gebhart/patrepeval huggingface dataset:
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1-antihistamines (1989)

A series of novel benzo- and pyrido-1,4-oxazepinones and -thiones which represents a new structural class of compounds possessing H1 antihistaminic activity was synthesized, and the SARs were evaluated. The antihistaminic activity was determined by blockade of histamine-induced lethality in guinea pigs. The sedative potential was determined by comparison of the EEG profiles of the compounds with those of known sedating and nonsedating antihistamines. Several of the compounds were shown to possess potent H1 antihistaminic activity and to be free of the cortical slowing with synchronized waves and spindling activity found in the EEG of sedative antihistamines. One compound, 2-[2-(dimethylamino)ethyl]-3,4-dihydro-4-methylpyrido[3,2-f]-1,4- oxazepine-5(2H)-thione (rocastine) is currently undergoing clinical evaluation as a nonsedating H1 antihistamine.
The Development of a Quantitative Music Skills Test for Patients with Alzheimer's Disease (1994)

A quantitative music therepy test, the Residual Music Skills Test (RMST), was developed for measuring music behaviors of persons with probable Alzheimer's disease. The instrument was piloted with eight subjects at Vanderbilt University and the Miami VA Medical Center. It was subsequently field tested with 37 subjects in two day treatment programs in Atlanta, Georgia. Results indicated that RMST items which incorporated singing produced the highest item discrimination indices. Coefficient alpha reliability on the RMST was less satisfactory. Scores on the RMST were also correlated with scores from Folstein's Mini Mental State Examination (MMSE, 1975). Interrater reliability was high for both tests. Language subscores of the RMST and the MMSE were also highly correlated. Correlations between total scores of the RMST and the MMSE produced an r of.61, suggesting that the RMST may be measuring unique cognitive functions as compared to the MMSE.
cAMP-Dependent PKA Negatively Regulates Polyadenylation of c-<i>mos</i>mRNA in Rat Oocytes (2002)

Activation of members of the MAPK family, Erk 1 and 2, in oocytes resuming meiosis is regulated by Mos. The cAMP-dependent PKA-mediated cAMP action that inhibits the resumption of meiosis also prevents MAPK activation. We hypothesized that PKA interferes with the MAPK signaling pathways at the level of Mos. We also assumed that this regulatory cascade may involve p34cdc2. To test our hypothesis we explored the role of PKA and p34cdc2 in regulating Mos expression. Rat oocytes that resume meiosis spontaneously served as our experimental model. We found that meiotically arrested rat oocytes express the c-mos mRNA with no detectable Mos protein. The presence of Mos was initially demonstrated at 6 h after meiosis reinitiation and was associated with its mRNA polyadenylation. (Bu)(2)cAMP inhibited Mos expression as well as c-mos mRNA polyadenylation. Both these cAMP actions were reversed by the highly selective inhibitor of the catalytic subunit of PKA, 4-cyano-3-methylisoquinoline. Polyadenylation of c-mos mRNA was also prevented by roscovitine, which is a potent inhibitor of p34cdc2. Ablation of MAPK activity by two specific MAPK signaling pathway inhibitors, either PD 98059 or U0126, did not interfere with Mos accumulation. Our results suggest that translation of Mos in rat oocytes is negatively regulated by a PKA-mediated cAMP action that inhibits c-mos mRNA polyadenylation and involves suppressed activity of p34cdc2. We also demonstrate that stimulation of Mos synthesis in the rat does not require an active MAPK.
Photoaddition of Ru(tap)<sub>2</sub>(bpy)<sup>2+</sup>to DNA:  A New Mode of Covalent Attachment of Metal Complexes to Duplex DNA (1997)

Near-UV or visible light irradiation of Ru(tap)2(bpy)2+ (1) (tap = 1,4,5,8-tetraazaphenanthrene; bpy = 2,2‘-bipyridyl) in the presence of duplex DNA induces the formation of covalent adducts with guanine. The adduct has been isolated from the photomodified DNA as both its nucleotide and nucleobase derivatives by using a combination of enzymatic and acid hydrolytic procedures in conjunction with HPLC. Characterization by electrospray mass spectrometry and NMR spectroscopy shows that two isomeric covalent adducts are formed in which the exocyclic amino group of a guanine nucleobase is linked to the C2 or C7 position of one of the tap ligands. It is proposed that the products are generated from the reduced ruthenium complex and the guanine radical cation resulting from photoinduced electron transfer between 1 and guanine.
Low-voltage-operation avalanche photodiode based on n-gallium oxide/p-crystalline selenium heterojunction (2014)

In this study, we demonstrate the avalanche multiplication phenomenon in a crystalline-selenium (c-Se)-based heterojunction photodiode. The carrier injection from an external electrode, which is considered to be the major factor contributing to dark current at a high electric field, was significantly decreased by employing a thin n-type Ga2O3 layer with a high hole-injection barrier. The fabricated Ga2O3/c-Se diode exhibited extremely high external quantum efficiency of over 100% in the short-wavelength region at a relatively low reverse-bias voltage of ∼20 V. Furthermore, Sn-doping of the Ga2O3 layer increases the carrier concentration; hence, the resulting device has a lower threshold voltage for avalanche multiplication.
A Systems Biology Approach to Investigate Human Lung Cell Response to Air Pollutants (2019)

Exposure to air pollution is associated with many serious diseases, such as asthma, chronic bronchitis, decreased lung function, cardiovascular disease, and lung cancer. Consequently, air pollution is currently contributing to significant increases in morbidity and mortality worldwide. Despite these adverse health effects, the cellular mechanisms underlying air pollutant-induced disease remain largely unknown. In this study we set out to investigate the genome-wide responses of lung cells exposed to multiple air pollutant exposure conditions. We first employ a toxicogenomic approach to evaluate the response of human lung cells exposed to gaseous pollutant mixtures present in urban atmospheres. Specifically, genomic responses are evaluated by identifying transcripts and molecular networks modulated upon exposure to freshly emitted air pollutants. These responses are then compared to those modulated upon exposure to photochemically altered pollutant mixtures, containing secondary pollutants. The results demonstrate that secondary pollutant mixtures produced from primary pollutants reacting under sunlight initiate a robust genomic response in lung cells, far greater than primary pollutants After identifying this trend, we focus a more detailed analysis on potential mechanisms underlying lung cell response to individual secondary pollutants. Here, we evaluate global microRNA expression modifications within lung cells exposed to formaldehyde, a secondary pollutant found in both indoor and outdoor air pollution. Our analysis reveals that formaldehyde induces significant changes in microRNA levels, which may in turn, regulate genes associated with inflammation and cancer. Together, these investigations reveal novel mechanisms potentially underlying air pollutant-induced disease.
IF-Matching: Towards Accurate Map-Matching with Information Fusion (2017)

With the advance of various location-acquisition technologies, a myriad of GPS trajectories can be collected every day. However, the raw coordinate data captured by sensors often cannot reflect real positions due to many physical constraints and some rules of law. How to accurately match GPS trajectories to roads on a digital map is an important issue. Many existing methods still cannot meet stringent performance requirements, especially for low/unstable sampling rate and noisy/lost data. As in practice, some other measurements such as speed and moving direction are collected together with the spatial locations acquired, we can make use of not only location coordinates but all data collected. In this paper, we propose a novel model using the related meta-information to describe a moving object, and present an algorithm called IF-Matching for map-matching. It can handle many ambiguous cases which cannot be correctly matched by existing methods. We run our algorithm with taxi trajectory data on a city-wide road network. Compared with two state-of-the-art algorithms of ST-Matching and the winner of GIS Cup 2012, our approach achieves more accurate results.
Recent advances in the production of graded-index fibers using phase-separable glasses (1979)

Previous work in the area of molecular-stuffed preforms1 indicated the possibility of producing step-index fibers with low loss, high numerical aperture, low dispersion, and low cost. We discuss the process through which preforms (capable of producing up to 10 km of fiber) are produced in batch quantities. The results given indicate the areas where future work will be concentrated in order to manufacture preforms capable of competing with the attenuation and bandwidth of fiber produced from CVD processes.
Cultural capital and young people's career progression - Part 1: Daniel Johnson and Tamsin Roorke (2022)

Not available
262. The identification of amino-acids by means of 3 : 5-dinitrobenzoyl chloride. Part II (1938)

B. C. Saunders, J. Chem. Soc., 1938, 1397 DOI: 10.1039/JR9380001397
Intestinal Absorption of Glycine and Glycyl-L-Proline in the Rat (1977)

1. Absorption of [3H]glycine and [14C]-glycyl-l-proline at concentrations between 0·5 and 4 mmol/l was studied by perfusion in vivo of rat jejunal and ileal segments. Absorption was defined as net removal of radioisotope from the perfusate. Radioactivity assays and amino acid analyses were performed on perfusates and on mucosal tissue samples obtained from the perfused segments. 2. At the concentrations studied, absorption rates of glycine and glycylproline were proportional to concentration. Ileal rates were approximately 60% of jejunal rates. Glycylproline absorption was slightly faster than glycine absorption and was associated with the appearance in the perfusate of free glycine and proline in the ratio approximately 3:1. Intraluminal hydrolysis was insufficient to account for the amounts of free amino acids found and glycylproline hydrolase activity at the brush border is known to be minimal. 3. Glycylproline absorption apparently occurred by transport of the intact peptide followed by its intracellular hydrolysis. However, more than one-third of absorbed glycine and one-eighth of absorbed proline returned to the lumen as free amino acid. This reflux of glycine and proline was not proportional to their concentrations in the mucosa.
A Pneumatic Orthotic Cranial Molding Helmet for Correcting Positional Plagiocephaly (2006)

The objective of this study was o determine the efficacy of a newly developed pneumatic orthotic cranial molding helmet for correcting positional plagiocephaly. The design was retrospective and the setting was a tertiary care center. Subjects were all patients in whom positional plagiocephaly has been diagnosed and who have been fitted by the Orthotics and Prosthetics Department for the helmet. Diagonal cranial lengths and widths were measured at each visit. Analysis included the calculation of the ratio change in oblique diameters compared with time, patient's age, and head circumference. Seventy-five patients met inclusion criteria (50 boys, 25 girls). Patients with pneumatic orthotic cranial molding helmet therapy had significantly improved outcomes as compared with pretreatment measurements (P < or = 0.0001). The helmet did not limit cranial growth as evidenced by significant normalization of the oblique measurement ratio when compared with increasing cranial circumference and age (P = 0.0003, P < or = 0.0001, respectively). The pneumatic orthotic cranial molding helmet successfully corrects positional plagiocephaly and does not hinder cranial growth.
Insect Cytokine Paralytic Peptide (PP) Induces Cellular and Humoral Immune Responses in the Silkworm Bombyx mori (2010)

In the blood (hemolymph) of the silkworm Bombyx mori, the insect cytokine paralytic peptide (PP) is converted from an inactive precursor to an active form in response to the cell wall components of microorganisms and contributes to silkworm resistance to infection. To investigate the molecular mechanism underlying the up-regulation of host resistance induced by PP, we performed an oligonucleotide microarray analysis on RNA of blood cells (hemocytes) and fat body tissues of silkworm larvae injected with active PP. Expression levels of a large number of immune-related genes increased rapidly within 3 h after injecting active PP, including phagocytosis-related genes such as tetraspanin E, actin A1, and ced-6 in hemocytes, and antimicrobial peptide genes cecropin A and moricin in the fat body. Active PP promoted in vitro and in vivo phagocytosis of Staphyloccocus aureus by the hemocytes. Moreover, active PP induced in vivo phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK) in the fat body. Pretreatment of silkworm larvae with ML3403, a pharmacologic p38 MAPK inhibitor, suppressed the PP-dependent induction of cecropin A and moricin genes in the fat body. Injection of active PP delayed the killing of silkworm larvae by S. aureus, whereas its effect was abolished by preinjection of the p38 MAPK inhibitor, suggesting that p38 MAPK activation is required for PP-dependent defensive responses. These findings suggest that PP acts on multiple tissues in silkworm larvae and acutely activates cellular and humoral immune responses, leading to host protection against infection.
Molecular polarizabilities and induced dipole moments in molecular mechanics (2000)

Molecular polarizabilities may be divided into either atomic contributions or bond contributions. The common way to estimate molecular polarizabilities is to assign atomic or bond parameters for each atom or bond type to fit experimental or quantum mechanical results. In this study we have taken a different approach. A general formula based on MM3 force constants and bond lengths was used to compute bond polarizabilities and molecular polarizabilities. New parameters for polarizabilities are not required. A fair agreement between experimental and computed molecular polarizabilities was obtained, with a RMS deviation of 0.82 Å3 (11.7%) and signed average error of 0.01 Å3 for a broad selection of 57 molecules studied. Two methods, the many-body interaction and the pair-interaction approaches, have been used to study induced dipole moments using the bond polarizabilities estimated from the new formula. The pair-interaction approximation, which involves much less computation than the many-body interaction approach, gives a satisfactory representation of induced dipole interaction. © 2000 John Wiley & Sons, Inc. J Comput Chem 21: 813–825, 2000
Glycol Esters from Aldehydes (1946)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTGlycol Esters from AldehydesFrank J. Villani and F. F. NordCite this: J. Am. Chem. Soc. 1946, 68, 8, 1674–1675Publication Date (Print):August 1, 1946Publication History Published online1 May 2002Published inissue 1 August 1946https://pubs.acs.org/doi/10.1021/ja01212a519https://doi.org/10.1021/ja01212a519research-articleACS PublicationsRequest reuse permissionsArticle Views118Altmetric-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
Dopamine receptor modulation by a highly rigid spiro bicyclic peptidomimetic of Pro-Leu-Gly-NH2 (1993)

A peptidomimetic analogue of Pro-Leu-Gly-NH2 (PLG), compound 3, has been synthesized that contains a highly constrained spiro bicyclic type-II beta-turn mimic. Peptidomimetic 3 enhanced the binding of the dopamine receptor agonist ADTN to dopamine receptors by 40% at 10(-6) M. At this same concentration PLG enhanced the binding of ADTN by 26%. Like PLG, 3 exhibited a bell-shaped dose-response curve with the maximum effect occurring at a concentration of 10(-6) M. Because of the highly rigid nature of the spiro bicyclic type-II beta-turn constraint found in 3, these results lend strong support for the hypothesis that the biologically active conformation of PLG is a type-II beta-turn.
The Emerging Frontiers and Applications of High-Resolution 3D Printing (2017)

Over the past few decades, there has been an increasing interest in the fabrication of complex high-resolution three-dimensional (3D) architectures at micro/nanoscale. These architectures can be obtained through conventional microfabrication methods including photolithography, electron-beam lithography, femtosecond laser lithography, nanoimprint lithography, etc. However, the applications of these fabrication methods are limited by their high costs, the generation of various chemical wastes, and their insufficient ability to create high-aspect-ratio 3D structures. High-resolution 3D printing has recently emerged as a promising solution, as it is capable of building multifunctional 3D constructs with optimal properties. Here we present a review on the principles and the recent advances of high-resolution 3D printing techniques, including two-photon polymerization (TPP), projection microstereoLithography (PµSL), direct ink writing (DIW) and electrohydrodynamic printing (EHDP). We also highlight their typical applications in various fields such as metamaterials, energy storage, flexible electronics, microscale tissue engineering scaffolds and organ-on-chips. Finally, we discuss the challenge and perspective of these high-resolution 3D printing techniques in technical and application aspects. We believe that high-resolution 3D printing will eventually revolutionize the microfabrication processes of 3D architectures with high product quality and diversified materials. It will also find applications in a wide scope.
Proliferation-induced decline of primitive hematopoietic progenitor cell activity is coupled with an increase in apoptosis of ex vivo expanded CD34+ cells. (1998)

We examined the decline in hematopoietic potential observed when human CD34+ cells are cultured in vitro by evaluating the association between proliferation history and the fate of long-term hematopoietic culture-initiating cells (LTHC-ICs) as well as the onset of programmed cell death. The membrane dye PKH2 was used to track ex vivo expanded human CD34+ cells from bone marrow, cord blood, and mobilized peripheral blood, and to identify and isolate CD34+ cells that had divided once, twice, three, or four times or more, as well as cells that had remained cytokine nonresponsive and therefore failed to proliferate. These isolated groups of cells were assayed for their hematopoietic potential, cell cycle status, and percentage of apoptotic cells. A gradual decline in the content of LTHC-ICs, as well as in their ability to initiate and sustain in vitro hematopoiesis, was found to correlate with the number of in vitro cellular divisions, such that the hematopoietic potential of CD34+ cells dividing four or more times was nearly depleted. DNA analysis revealed that cells dividing more than three times resided predominantly in G0/G1 phases of the cell cycle. In addition, the percentage of CD34+ cells undergoing apoptosis was found to increase concomitantly with the number of in vitro cellular divisions; less than 10% of cells dividing once were apoptotic, whereas more than 25% of CD34+ cells dividing four or more times underwent programmed cell death. Together, these data suggest that a proliferation-associated, and possibly activation-induced, loss of hematopoietic potential among dividing CD34+ cells may result from an increase in programmed cell death among dividing primitive hematopoietic progenitor cells.
EMWF for Flexible Automation and Assistive Devices (2009)

This paper describes an embedded workflow framework (EMWF) that enables flexible personal and home automation and assistive devices and service and social robots (collectively referred to as SISARL) to be built on workflow architecture The process definition language supported by EMWF is called SISARL-XPDL. It consists of a subset of the WfMC standard XML Process Definition Language (XPDL) 2.0, together with elements that implement common mechanisms for robot behavior coordination. SISARL-XPDL definitions of workflows are first translated into standard XPDL and execution directives and then are parsed either directly into binary workflow scripts for execution or into intermediate scripts in C. EMWF provides workflow engines for Linux and Windows CE platforms. The engines are written in C in order to keep their memory footprint and runtime overhead small. Performance data show that the overheads introduced by the engine and workflow data are tolerable for most SISARL devices.
Crystal structure of the inclusion complex of cholesterol in β-cyclodextrin and molecular dynamics studies (2018)

The role of beta-cyclodextrin (β-CD) in cholesterol removal primarily from mammalian cells and secondly from dairy products has been studied thoroughly in recent years. Although the physicochemical characterization of the inclusion compound of cholesterol in β-CD has been achieved by various methods, no crystal structure has been determined so far. We report here the crystal structure of the inclusion compound of cholesterol in β-CD. The inclusion complex crystallizes in the triclinic space group <i>P</i>1 forming head-to-head dimers which are stacked along the <i>c</i>-axis. One well-defined cholesterol molecule 'axially' encapsulated inside the β-CD dimer and 22 water molecules that stabilize the complexes in the crystalline state comprise the asymmetric unit of the structure. The dimers are arranged in an intermediate (IM) channel packing mode in the crystal. Moreover, MD simulations, at 300 and 340 K, based on the crystallographically determined coordinates of the complex show that the formed cholesterol/β-CD inclusion compound remains very stable in aqueous solution at both temperatures.
Crystal Forms of Semisynthetic Ergot Alkaloid Terguride (2002)

Two new structures of semisynthetic ergot alkaloid terguride created by unusual number of symmetry-independent molecules were determined by X-ray diffraction methods at 150 K. Form A (monoclinic, P2 1 2 1 2 1 , Z = 12) contains three symmetry-independent terguride molecules and two molecules of water in the asymmetric part of the unit cell. The form C A (monoclinic, P2 1 , Z = 8) is an anhydrate remarkable by the presence of four symmetry-independent molecules in the crystal structure. Conformations of twelve symmetry-independent molecules that were found in four already described terguride structures are compared with torsion angles obtained by ab initio quantum-mechanical calculations for the simplified model of N -cyclohexyl- N' -diethylurea.
Congenital Hypothyroidism Treatment in Infants: A Comparative Study between Liquid and Tablet Formulations of Levothyroxine (2013)

We confirmed the efficacy and safety of both formulations. The TSH inhibition trend when using liquid L-T4 may be linked to a higher absorption in comparison to the tablets.