gebhart/patrepeval huggingface dataset:
Orally Active Adenosine A<sub>1</sub>Receptor Agonists with Antinociceptive Effects in Mice (2012)

Adenosine A1 receptor (A1AR) agonists have antinociceptive effects in multiple preclinical models of acute and chronic pain. Although numerous A1AR agonists have been developed, clinical applications of these agents have been hampered by their cardiovascular side effects. Herein we report a series of novel A1AR agonists, some of which are structurally related to adenosine 5′-monophosphate (5′-AMP), a naturally occurring nucleotide that itself activates A1AR. These novel compounds potently activate A1AR in several orthogonal in vitro assays and are subtype selective for A1AR over A2AAR, A2BAR, and A3AR. Among them, UNC32A (3a) is orally active and has dose-dependent antinociceptive effects in wild-type mice. The antinociceptive effects of 3a were completely abolished in A1AR knockout mice, revealing a strict dependence on A1AR for activity. The apparent lack of cardiovascular side effects when administered orally and high affinity (Ki of 36 nM for the human A1AR) make this compound potentially suitable as a therapeutic.
Benzacridines. I. Synthesis and Reactions of 5,6-Dihydrobenz[c]acridines (1958)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTBenzacridines. I. Synthesis and Reactions of 5,6-Dihydrobenz[c]acridinesVERNON L. BELL and NORMAN H. CROMWELLCite this: J. Org. Chem. 1958, 23, 6, 789–793Publication Date (Print):June 1, 1958Publication History Published online1 May 2002Published inissue 1 June 1958https://pubs.acs.org/doi/10.1021/jo01100a004https://doi.org/10.1021/jo01100a004research-articleACS PublicationsRequest reuse permissionsArticle Views187Altmetric-Citations18LEARN 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
Actin-driven cell dynamics probed by Fourier transform light scattering (2010)

We applied the newly developed Fourier transform light scattering (FTLS) to study dynamic light scattering in single live cells, at a temporal scale of seconds to hours. The nanoscale cell fluctuations were measured with and without the active actin contribution. We found experimentally that the spatio-temporal signals rendered by FTLS reveal interesting cytoskeleton dynamics in glial cells (the predominant cell type in the nervous system). The active contribution of actin cytoskeleton was obtained by modulating its dynamic properties via Cytochalasin-D, a drug that inhibits actin polymerization/depolymerization.
Use of Electrochemistry in the Synthesis of Heterocyclic Structures (2017)

The preparation and transformation of heterocyclic structures have always been of great interest in organic chemistry. Electrochemical technique provides a versatile and powerful approach to the assembly of various heterocyclic structures. In this review, we examine the advance in relation to the electrochemical construction of heterocyclic compounds published since 2000 via intra- and intermolecular cyclization reactions.
Sleep staging classification based on HRV: Time-variant analysis (2009)

An algorithm to evaluate the sleep macrostructure based on heart rate fluctuations from ECG signal is presented. This algorithm is an attempt to evaluate the sleep quality out of sleep centers. The algorithm is made up by a) a time-variant autoregressive model used as feature extractor and b) a hidden Markov model used as classifier. Characteristics coming from the joint probability of HRV features were used to fed the HMM. 17 full polysomnography recordings from healthy subjects were used in the current analysis. When compared to Wake-NREM-REM given by experts, the automatic classifier achieved a total accuracy of 78.21+/-6.44% and a kappa index of 0.41+/-.1085 using two features and a total accuracy of 79.43+/-8.83% and kappa index of 0.42+/-.1493 using three features.
Effects of oral administration of L-arginine on renal function in patients with heart failure (2000)

Oral administration of L-arginine has beneficial effects on glomerular filtration rate, natriuresis, and plasma endothelin level in patients with chronic congestive heart failure.
A STUDY OF THE EFFICIENCY OF THE SECONDARY LEVEL SCHOOLS IN KERALA (2017)

Abstract

Students form the nucleus of every educational process. The entire gamut of educational process aims at maximising the structural discourses of a learner. Structural discourses are broadened when all the intervening factors in the learning process are properly intertwined. Educational management constitutes the decisive factor that moulds the structural base and the very beginning of educational process. In Kerala, educational management system has got a well-defined hierarchy. Each layer of the hierarchy has its own fixed goals and objectives. At the same time, educational management has, at present, changed meaning and implication with innovative ideas and practices. In view of the changed version of management strategies, the role and functions of management in the educational system should also be redefined but how far these changes have been reflected in the contemporary educational management practices in Kerala and how far the new trends have succeeded in new roles and functions of the management system is a question of great concern. The investigator tries to investigate the problems faced by the educational management in Kerala and hence the study. Survey method was adopted for the present study. The sample for the study constitutes twenty seven headmasters/headmistresses who come into the management of secondary school level. From the study it is found out that the educational administration in Kerala has yet to be democratized. 
Key words: 
Educational management, Secondary level, Administration, Head master/Head mistress.
Using Ethanol as an Energy Source (2004)

The Report by G. A. Deluga et al. describing a new method of producing hydrogen from ethanol is an important contribution toward practical methods of producing hydrogen for use in fuel cells (“Renewable hydrogen from ethanol by autothermal reforming,” 13 Feb., p. [993][1]). However, the Report
Downhole Emulsification: Viscosity Reduction Increases Production (1996)

Abstract The purpose of this paper is to present a further update on the use of surfactants to assist in the pumping of viscous crude oils in Western Canada. Typically, crude oils present downhole pumping problems due to the high natural viscosity of the oil, such as Alberta's heavy oils, or in lighter oils which may have formed viscous oil exterior emulsions in situ, during combustion or by the agitation of the rod string and downhole pump during production. Viscosity reductions using DownHole Emulsification (DHE*) technology are possible, with oil viscosities from 10,000 to 500,000 centipoise capable of being reduced to less than 200 centipoise by the formation of water continuous emulsions. Wells which have high fluid levels, rod fall problems, high hydraulic pressures, poor pump efficiencies or excessive pressure losses in gathering systems are good candidates. Solving these viscosity concerns can cause production to be significantly enhanced, with costs being minimal: in general, less than 50 cents per incremental barrel. Reduced power consumption, decreased mechanical loads, reduced flowline pressures, more constant daily production and the reduction of flushbys or well loading are other potential benefits. Background Many techniques have been used to assist the producer in the production and handling of heavy oil. The use of heat by downhole combustion, steam drive or cyclic steam (Huff n' Puff) come readily to mind. One of the more easily understood techniques is the addition of condensate or light hydrocarbon diluent to cut viscosity in the tubing or flowlines. This is used primarily to mitigate rod fall problems and the sanding of pump checks, and allows rod speed to be increased. With rotary equipment, the addition of diluent causes pump efficiencies to be improved, torque to decrease and pump speed to increase. Another method of producing crudes that has the same effect as the use of diluent, is to make a water continuous emulsion of the oil in the wellbore by means of adding surfactants. It is likely that diluent will be required in the final processing of the oil, at the treaters and for gravity control in order to meet pipeline specifications. However, one has more economical control of the amount of diluent required at these sites, than by trying to alter the viscosity of the wet sandy crude in the wellbore. Figure 1 shows the viscosity of the crude oil and that of the emulsions formed (depending on the oil/water ratio) over a reasonable temperature range. This graph is for oil from the Clearwater formation, but other oils such as the Cummings exhibit similar responses. When emulsions are formed having water as the exterior phase, the viscosity of the final emulsion is almost independent of the original oil viscosity. Noticeably, the emulsion viscosity is only about 1% of the original oil viscosity at the bottomhole temperatures of these shallow wells (22 °C). It is evident that the use of surfactant and water can accomplish significant reductions in well bore viscosity. Nevertheless, as Figure 2 shows, not every heavy oil well is a good candidate.
RAFT polymerization: an avenue to functional polymeric micelles for drug delivery (2008)

RAFT (Reversible addition fragmentation chain transfer) polymerization is demonstrated as a versatile tool to obtain functional and crosslinked micelles for drug delivery purposes.
Microprocessor Bit Synchronizer for Shuttle Payload Communications (1978)

An example of the growing influence of the microprocessor in communications is illustrated in this description of the payload bit synchronizer and other related payload signal processing functions for the Space Shuttle. Stored in firmware the microprogrammed control at 2.56 M-instructions/s accomplishes bit synchronization, matched filter detection, NRZ- <tex xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">L</tex> conversion and frame synchronization for some thirty combinations of PCM formats and data rates.
A role for CKII phosphorylation of the Cactus PEST domain in dorsoventral patterning of the <i>Drosophila</i> embryo (1997)

Regulated proteolysis of Cactus, the cytoplasmic inhibitor of the Rel-related transcription factor Dorsal, is an essential step in patterning of the Drosophila embryo. Signal-induced Cactus degradation frees Dorsal for nuclear translocation on the ventral and lateral sides of the embryo, establishing zones of gene expression along the dorsoventral axis. Cactus stability is regulated by amino-terminal serine residues necessary for signal responsiveness, as well as by a carboxy-terminal PEST domain. We have identified Drosophila casein kinase II (CKII) as a Cactus kinase and shown that CKII specifically phosphorylates a set of serine residues within the Cactus PEST domain. These serines are phosphorylated in vivo and are required for wild-type Cactus activity. Conversion of these serines to alanine or glutamic acid residues differentially affects the levels and activity of Cactus in embryos, but does not inhibit the binding of Cactus to Dorsal. Taken together, these data indicate that wild-type axis formation requires CKII-catalyzed phosphorylation of the Cactus PEST domain.
p53-dependent DNA repair and apoptosis respond differently to high- and low-dose ultraviolet radiation. (1998)

p53 plays an essential part in the maintenance of the cellular genetic stability after a DNA-damaging event such as ultraviolet (UV) radiation. Following UV radiation, the amount of p53 protein is elevated. The increased p53 is believed to induce cell cycle arrest, promote nucleotide excision repair (NER) and apoptosis. To study if cells respond differently to high- and low-dose UV radiation, we examined the DNA repair efficiency and apoptosis rate of human and murine fibroblasts after UV radiation. Using a host cell reactivation assay, we found that NER was increased after low doses but not after high doses of UV radiation. In contrast, apoptosis occurred only after the cells received high doses (over 200 J/m2), but not low doses of UVB. The induction of both NER and apoptosis was observed only in p53+/+ murine fibroblasts, not in p53-/- cells, indicating that both stress response mechanisms are dependent on wild-type p53 function. UV radiation induced the expression of p53 protein in a dose-dependent manner up to 400 J/m2. In contrast, p21waf1/cip1 was induced only after low doses and bax only after high doses of UV radiation, supporting the roles of p21waf1/cip1 and bax in NER and apoptosis, respectively. Taken together, these results indicate that cellular stress response to UV radiation depends on UV dose, DNA repair after low doses and apoptosis after high doses, and that both mechanisms are dependent on wild-type p53 function.
Contributions of natural and anthropogenic sources to atmospheric methane variations over western Siberia estimated from its carbon and hydrogen isotopes (2012)

Aircraft measurements of carbon and hydrogen isotopic ratios of atmospheric CH 4 ( δ 13 CH 4 and δ D‐CH 4 ), with the respective precisions of 0.08‰ and 2.2‰, as well as CH 4 concentration were made at 1 and 2 km altitudes over western Siberia during 2006–2009. δ 13 CH 4 and δ D‐CH 4 were almost always lower at lower altitudes, while the CH 4 concentration was higher, implying strong sources on the ground with low isotopic values. δ 13 CH 4 showed a clear seasonal minimum in the late summer, while seasonality of CH 4 and δ D‐CH 4 was ambiguous due to the local disturbances. By inspecting the relationships between the CH 4 concentration and isotopes, we found that isotopic source signatures in the winter (December–April) are −41.2 ± 1.8 and −187 ± 18‰ for δ 13 CH 4 and δ D‐CH 4 , respectively, and the corresponding values in the summer (June–October) are −65.0 ± 2.5 and −282 ± 25‰. These values indicate predominant CH 4 emissions from fossil fuel facilities in the winter and wetlands in the summer. It was also found that the shorter‐term CH 4 variations are more influenced by fossil CH 4 than that from wetlands. The finding presumably reflects the fact that the former is released from limited areas such as leakage from fossil fuel facilities, while the latter is released from a vast expanse of wetland. By employing a CH 4 emission data set used in an atmospheric chemistry transport model, we calculated seasonal isotopic changes of CH 4 sources in western Siberia and compared them to the estimates obtained in this study. The results indicated that the seasonal change in the CH 4 emission data set is reasonable, at least in terms of a ratio of fossil to biogenic emissions.
Comparison of methods for in vitro testing of susceptibility of porcine Mycoplasma species to antimicrobial agents (1991)

The MICs of 18 antimicrobial agents used against strains of three porcine Mycoplasma species were determined by a serial broth dilution method. Twenty field strains of M. hyorhinis, ten field strains of M. hyopneumoniae, six field strains of M. flocculare, and the type strains of these species were tested. Twelve field strains and the type strain of M. hyorhinis were also tested by an agar dilution method. Tests were read at various time points. When the broth dilution method was used, the final MIC had to be read 2 days after color changes had stopped. MICs of tetracycline, oxytetracycline, doxycycline, and minocycline were low for the three Mycoplasma species tested. MICs of chlortetracycline were 8 to 16 times higher than MICs of the other tetracyclines. Spiramycin, tylosin, kitasamycin, spectinomycin, tiamulin, lincomycin, and clindamycin were effective against all strains of M. hyorhinis and M. hyopneumoniae. The quinolones were highly effective against M. hyopneumoniae but less effective against M. hyorhinis. The susceptibility patterns for M. hyopneumoniae and M. flocculare were similar.
Transcriptional Signatures of Ral GTPase Are Associated with Aggressive Clinicopathologic Characteristics in Human Cancer (2012)

RalA and RalB are small GTPases that support malignant development and progression in experimental models of bladder, prostate, and squamous cancer. However, demonstration of their clinical relevance in human tumors remains lacking. Here, we developed tools to evaluate Ral protein expression, activation, and transcriptional output and evaluated their association with clinicopathologic parameters in common human tumor types. To evaluate the relevance of Ral activation and transcriptional output, we correlated RalA and RalB activation with the mutational status of key human bladder cancer genes. We also identified and evaluated a transcriptional signature of genes that correlates with depletion of RalA and RalB in vivo. The Ral transcriptional signature score, but not protein expression as evaluated by immunohistochemistry, predicted disease stage, progression to muscle invasion, and survival in human bladder cancers and metastatic and stem cell phenotypes in bladder cancer models. In prostate cancer, the Ral transcriptional signature score was associated with seminal vesicle invasion, androgen-independent progression, and reduced survival. In squamous cell carcinoma, this score was decreased in cancer tissues compared with normal mucosa, validating the experimental findings that Ral acts as a tumor suppressor in this tumor type. Together, our findings show the clinical relevance of Ral in human cancer and provide a rationale for the development of Ral-directed therapies.
Bridged azapolycyclic alcohols from intramolecular epoxide ring openings by amides (1973)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTBridged azapolycyclic alcohols from intramolecular epoxide ring openings by amidesR. J. Schultz, W. H. Staas, and L. A. SpurlockCite this: J. Org. Chem. 1973, 38, 18, 3091–3093Publication Date (Print):September 1, 1973Publication History Published online1 May 2002Published inissue 1 September 1973https://pubs.acs.org/doi/10.1021/jo00958a004https://doi.org/10.1021/jo00958a004research-articleACS PublicationsRequest reuse permissionsArticle Views455Altmetric-Citations10LEARN 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
Synthesizing wide-angle and arbitrary view-point images from a circular camera array (2006)

We propose a technique of Imaged-Based Rendering(IBR) using a circular camera array. By the result of having recorded the scene as surrounding the surroundings, we can synthesize a more dynamic arbitrary viewpoint images and a wide angle images like a panorama . This method is based on Ray- Space, one of the image-based rendering, like Light Field. Ray-Space is described by the position (x, y) and a direction (θ, φ) of the ray's parameter which passes a reference plane. All over this space, when the camera has been arranged circularly, the orbit of the point equivalent to an Epipor Plane Image(EPI) at the time of straight line arrangement draws a sin curve. Although described in a very clear form, in case a rendering is performed, pixel of which position of which camera being used and the work for which it asks become complicated. Therefore, the position (u, v) of the position (s, t) pixel of a camera like Light Filed redescribes space expression. It makes the position of a camera a polar-coordinates system (r, theta), and is making it close to description of Ray-Space. Thereby, although the orbit of a point serves as a complicated periodic function of periodic 2pi, the handling of a rendering becomes easy. From such space, the same as straight line arrangement, arbitrary viewpoint picture synthesizing is performed only due to a geometric relationship between cameras. Moreover, taking advantage of the characteristic of concentrating on one circular point, we propose the technique of generating a wide-angle picture like a panorama. When synthesizing a viewpoint, since it is overlapped and is recording the ray of all the directions of the same position, this becomes possible. Having stated until now is the case where it is a time of the camera fully having been arranged and a plenoptic sampling being filled. The discrete thing which does not fill a sampling is described from here. When arranging a camera in a straight line and compounding a picture, in spite of assuming the pinhole camera model, an effect like a focus shows up. This is an effect peculiar to Light Field when a sampling is not fully performed, and is called a synthetic aperture. We have compounded all focal images by processing called an "Adaptive Filter" to such a phenomenon. An adaptive filter is the method of making the parallax difference map of perfect viewpoint dependence centering on a viewpoint to make. This is a phenomenon produced even when it has arranged circularly. Then, in circular camera arrangement, this adaptive filter is extended, and all focal pictures are compounded. Although there is a problem that an epipor line is not parallel etc. when it has arranged circularly, extension obtains enough, it comes only out of geometric information, and a certain thing is clarified By taking such a method, it succeeded in performing a wide angle and arbitrary viewpoint image synthesis also from discrete space also from the fully sampled space.
The effect of pioglitazone on weight, lipid profile and liver enzymes in type 2 diabetic patients (2015)

Although pioglitazone causes a significant decrease in FBS, HbA1C and triglyceride levels, it is associated with weight gain, which would limit its utility. IRCT registration code: IRCT201209276712N2.