gebhart/patrepeval huggingface dataset:
Improvement of Solubility and Oral Bioavailability of 2-(N-Cyanoimino)-5-{(E)-4-styrylbenzylidene}-4-oxothiazolidine (FPFS-410) with Antidiabetic and Lipid-Lowering Activities in Dogs by 2-Hydroxypropyl-.BETA.-cyclodextrin (2006)

2-(N-Cyanoimino)-5-[(E)-4-styrylbenzylidene]-4-oxothiazolidine (FPFS-410) is a newly synthesized thiazolidine derivative having not only antidiabetic but also lipid-lowering activities. However, this compound has an extremely low aqueous solubility (2.8 (+/-0.33) x 10(-8) M (0.0094+/-0.0011 microg/ml) in 1.0 M phosphate buffer (pH 7.0) at 25 degrees C). In this study, we investigated the effect of various hydrophilic cyclodextrins (CyDs) on the solubility of FPFS-410 to select a CyD suitable for formulations of the compound. Among various CyDs, 2-hydroxypropyl-beta-CyD (HP-beta-CyD) had the highest solubilizing ability to FPFS-410, e.g., the solubility of the compound was increased 200000-fold by the addition of 40 mM HP-beta-CyD, which was attributable to the formation of the 1 : 2 (guest : host) inclusion complexes. The interaction of HP-beta-CyD with FPFS-410 was studied using 1H-nuclear magnetic resonance (NMR) spectroscopies including ROESY spectroscopy and a molecular modeling calculation. These results suggested that HP-beta-CyD forms a 1:2 (guest : host) inclusion complex with FPFS-410 by including both the stilbene and thiazolidine moieties. FPFS-410/HP-beta-CyD solid complexes with various stoichiometries were prepared by the spray drying and cogrinding methods, and confirmed by powder X-ray diffractometry that these complexes are in an amorphous state. The dissolution of FPFS-410 in water was significantly accelerated by the complexation with HP-beta-CyD. In vivo studies revealed that HP-beta-CyD markedly increases the bioavailability of FPFS-410 after oral administration in dogs. The present results suggest that HP-beta-CyD is useful for improvement of the extremely low bioavailability of FPFS-410.
Stable Dianion Radicals and Trianions in Substituted Pentadienyl Systems (1964)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStable Dianion Radicals and Trianions in Substituted Pentadienyl SystemsNathan L. BauldCite this: J. Am. Chem. Soc. 1964, 86, 11, 2305–2306Publication Date (Print):June 1, 1964Publication History Published online1 May 2002Published inissue 1 June 1964https://pubs.acs.org/doi/10.1021/ja01065a054https://doi.org/10.1021/ja01065a054research-articleACS PublicationsRequest reuse permissionsArticle Views62Altmetric-Citations7LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
A pilot safety and immunogenicity study of the malaria vaccine SPf66 in Gambian infants (1995)

A pilot safety and immunogenicity trial of the malaria vaccine SPf66 has been undertaken in 150 Gambian infants. No significant systemic side effects were recorded but modest local reactions were seen after the administration of a third 1.0 mg dose. SPf66 produced in Colombia was more immunogenic than SPf66 produced in the USA and a 1.0 mg dose of each vaccine gave higher antibody levels than a 0.5 mg dose. However, antibody levels fell rapidly after administration of the third dose of vaccine and showed little change over the following malaria transmission season. The incidence of clinical malaria was higher among children who received SPf66 than among children who received inactivated polio vaccine, the effect being most marked among children who received 1.0 mg Colombian SPf66. As the trial was not designed to measure the effect of SPf66 on morbidity from malaria, the significance of this finding is uncertain.
Synthesis and in vitro anti‐human cytomegalovirus (hcmv) activity of certain alkenyl substituted cytosines and 5‐halocytosines (1995)

Abstract The 1‐[(Z)‐2‐penten‐1‐yl] and 1‐(3‐methyl‐2‐buten‐1‐yl) derivatives of cytosine, 5‐bromocytosine, 5‐fluorocytosine, and 5‐iodocytosine were prepared by a reaction of the sodium salt of the requisite cytosine with (Z)‐1‐bromo‐2‐pentene and 4‐bromo‐2‐methyl‐2‐butene, respectively. The eight alkenylcytosines 5a‐5h were evaluated in cell culture for their anti‐HCMV activity. Only the derivatives of 5‐bromocytosine, 5c and 5d , showed slight activity in this assay.
Progress towards a dual-isotope trapped mercury ion atomic clock: Further studies of background gas collision shifts (2012)

As part of an on-going effort to build a dual-isotope ion trap clock based on the <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">199</sup> Hg <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> and <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">201</sup> Hg <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> ground state hyperfine transitions, we continue to characterize the systematic sensitivities of the <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">201</sup> Hg <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> 29.9GHz clock transition. Here we present an extension to the previous <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">201</sup> Hg <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> collision shift measurement for helium[1] to other background gases. We also measured the collision shifts in the <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">199</sup> Hg <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> 40.5GHz clock transition in the same physical system. We find that frequency sensitivities to collisions with background gas for the two isotopes agree within a factor of two. We will also discuss planned collision shift measurements with co-trapped <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">199</sup> Hg <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> and <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">201</sup> Hg <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> , as an important step towards a dual-isotope atomic clock.
Personal noise exposure assessment from small firearms (2003)

The National Institute for Occupational Safety and Health conducted noise exposure evaluations of law-enforcement personnel during firearms training at indoor and outdoor firing ranges. A representative cross section of weapons used by officers was measured. Shooters participated in live-fire exercise at an indoor firing range using three different weapons: a Beretta .400 caliber pistol, a Remington 12-gauge shotgun, and an M4 .223-caliber assault rifle. Indoor and outdoor measurements were obtained for the Smith and Wesson .357 pistol and Colt .450 and 9-mm pistols, the Glock .400 pistol, and the Heckler and Koch and Colt AR15 .223 rifles. Impulses were measured using a Bruel and Kjaer 4136 1/4-in. microphone and TASCAM digital audio tape recorder. Relevant impulse noise metrics were calculated. Peak levels ranged from 155 to 168 dB SPL. A-weighted equivalent levels ranged from 124 to 128 dBA. The contributions of the secondary weapon firings were approximately 1 to 9 dBA. Other parameters such as A/B durations, number and mixture of impulses, spectral content, energy, kurtosis, temporal spacing, and hearing protectors’ effectiveness were examined. Comparisons of applicable damage risk criteria are presented. Further studies are needed to establish an occupational impulse noise damage risk criterion.
Selection of High Contrast Color Sets (1996)

We present an algorithm for the selection of high contrast color sets which performs very well and does not require that the function adopted to code the similarity between two colors is a distance function.
Distinct Cerebrospinal Fluid Proteomes Differentiate Post-Treatment Lyme Disease from Chronic Fatigue Syndrome (2011)

nPTLS and CFS have distinguishing CSF protein complements. Each condition has a number of CSF proteins that can be useful in providing candidates for future validation studies and insights on the respective mechanisms of pathogenesis. Distinguishing nPTLS and CFS permits more focused study of each condition, and can lead to novel diagnostics and therapeutic interventions.
Advances in the Understanding of the Gabaergic Neurobiology of FMR1 Expanded Alleles Leading to Targeted Treatments for Fragile X Spectrum Disorder (2015)

Fragile X spectrum disorder (FXSD) includes: fragile X syndrome (FXS), fragile X-associated tremor ataxia syndrome (FXTAS) and fragile X-associated primary ovarian insufficiency (FXPOI), as well as other medical, psychiatric and neurobehavioral problems associated with the premutation and gray zone alleles. FXS is the most common monogenetic cause of autism (ASD) and intellectual disability (ID). The understanding of the neurobiology of FXS has led to many targeted treatment trials in FXS. The first wave of phase II clinical trials in FXS were designed to target the mGluR5 pathway; however the results did not show significant efficacy and the trials were terminated. The advances in the understanding of the GABA system in FXS have shifted the focus of treatment trials to GABA agonists, and a new wave of promising clinical trials is under way. Ganaxolone and allopregnanolone (GABA agonists) have been studied in individuals with FXSD and are currently in phase II trials. Both allopregnanolone and ganaxolone may be efficacious in treatment of FXS and FXTAS, respectively. Allopregnanolone, ganaxolone, riluzole, gaboxadol, tiagabine, and vigabatrin are potential GABAergic treatments. The lessons learned from the initial trials have not only shifted the targeted system, but also have refined the design of clinical trials. The results of these new trials will likely impact further clinical trials for FXS and other genetic disorders associated with ASD.
Superficial Femoral Lymph Node Dissection After Positive Sentinel Lymphadenectomy for Early-Stage Melanoma of the Lower Extremity (2003)

The purpose of this study was to evaluate retrospectively the value of a subsequent superficial femoral lymph node dissection for patients with early melanoma of the lower extremity after a positive sentinel lymphadenectomy. During a 6-year period at the H. Lee Moffitt Cancer Center & Research Institute, 16 consecutive patients with clinical stage I or stage II melanoma of the lower extremity underwent subsequent superficial femoral lymph node dissections after positive sentinel lymphadenectomies and wide local excisions of the primary lesions. Fifteen patients (94%) were found to have no additional positive lymph nodes from their superficial femoral lymph node dissection specimens. In contrast, only 1 patient (6%) with a thick primary lesion (7.5 mm) was found to have one additional positive lymph node on a subsequent superficial femoral lymph node dissection. No patients developed any regional nodal recurrences during a mean follow-up of 31.1 months (range, 3-80 months). This preliminary report suggests that the majority of the time the sentinel lymph node may be the only site of regional microscopic nodal disease and that a subsequent superficial femoral lymph node dissection may not be necessary in patients with early melanoma of the lower extremity after a positive sentinel lymphadenectomy. However, whether the sentinel lymphadenectomy can be used solely as a regional surgical treatment for this subgroup of patients still warrants further evaluation.
Relationship between the positive temperature coefficient of resistivity and dynamic rheological behavior for carbon black‐filled high‐density polyethylene (2003)

Abstract Studies on the relationship between resistivity and dynamic rheological properties of carbon black‐filled high‐density polyethylene (CB/HDPE) composites were carried out. Change of resistivity ρ is associated with the dynamic modulus before the positive temperature coefficient/negative temperature coefficient (PTC/NTC) transition temperature. When the temperature approaches the melting point of HDPE, ρ increases rapidly with a decreasing modulus, corresponding to PTC transition. The resistivity‐dynamic viscoelasticity relationship in the PTC region can be divided into two parts in which the changes of ρ with storage modulus G ′ and loss modulus G ″ can be described by the scaling laws given by the critical storage modulus and loss modulus G ′ c and G ″ c ; adjustable parameters ρ′ 1c , ρ′ 2c , ρ″ 1c and ρ″ 2c ; and nonlinear exponents n and m , respectively. The accordance between the experimental data and the scaling functions of the dimensionless quantities ( G ′/ G ′ c − 1) and ( G ″/ G ″ c − 1) in the PTC transition region suggests that the ρ jump may be the result of a modulus‐induced percolation. G ′ c and G ″ c increase, but the four scaling resistivitis, ρ′ 1c , ρ′ 2c , ρ″ 1c , and ρ″ 2c , decrease with increasing CB concentration, implying that the microstructure change of the composites is the determinant factor for the PTC behavior and the resistivity‐dynamic modulus relationship. However, ρ′ 2c and ρ″ 2c exhibit no scaling dependence. It is suggested that a threshold concentration exists for the modulus of the composites on the basis of examining the plot of both G ′ c and G ″ c against CB concentration. The scaling laws G ′ ∼ Φ x and G ″ ∼ Φ y hold for the concentration dependence of the critical modulus when Φ &gt; Φ c and the estimated values of x and y are 1.10 ± 0.10 and 0.89 ± 0.29, respectively. The resistivity‐dynamic modulus can shift to form a master curve. The horizontal factors a G ′ and a G ″ and the vertical factors a ′ and a ″ are relevant to the concentration dependence of the dynamic modulus or PTC behavior. It is believed that the former would be involved in changing the mechanical microstructure formed by the complicated interaction of CB particle and polymer segments, and the latter would be involved in the overall changes of conducting a network during the PTC transition region. © 2003 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys 41: 983–992, 2003
Mapping of High-Quality Optical Flats without Reflection Coating* (1962)

Get PDF Email Share Share with Facebook Tweet This Post on reddit Share with LinkedIn Add to CiteULike Add to Mendeley Add to BibSonomy Get Citation Copy Citation Text F. L. Roesler, "Mapping of High-Quality Optical Flats without Reflection Coating*," J. Opt. Soc. Am. 52, 471-471 (1962) Export Citation BibTex Endnote (RIS) HTML Plain Text Citation alert Save article
New sources of β-cells for treating diabetes (2009)

The treatment of diabetes by islet transplantation is presently hampered by the shortage of organ donors. The generation of insulin-producing cells is therefore a major objective in the long-term goal of curing diabetes. Alternative sources of pancreatic beta-cells include existing pancreatic cells, embryonic stem cells, and cells from other tissues such as liver. This commentary considers evidence for two new sources of beta-cells: intrahepatic biliary epithelial cells and gall bladder epithelium. These observations raise the possibility that a patient's own cells may be used as a source of insulin-producing cells for cell replacement in diabetes.
Energy Planning in Bulgaria (2022)

The article examines the state and organization of the national energy planning in Bulgaria. It justifies the need for a scientific methodology and legal regulations for drawing up, certification, implementation, analyzing and renewing of a strategic plan for national energy development.
Audiences, Aesthetics and Affordances: Analysing Practices of Visual Communication on Social Media (2017)

This research investigates how the practices of sharing pictures with specific audiences on social media may be related to aesthetics and affordances. Based on fieldwork (interviews, picture analysis and digital ethnography) with a group of female teenagers in Vienna, Austria, how they visually curate their accounts is mapped and reconstructed. Regarding content and aesthetics, different kinds of pictures are shared using different apps. Snapchat, for example, (for this specific group at the time of the investigation) is the preferred medium for live communication with very close friends using fast, pixelated, “ugly” pictures, while Instagram serves to share polished, conventional, “beautiful” pictures with broader audiences. Based on this case study, three conceptual arguments can be made. First, visual communication is practised in relation to specific social settings or audiences. Social media is part of these practices, and users navigate differences between platforms to manage identities and relationships. Second, the analysis of practices embedded in specific software, therefore, has to be contextualised and related to the structures of these environments. Software co-constructs processes of editing, distribution, sharing and affirmation, and its affordances have to be related to the ways in which users exploit them. Third, as visual communication becomes an intrinsic part of online communication, the exploration of how distinctions between audiences and affordances play out stylistically appears to be of particular interest, which entails calibrated aesthetics; however, this visual layer is seldom investigated closely.
Situation normal [Gourand and Phong shading] (1997)

Two of the most famous graphics techniques, derived from shading algorithms by Henri Gouraud and Bui Tuong Phong, have been implemented in hardware and software worldwide. Both methods use various hacks to smooth out the shading of a polygonal surface. So rather than looking like an assembly of flat slabs, a smooth-shaded model seems smoother. The sharp creases between polygons are gone, replaced by a continuous change in tone or color. But if the original polygons aren't being rendered directly, then the shading doesn't correspond to the original model. What model does it correspond to? In other words, what is the smooth surface which, when rendered accurately, has the same appearance as a Phong shaded polygonal model? Phong normal interpolation is the process of computing a point's surface normal by linear interpolation of the components of two normals at either end of a line containing that point. This normal may then be used as part of a shading equation that takes into account specular highlights in an empirical manner, Phong illumination. Throughout this article, I deal only with perfectly diffuse surfaces lit by a single light source, so Phong illumination isn't part of the discussion. We assume that the light source is conveniently located at infinity. Gourand shading means the process of interpolating a color component to find intermediate color values across a polygon. Phong shading means interpolating surface normals to find intermediate normals that we can then evaluate with respect to the light source to find a color for that point.
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure (2017)

A novel class of therapeutic drug candidates for heart failure, highly potent and selective GRK2 inhibitors, exhibit potentiation of β-adrenergic signaling in vitro studies. Hydrazone derivative 5 and 1,2,4-triazole derivative 24a were identified as hit compounds by HTS. New scaffold generation and SAR studies of all parts resulted in a 4-methyl-1,2,4-triazole derivative with an N-benzylcarboxamide moiety with highly potent activity toward GRK2 and selectivity over other kinases. In terms of subtype selectivity, these compounds showed enough selectivity against GRK1, 5, 6, and 7 with almost equipotent inhibition to GRK3. Our medicinal chemistry efforts led to the discovery of 115h (GRK2 IC<sub>50</sub> = 18 nM), which was obtained the cocrystal structure with human GRK2 and an inhibitor of GRK2 that potentiates β-adrenergic receptor (βAR)-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol. Therefore, 115h appears to be a novel class of therapeutic for heart failure treatment.
Ballistic electron studies and modification of the Au/Si interface (1990)

The Au/Si(111) interface has been investigated with ballistic electron emission microscopy. The Schottky barrier (SB) height and ballistic transmittance have been measured on interfaces which have been prepared with different types of monolayer-level dopants. Transmission rates but not the SB are found to depend strongly on the resulting degree of interdiffusion of the Au and Si at the interface. An irreversible modification in the transport properties of the buried interface can occur when the system is stressed with electrons injected at several volts above the Schottky barrier.
CAD-Phone SAR Computational Inter-Laboratory Study IEEE TC34, SC2-WG2 1528.3 (2008)

The recent international inter-laboratory study conducted by IEEE TC34, SC2, WG2 to develop the IEEE 1528.3 standard for computational compliance assessment of cell phone exposure is presented. Thirteen laboratories participated in this project with the goal to model and evaluate exposure from CAD based cell phone models using the Specific Anthropomorphic Mannequin (SAM) and exposure configurations developed for IEEE Std 1528-2003. The main objective was to test the feasibility of the CAD based computational SAR evaluation using the CAD models of cell phones, and to determine the practicality of the protocol which specifies the steps and procedures to be included in the IEEE 1528.3 standard. The available results at time of conference will be presented and discussed.
The Overnight Drift in U.S. Equity Returns (2021)

Since the advent of electronic trading in the late 1990s, S&P 500 futures have traded close to 24 hours a day. In this post, which draws on our recent Staff Report, we document that holding U.S. equity futures overnight has earned a large positive return during the opening hours of European markets. The largest positive returns in the 1998–2019 sample have accrued between 2 a.m. and 3 a.m. U.S. Eastern time—the opening of European stock markets—and averaged 3.6 percent on an annualized basis, a phenomenon we call the overnight drift.
Single-mode fiber measurements (1983)

This paper will discuss the measurement of those optical performance properties that are unique to single-mode fibers; chromatic dispersion; cutoff wavelengths associated with the fundamental and higher-order modes; and mode diameter or spot size. I shall review the various techniques available for measuring these properties and emphasize those that are in widespread use in research and development laboratories.