and strains. Sources of differences between the predictions of the various three-dimensional failure theories are discussed. Further publications are planned in Part B in which comparison will be made between the predictions described here and the experimental results.
Epithelial properties of human colonic carcinoma cell line Caco-2: electrical parameters (1984)

Human colonic carcinoma Caco-2 cells grown in vitro undergo epithelial differentiation. Electrical measurements showed that they form resistant monolayers of polarized cells. On millipore filters, transepithelial electrical resistance (154 +/- 6.5 omega X cm2) was accompanied by a small potential difference (0.29 +/- 0.02 mV, serosal side positive) and by short-circuit current (1.9 +/- 0.14 microA X cm-2), both of which were ouabain sensitive. Micropuncture of domes formed on plastic supports under standard culture conditions revealed electrical polarity similar to that of filter-grown cells (0.8 +/- 0.2 mV, serosal side positive) combined with a highly negative cytoplasm (-57 +/- 1 mV) and very marked cell asymmetry (76% of total electrical cell resistance was located in the mucosal membrane). These parameters were not affected by the diuretic amiloride nor the hormone aldosterone, suggesting that sodium conductance is very limited in the mucosal membrane. Addition to the mucosal side of the ionophore nystatin or amphotericin B unmasked the possibility of high electrical transport activity. Electrical measurements made it possible to define the epithelial properties of Caco-2 cells, which may resemble those of colonic crypt or fetal cells. These measurements also confirmed that functional differentiation is homogeneous in Caco-2 cells. It is suggested that dome cell micropuncture may be useful in investigating the functional properties of other dome-forming cell lines.
GalVR (2017)

GalVR is a navigation interface that uses galvanic vestibular stimulation (GVS) during walking to cause users to turn from their planned trajectory. We explore GalVR for collaborative navigation in a two-player virtual reality (VR) game. The interface affords a novel game design that exploits the differences in first and third person perspectives, allowing VR and non-VR users to share a play experience. By introducing interdependence arising from dissimilar points of view, players can uniquely contribute to the shared experience based on their roles. We detail the design of our asymmetrical game, Dark Room and present some insights from a pilot study. Trust emerged as the defining factor for successful play.
Defect/Interface Recombination Limited Quasi-Fermi Level Splitting and Open-Circuit Voltage in Mono- and Triple-Cation Perovskite Solar Cells (2020)

Multication metal-halide perovskites exhibit desirable performance and stability, compared to their monocation counterparts. However, the study of the photophysical properties and the nature of defect states in these materials is still a challenging and ongoing task. Here, we study bulk and interfacial energy loss mechanisms in solution-processed MAPbI<sub>3</sub> (MAPI) and (CsPbI<sub>3</sub>)<sub>0.05</sub>[(FAPbI<sub>3</sub>)<sub>0.83</sub>(MAPbBr<sub>3</sub>)<sub>0.17</sub>]<sub>0.95</sub> (triple cation) perovskite solar cells using absolute photoluminescence (PL) measurements. In neat MAPI films, we find a significantly smaller quasi-Fermi level splitting than for the triple cation perovskite absorbers, which defines the open-circuit voltage of the MAPI cells. PL measurements at low temperatures (∼20 K) on MAPI films demonstrate that emissive subgap states can be effectively reduced using different passivating agents, which lowers the nonradiative recombination loss at room temperature. We conclude that while triple cation perovskite cells are limited by interfacial recombination, the passivation of surface trap states within the MAPI films is the primary consideration for device optimization.
Synthesis of Cyclic Aza-Ether Compounds and Studies of Their Use as Anion Receptors in Nonaqueous Lithium Halide Salts Solution (2000)

A series of new anion receptors, based on cyclic aza‐ether compounds, have been synthesized. The synthesis and characterization of these compounds are described. In all these cyclic aza‐ether compounds, the electron‐withdrawing group was attached to each of the nitrogen atoms. Each member of this class of compounds contains a different number of nitrogen atoms. When used as additives, all of them can significantly increase the ionic conductivity of lithium halide salts in tetrahydrofuran solutions due to the ion‐pair dissociation effect. This ion‐pair dissociation effect is a result of complexation between these compounds and the halide anions. Ionic conductivity studies show that the complexation behavior is related to both the ring structure of the cyclic compounds and the characteristics of the halide anions. X‐ray diffraction data show that the diffraction patterns of the complex crystals grown from cosolution of the cyclic aza‐ether compound and lithium halide salts are completely different than those from the pure cyclic aza‐ether compounds. New Bragg peaks representing a large d‐spacing (∼15 Å) are observed for the complex crystals. This is clear evidence of the complexation between the cyclic aza‐ether compound and halide anions. © 2000 The Electrochemical Society. All rights reserved.
Cell membrane electroporation-Part 3: the equipment (2014)

As described in Part 1, a cell membrane can be made permeable to various molecules by carrying out a procedure called electroporation [1]. This procedure is being successfully used in biology, biotechnology, and medicine [2], [3]. It requires electroporators and electrodes. An electroporator generates short HV pulses of specific shape, amplitude, duration, number, and repetition frequency [4], and the pulses are applied to the target cells or load through the electrodes [5]. The energy delivered to the load is governed by the number of pulses and the pulse voltage, current, and duration. In biomedical applications that energy can be several joules; in biotechnology, where electroporation is used for treatment of agricultural products and water, it can be several kilojoules.