gebhart/patrepeval huggingface dataset:
Cannabinoid Suppression of Noxious Heat-Evoked Activity in Wide Dynamic Range Neurons in the Lumbar Dorsal Horn of the Rat (1999)

The effects of cannabinoid agonists on noxious heat-evoked firing of 62 spinal wide dynamic range (WDR) neurons were examined in urethan-anesthetized rats (1 cell/animal). Noxious thermal stimulation was applied with a Peltier device to the receptive fields in the ipsilateral hindpaw of isolated WDR neurons. To assess the site of action, cannabinoids were administered systemically in intact and spinally transected rats and intraventricularly. Both the aminoalkylindole cannabinoid WIN55,212-2 (125 microg/kg iv) and the bicyclic cannabinoid CP55,940 (125 microg/kg iv) suppressed noxious heat-evoked activity. Responses evoked by mild pressure in nonnociceptive neurons were not altered by CP55,940 (125 microg/kg iv), consistent with previous observations with another cannabinoid agonist, WIN55,212-2. The cannabinoid induced-suppression of noxious heat-evoked activity was blocked by pretreatment with SR141716A (1 mg/kg iv), a competitive antagonist for central cannabinoid CB1 receptors. By contrast, intravenous administration of either vehicle or the receptor-inactive enantiomer WIN55,212-3 (125 microg/kg) failed to alter noxious heat-evoked activity. The suppression of noxious heat-evoked activity induced by WIN55,212-2 in the lumbar dorsal horn of intact animals was markedly attenuated in spinal rats. Moreover, intraventricular administration of WIN55,212-2 suppressed noxious heat-evoked activity in spinal WDR neurons. By contrast, both vehicle and enantiomer were inactive. These findings suggest that cannabinoids selectively modulate the activity of nociceptive neurons in the spinal dorsal horn by actions at CB1 receptors. This modulation represents a suppression of pain neurotransmission because the inhibitory effects are selective for pain-sensitive neurons and are observed with different modalities of noxious stimulation. The data also provide converging lines of evidence for a role for descending antinociceptive mechanisms in cannabinoid modulation of spinal nociceptive processing.
Real-time Traffic Flow Forecasting Based on MW-AOSVR (2009)

Accurate traffic flow forecasting is the key to the development of intelligent transportation systems (ITS). However, the classical forecasting method using the support vector regression (SVR) based on RBF kernel does not support online learning and has the problems of information loss, long processing time, low robustness and so on. An effective Marr Wavelet kernel which we combine the wavelet theory with AOSVR (MW-AOSVR) to construct for traffic flow forecasting is presented in this paper. The forecasting performance of MW-AOSVR is evaluated by real-time traffic flow data of southbound US 101 Freeway, in Los Angeles, USA and a variety of experiments are carried out. The experimental results demonstrate that the proposed approach with Marr Wavelet kernel provides more optimal performance than that with radial basis function (RBF) kernel and has much more precise forecasting rate and higher efficiency, especially for boundary approximation.
K252a, KT5720, KT5926, and U98017 support paclitaxel (taxol)-dependent cells and synergize with paclitaxel. (1994)

We have used paclitaxel-dependent Tax 2-4 cells to screen for compounds that have paclitaxel-like functional activity. The indolocarbazole serine/threonine kinase inhibitor K252a and analogues such as KT5926, KT5720, and K252b partially support the growth of the paclitaxel-dependent cells in the absence of paclitaxel. A novel kinase inhibitor of similar structure, U98017, supports the growth of the dependent cells to 48% of that seen with paclitaxel. Used in combination with paclitaxel, these compounds reduce the amount of paclitaxel required for maximum growth of the dependent cells. Isobologram analysis demonstrates that these compounds also act synergistically with paclitaxel to promote toxicity in wild-type Chinese hamster ovary cells. These selected indolocarbazoles may act at sites distinct from that of paclitaxel and may specifically inhibit kinases that contribute to the destabilization of microtubules. Other indolocarbazoles such as staurosporine and rebeccamycin do not support paclitaxel-dependent cell growth. Structurally unrelated serine/threonine kinase inhibitors such as H-9 and H-7 or tyrosine kinase inhibitors such as lavendustin do not support the growth of these cells. These results define a screen for functional paclitaxel analogues and suggest that it may be useful to investigate the possible synergy of selected indolocarbazoles and paclitaxel in vivo.
Doctors asked to take pledge to shun drug company freebies (2001)

Organizers hope that a new program in Edmonton will help bridge the gap between academic and clinical ethics. The Royal Alexandra Hospital program offers ethicists a year-long lesson in ethical issues that arise at the bedside. “Many hospitals have hired ethicists with a very strong theoretical
Multiple convolutional neural networks for facial expression sequence recognition (2018)

<p>As an important part of the human-computer interaction system, facial expression recognition has been a hot research field. The convolutional neural network cannot recognize expression sequence although it can train the classification features automatically for the reason that the direction of feature training need to be specified manually. In order to solve this problem, this paper improves the network structure, and proposes a multi convolutional network fusion method that can be used to identify the expression sequences containing multiple frames. First, we construct a number of convolutional neural networks, so that each network processes one frame, and then merge the results in the merge layer, and finally pass the softmax classifier to give the identity result. On the CK+facial expression database, experiments are carried out on the 3rd, 4th and 5th frames of expression sequences, and a high recognition rate is obtained for all experiments. &copy; 2018, The Editorial Board of Journal of Xidian University. All right reserved.</p>
Comparison of buprenorphine and pethidine given intravenously on demand to relieve postoperative pain. (1979)

In a double-blind study of on-demand intravenous analgesia buprenorphine was found to be about 600 times as potent as pethidine. The incidence of side effects was similar with both drugs. The quality of analgesia, subjectively assessed, was good with both drugs using this method of administration. Provided that its low potential for abuse is substantiated, buprenorphine appears to be a powerful analgesic that may successfully be given intravenously on demand.
Tendencias observadas en España en precipitación y temperatura. (2011)

La Agencia Estatal de Meteorologia (AEMET) tiene entre sus misiones la observacion y archivo de datos climatologicos atmosfericos que permiten proporcionar informacion a un amplio abanico de usuarios. En esta breve contribucion se pretende presentar algunos resultados de las tendencias observadas sobre Espana peninsular e Islas Baleares para precipitacion y temperatura a partir de bases de datos generadas y utilizadas en AEMET para diversos estudios climaticos. Se ha intentado complementar la exhaustiva revision realizada por Blade y Castro-Diez (2010) en el reciente informe “Clima en Espana: pasado, presente y futuro”. Se presentan tambien algunos resultados de este informe para dar una vision de conjunto de las tendencias lo mas completa posible.
Time-Extended Policies in Multi-Agent Reinforcement Learning (2004)

Many algorithms such as Q-learning successfully address reinforcement learning in single-agent multi-time-step problems. In addition there are methods that address reinforcement learning in multi-agent single-time-step problems. However, unmodified single-agent multi-time-step methods and multi-agent single-time-step methods cannot necessarily be combined to solve multi-agent multi-time-step problems due to strong coupling between multi-agent interactions between time steps. Rewards that result in multi-agent collaboration for a single time-step may result in poor collaboration in future time-steps. This paper shows how to avoid this problem.
Influence of alloy additions on oxidation (1989)

Some of the important principles of alloy oxidation are discussed, with emphasis on the formation of protective Cr2O3, Al2O3, and SiO2 scales on iron and nickel base alloys. The competition between internal and external oxidation is considered and it is shown how establishment of the protective layer is influenced by various parameters, including alloy interdiffusion coefficient, oxygen solubility and diffusivity in the alloy, and the relative growth rates of the various oxides. The importance of the transient stage of oxidation is emphasised, with particular reference to the population densities of the initial nuclei of the protective oxide and the rates of growth and coalescence of these particles to develop the healing barrier layer. Consideration is given to the effectiveness of the protective scales in service, with respect to transport processes and mechanical integrity. The influence of the minor alloying elements, manganese, titanium, aluminium, silicon, molybdenum, and niobium, on oxidation of Cr2O3 forming alloys is discussed.MST/1017
The Three-Dimensional Structure of Asn <sup>102</sup> Mutant of Trypsin: Role of Asp <sup>102</sup> in Serine Protease Catalysis (1987)

The structure of the Asn102 mutant of trypsin was determined in order to distinguish whether the reduced activity of the mutant at neutral pH results from an altered active site conformation or from an inability to stabilize a positive charge on the active site histidine. The active site structure of the Asn102 mutant of trypsin is identical to the native enzyme with respect to the specificity pocket, the oxyanion hole, and the orientation of the nucleophilic serine. The observed decrease in rate results from the loss of nucleophilicity of the active site serine. This decreased nucleophilicity may result from stabilization of a His57 tautomer that is unable to accept the serine hydroxyl proton.
Inactivation of the sodium channel. II. Gating current experiments. (1977)

Gating current (Ig) has been studied in relation to inactivation of Na channels. No component of Ig has the time course of inactivation; apparently little or no charge movement is associated with this step. Inactivation nonetheless affects Ig by immobilizing about two-thirds of gating charge. Immobilization can be followed by measuring ON charge movement during a pulse and comparing it to OFF charge after the pulse. The OFF:ON ratio is near 1 for a pulse so short that no inactivation occurs, and the ratio drops to about one-third with a time course that parallels inactivation. Other correlations between inactivation and immobilization are that: (a) they have the same voltage dependence; (b) charge movement recovers with the time coures of recovery from inactivation. We interpret this to mean that the immobilized charge returns slowly to "off" position with the time course of recovery from inactivation, and that the small current generated is lost in base-line noise. At -150 mV recover is very rapid, and the immobilized charge forms a distinct slow component of current as it returns to off position. After destruction of inactivation by pronase, there is no immobilization of charge. A model is presented in which inactivation gains its voltage dependence by coupling to the activation gate.
A mathematical model of an electromechanically coupled poroelastic medium (1987)

Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Mathematics, 1987.
Cell removal with supercritical carbon dioxide for acellular artificial tissue (2008)

Abstract BACKGROUND: The objective of this work was to decellularize artificial tissue without using surfactant solutions. For this purpose, supercritical carbon dioxide was used as the extraction medium. RESULTS: Supercritical carbon dioxide containing a small amount of entrainer was a suitable medium to extract both cell nuclei and cell membranes from artificial tissue. Under gentle extraction conditions (15 MPa, 37 °C), cell nuclei were satisfactorily extracted from tissue within 1 h. In contrast, the efficiency of phospholipid removal depended strongly on the transfer rate of carbon dioxide in the interior of the tissue. Mechanical strength of tissue was not decreased even with prolonged treatment. CONCLUSION: Acellular artificial tissues could be prepared quickly by treatment with a carbon dioxide/entrainer system. The prepared acellular tissue could be obtained in absolutely dry condition. This is advantageous from the viewpoint of long‐term preservation without putrefaction and contamination. Copyright © 2008 Society of Chemical Industry
Imidapril, an Angiotensin-Converting Enzyme Inhibitor, Inhibits Thrombosis via Reduction in Aortic Plasminogen Activator Inhibitor Type-1 Levels in Spontaneously Hypertensive Rats. (1999)

It is known that angiotensin II (Ang II) exerts an antifibrinolytic effect by stimulating synthesis of plasminogen activator inhibitor type-1 (PAI-1), a specific inhibitor of tissue plasminogen activator (t-PA). The aim of this study was to compare the antithrombotic potency of imidapril, an angiotensin-converting enzyme (ACE) inhibitor, and candesartan, an angiotensin II type 1 (AT1) receptor antagonist, in a model of arterial thrombosis in spontaneously hypertensive rats (SHRs). Oral treatment with 5 mg/kg imidapril 1 h before induction of thrombosis resulted in a significant reduction in thrombus weight, whereas candesartan did not affect thrombus weight under the same treatment conditions. Candesartan lowered blood pressure to the same degree as in the imidapril-treated rats. Imidapril not only reduce the serum and aortic ACE activities, but also reduced aortic PAI-1 protein levels, while candesartan had no effect on theses. These results suggest that imidapril, but not the AT1 receptor antagonist, candesartan, enhances fibrinolysis via a reduction of aortic PAI-1 levels by inhibiting ACE and prevents thrombus formation in SHRs.
Identification of a Human Immunodeficiency Virus Type 2 (HIV-2) Encapsidation Determinant and Transduction of Nondividing Human Cells by HIV-2-Based Lentivirus Vectors (1998)

Although previous lentivirus vector systems have used human immunodeficiency virus type 1 (HIV-1), HIV-2 is less pathogenic in humans and is amenable to pathogenicity testing in a primate model. In this study, an HIV-2 molecular clone that is infectious but apathogenic in macaques was used to first define cis-acting regions that can be deleted to prevent HIV-2 genomic encapsidation and replication without inhibiting viral gene expression. Lentivirus encapsidation determinants are complex and incompletely defined; for HIV-2, some deletions between the major 5' splice donor and the gag open reading frame have been shown to minimally affect encapsidation and replication. We find that a larger deletion (61 to 75 nucleotides) abrogates encapsidation and replication but does not diminish mRNA expression. This deletion was incorporated into a replication-defective, envelope-pseudotyped, three-plasmid HIV-2 lentivirus vector system that supplies HIV-2 Gag/Pol and accessory proteins in trans from an HIV-2 packaging plasmid. The HIV-2 vectors efficiently transduced marker genes into human T and monocytoid cell lines and, in contrast to a murine leukemia virus-based vector, into growth-arrested HeLa cells and terminally differentiated human macrophages and NTN2 neurons. Vector DNA could be detected in HIV-2 vector-transduced nondividing CD34(+) CD38(-) human hematopoietic progenitor cells but not in those cells transduced with murine vectors. However, stable integration and expression of the reporter gene could not be detected in these hematopoietic progenitors, leaving open the question of the accessibility of these cells to stable lentivirus transduction.
Selection of top-K influential users based on radius-neighborhood degree, multi-hops distance and selection threshold (2018)

Influence maximization in the social network becomes increasingly important due to its various benefit and application in diverse areas. In this paper, we propose DERND D-hops that adapt the radius-neighborhood degree to a directed graph which is an improvement of our previous algorithm RND d-hops. Then, we propose UERND D-hops algorithm for the undirected graph which is based on radius-neighborhood degree metric for selection of top-K influential users by improving the selection process of our previous algorithm RND d-hops. We set up in the two algorithms a selection threshold value that depends on structural properties of each graph data and thus improves significantly the selection process of seed set, and use a multi-hops distance to select most influential users with a distinct range of influence. We then, determine a multi-hops distance in which each consecutive seed set should be chosen. Thus, we measure the influence spread of selected seed set performed by our algorithms and existing approaches on two diffusion models. We, therefore, propose an analysis of time complexity of the proposed algorithms and show its worst time complexity. Experimental results on large scale data of our proposed algorithms demonstrate its performance against existing algorithms in term of influence spread within a less time compared with our previous algorithm RND d-hops thanks to a selection threshold value.
13[C]-Urea Breath Test as a Novel Point-of-Care Biomarker for Tuberculosis Treatment and Diagnosis (2010)

Urea breath testing may provide a useful diagnostic and biomarker assay for tuberculosis and for treatment response. Future work will test specificity for M. tuberculosis using lung-targeted dry powder inhalation formulations, combined with co-administering oral urease inhibitors together with a saturating oral dose of unlabeled urea, which would prevent the delta(13)CO(2) signal from urease-positive gastrointestinal organisms.
Suitability of AFLP and Microsatellite Marker Analysis for Discriminating Intraclonal Variants of the Potato Cultivar Russet Norkotah (2005)

The objective of this study was to differentiate six intraclonal variants of the potato ( Solanum tuberosum L.) cultivar Russet Norkotah. One-hundred-twelve AFLP primer combinations producing 3755 bands and 79 microsatellite primers producing over 400 bands failed to identify any reproducible polymorphisms among the intraclonal variants and `Russet Norkotah'. The inability to detect differences between clones underscores the degree of genetic similarity between them, despite differences in phenotypic expression. This inability could be due to the tetraploid nature of the clones and/or to epigenetic differences not detected by the utilized procedures.
Polymer Substrates for Optical Discs (1987)

PMMA and PC are widely used as substrate materials for optical discs. Because of its barrier effect inorganic glass is sometimes preferred for DRAW and E-DRAW information carriers. PMMA is little sensitive to orientation and stress birefringence but absorbs water up to 2 wt.-%, thus PMMA substrates being prone to warping. With PC the situation is just the other way round. So we are looking for a polymer which combines low optical anisotropy with reduced water absorption. In view of the additivity of bond polarizabilities we might be able to solve the anisotropy problem via copolymerization and/or blending by compensating positive and negative anisotropies where molecular structure and compatibility are important factors. Process improvements including injection and compression molding as well as extrusion to keep the orientation low compete strongly with these chemical developments. Reduced water absorption may.be achieved by copolymers MMA/St and MMA/CHMA or by special polyolefines and partly by epoxy resins.
Electrochemically Exfoliated Graphene as Solution-Processable, Highly Conductive Electrodes for Organic Electronics (2013)

Solution-processable thin layer graphene is an intriguing nanomaterial with tremendous potential for electronic applications. In this work, we demonstrate that electrochemical exfoliation of graphite furnishes graphene sheets of high quality. The electrochemically exfoliated graphene (EG) contains a high yield (>80%) of one- to three-layer graphene flakes with high C/O ratio of 12.3 and low sheet resistance (4.8 kΩ/□ for a single EG sheet). Due to the solution processability of EG, a vacuum filtration method in association with dry transfer is introduced to produce large-area and highly conductive graphene films on various substrates. Moreover, we demonstrate that the patterned EG can serve as high-performance source/drain electrodes for organic field-effect transistors.
Geometric Deep Learning Autonomously Learns Chemical Features That Outperform Those Engineered by Domain Experts (2018)

Artificial Intelligence has advanced at an unprecedented pace, backing recent breakthroughs in natural language processing, speech recognition, and computer vision: domains where the data is euclidean in nature. More recently, considerable progress has been made in engineering deep-learning architectures that can accept non-Euclidean data such as graphs and manifolds: geometric deep learning. This progress is of considerable interest to the drug discovery community, as molecules can naturally be represented as graphs, where atoms are nodes and bonds are edges. In this work, we explore the performance of geometric deep-learning methods in the context of drug discovery, comparing machine learned features against the domain expert engineered features that are mainstream in the pharmaceutical industry.
Characterization of primary human hepatocytes, HepG2 cells, and HepaRG cells at the mRNA level and CYP activity in response to inducers and their predictivity for the detection of human hepatotoxins (2012)

In the pharmaceutical industry, improving the early detection of drug-induced hepatotoxicity is essential as it is one of the most important reasons for attrition of candidate drugs during the later stages of drug development. The first objective of this study was to better characterize different cellular models (i.e., HepG2, HepaRG cells, and fresh primary human hepatocytes) at the gene expression level and analyze their metabolic cytochrome P450 capabilities. The cellular models were exposed to three different CYP450 inducers; beta-naphthoflavone (BNF), phenobarbital (PB), and rifampicin (RIF). HepG2 cells responded very weakly to the different inducers at the gene expression level, and this translated generally into low CYP450 activities in the induced cells compared with the control cells. On the contrary, HepaRG cells and the three human donors were inducible after exposure to BNF, PB, and RIF according to gene expression responses and CYP450 activities. Consequently, HepaRG cells could be used in screening as a substitute and/or in complement to primary hepatocytes for CYP induction studies. The second objective was to investigate the predictivity of the different cellular models to detect hepatotoxins (16 hepatotoxic and 5 nonhepatotoxic compounds). Specificity was 100% with the different cellular models tested. Cryopreserved human hepatocytes gave the highest sensitivity, ranging from 31% to 44% (depending on the donor), followed by lower sensitivity (13%) for HepaRG and HepG2 cells (6.3%). Overall, none of the models under study gave desirable sensitivities (80-100%). Consequently, a high metabolic capacity and CYP inducibility in cell lines does not necessarily correlate with a high sensitivity for the detection of hepatotoxic drugs. Further investigations are necessary to compare different cellular models and determine those that are best suited for the detection of hepatotoxic compounds.