gebhart/patrepeval huggingface dataset:
Replacement of the Benzylpiperidine Moiety with Fluorinated Phenylalkyl Side Chains for the Development of GluN2B Receptor Ligands (2018)

Abstract The 4‐benzylpiperidine moiety is a central structural element of potent N ‐methyl‐ d ‐aspartate (NMDA) receptor antagonists containing the GluN2B subunit. To obtain novel GluN2B ligands suitable for positron emission tomography, the benzylpiperidine moiety was replaced with fluorinated ω‐phenylalkylamino groups. For this purpose three primary propyl‐ and butylamines 7 a – c and one butyraldehyde 7 d bearing a fluorine atom and an ω‐phenyl moiety were prepared in 3‐ to 7‐step syntheses. Compounds 7 a – d were attached to various scaffolds of potent GluN2B antagonists (scaffold hopping) instead of the original 4‐benzylpiperidine moiety. Although benzoxazol‐2‐ones and indoles with a benzylpiperidine moiety show high GluN2B affinity, the corresponding fluorophenylalkylamine derivatives did not result in high Glu2B affinity. Moderate GluN2B affinity was observed for a 3‐(fluoroalkyl)‐substituted tetrahydro‐1 H ‐3‐benzazepine ( K i =239 n m ). However, high GluN2B affinity was obtained for the tetrahydro‐5 H ‐benzo[7]annulen‐7‐amines 12 a – c ( K i =17–30 n m ). Docking studies resulted in the same binding pose for 12 a as for the lead compound Ro 25‐6981. It can be concluded that some GluN2B ligands (benzoxazolones, indoles) do not tolerate replacement of the 4‐benzylpiperidine moiety with flexible fluorinated phenylalkyl side chains, but other scaffolds such as tetrahydro‐3‐benzazepines and ‐benzo[7]annulenes retain interaction with NMDA receptors containing the GluN2B subunit.
Nafarelin vs. leuprolide acetate depot for endometriosis. Changes in bone mineral density and vasomotor symptoms. Nafarelin Study Group. (1997)

Nafarelin and LA depot were equally effective despite higher estradiol levels in nafarelin recipients. Nafarelin-treated subjects lost less BMD, had fewer days with hot flushes and had fewer objectively measured hot flushes.
Nutrient digestibility, rumen parameters, and (cannabinoid) residues in sheep fed a pelleted diet containing green hemp (Cannabis sativa L.) biomass (2022)

The feeding value for ruminants of green hemp biomass, from the low Δ<sup>9</sup>-tetrahydrocannabinol (Δ<sup>9</sup>-THC) variety of <i>Cannabis sativa</i> L., is unknown. Twelve Merino ewes were individually penned and randomly allocated on a stratified liveweight basis to one of two pelleted dietary treatments, control (0% hemp, <i>n</i> = 6) or hemp (42% green hemp biomass, <i>n</i> = 6) that delivered a diet meeting the nutrient requirements of the animals. The experimental period consisted of 17 d dietary and housing adaptation, followed by 7 d total urine and feces collection for determination of apparent nutrient digestibility. A ruminal fluid sample was collected on day 27 and assessed for pH, ammonia, volatile fatty acid (VFA), and cannabinoid concentrations. A blood sample from the jugular vein and incisional subcutaneous fat biopsy from an area around the base of the tail were collected on day 28 with additional fat biopsies taken 35 d and 140 d post-feeding to measure cannabinoids. The dry matter (DM), organic matter (OM), and crude protein (CP) digestibilities, along with total VFA concentration did not differ (<i>P</i> = 0.713) between the two diets; however, acid detergent fiber (ADF) and neutral detergent fiber (NDF) digestibilities (<i>P</i> < 0.001), water intake (<i>P</i> = 0.023), and fecal water output (<i>P</i> < 0.001) were significantly lower for the sheep-fed Hemp. Rumen pH did not vary (<i>P</i> = 0.256) between diets, but ruminal ammonia concentration was significantly lower (<i>P</i> = 0.024) for sheep consuming Hemp. Sheep-fed Hemp had significantly greater molar proportions of butyric (<i>P</i> = 0.039) and hexanoic (<i>P</i> = 0.012) acids and lower molar proportions of propionic acid (<i>P</i> = 0.003). There were no differences between diets for N intake (<i>P</i> = 0.175), fecal N output (<i>P</i> = 0.253), and N balance (<i>P</i> = 0.695), with all sheep in positive N balance; however, there was significantly lower (<i>P</i> = 0.001) urinary N output for sheep-fed Hemp. Cannabidiolic acid (CBDA) and tetrahydrocannabinolic acid (THCA) were detected in plasma of all sheep-fed Hemp. ∆<sup>9</sup>-tetrahydrocannabinol was present in the subcutaneous fat of four of the six sheep on the final day of being fed Hemp, and in all (six) sheep 35 d post-feeding and one sheep 140 d post-feeding Hemp. No cannabinoids were detected in the corresponding samples taken from the sheep-fed Control. Thus, despite green hemp biomass being nutritionally a suitable feed for ruminants, under current Food Standards in Australia, the presence of these cannabinoid residues restricts its use in ruminant diets.
SOFC Durability against Standby and Shutdown Cycling (2014)

To simulate realistic operating conditions in SOFC systems, we investigate the influence of thermal cycling on the performance of electrolyte-supported planar SOFCs. Thermal cycling is often associated with interruption of fuel supply, with three main modes; hot standby, cold standby, and shutdown. Cell performance degradation is most significant during shutdown cycles. Nickel oxidation and agglomeration are more pronounced when SOFCs are subjected to lower temperatures for longer periods of time, leading to significant performance degradation. Ostwald ripening at the anode leads to degradation as Ni grains increase in size with cycling. Ni particle precipitation on the anode zirconia grains and along electrolyte grain boundaries is found for the first time in shutdown cycling tests. When H2S is mixed with the fuel, the internal reforming reactions and electrode reactions are inhibited by sulfur poisoning of the Ni anodes, accelerating degradation. The SOFC cycling degradation mechanisms are discussed in detail.
Development of a Fit-for-Purpose Large-Scale Synthesis of an Oral PARP Inhibitor (2011)

Compound (1) a poly(ADP-ribose)polymerase (PARP) inhibitor has been made by a fit-for-purpose large-scale synthesis using either a classical resolution or chiral chromatographic separation. The development and relative merits of each route are discussed, along with operational improvements and extensive safety evaluations of potentially hazardous reactions.
Aminohaloborane in Organic Synthesis. VII.1A Directed Aldol Condensation Using Vinyloxyaminochloroborane (1979)

Abstract Vinyloxydichloroboranes (1) are scarcely found in literature2 probably because of certain unstable properties. We have found that some vinyloxyamino-chloroboranes (2), which can be prepared by formal substitution of one chlorine atom of 1 with a diethylamino group, are isolable stable compounds.
A quantitative study of cutaneous receptors and afferent fibres in the cat and rabbit (1967)

1. The discharge in myelinated afferent fibres innervating hairs in anaesthetized cats and rabbits, dissected from the saphenous nerve, was recorded during controlled movements of the hairs.2. Three types of rapidly adapting afferent unit were found and they innervated three kinds of hair follicle-down hair, guard hair and tylotrich.3. The down hair units had low thresholds (critical slopes) and some of the guard hairs had the highest thresholds and least sensitivity to displacement.4. There was a good fit to a power function for the relation between velocity of displacement of a hair and the frequency of discharge in the corresponding afferent fibre.5. It is concluded that the rapidly adapting hair follicle receptors can function as efficient exact movement detectors.6. Tylotrich follicles were often associated with touch corpuscles, but there was independent innervation of the rapidly adapting tylotrich follicle receptors and the slowly adapting touch corpuscle receptors.7. The conduction velocities of large populations of myelinated cutaneous axons innervating cutaneous mechanoreceptors were measured in cats and rabbits.
Nitric oxide, cGMP, and hormone regulation of active sodium transport. (1994)

The inter- and intracellular regulator nitric oxide (NO) has been suggested to play a role in the modulation of cellular excitability, but the mechanism(s) by which this occurs remain unclear. Using the kidney as a model system, we report here evidence that NO, produced in response to various hormones and cytokines, can effect long-term alterations in the activity of the membrane sodium pump. This regulation of Na, K-ATPase, which occurs in a system of NO-containing renal tubules, involves cGMP and cGMP-dependent protein kinase. Na, K-ATPase can also be regulated by alterations of cGMP initiated through NO-independent factors, such as atriopeptin, and in nonrenal tissues, such as cerebellum. Regulation of the membrane sodium pump by NO and cGMP, therefore, represents a mechanism for hormonal modulation of ion gradients, not only in kidney but also in other organs, including brain, where NO and cGMP play a prominent role in cellular function.
Names for Macromolecular Rotaxanes and Macromolecular Pseudorotaxanes (2016)

This document provides (i) definitions of terms related to macromolecular rotaxanes and macromolecular pseudorotaxanes and (ii) recommendations for naming these macromolecular assemblies. The nomenclature recommendations presented here have been developed by combining the nomenclature rules for the low-molar-mass (low-M) rotaxanes and those for macromolecules (both established in published IUPAC recommendations) in such a way that the developed nomenclature system provides unambiguous names for macromolecular rotaxanes (and pseudorotaxanes), including differentiation among various isomers of these supramolecular assemblies. Application of the nomenclature recommendations is illustrated using examples covering a wide range of structure types of macromolecular rotaxanes and pseudorotaxanes. An Alphabetical Index of Terms and a List of Abbreviations and Prefixes are included.
Defining Sub-Regions in Locally Sparsified Compressive Sensing MRI (2013)

Magnetic Resonance Imaging (MRI) is an important imaging technique. However, it is a time consuming process. The aim of this study is to make the imaging process ef?cient. MR images are sparse in the sensing domain and Compressive Sensing exploits this sparsity. Locally sparsi?ed Compressed Sensing is a specialized case of CS which sub-divides the image and sparsi?es each region separately; later samples are taken based on sparsity level in that region. In this paper, a new structured approach is presented for de?ning the size and locality of sub-regions in image. Experiments were done on the regions de?ned by proposed framework and local sparsity constraints were used to achieve high sparsity level and to reduce the sample set. Experimental results and their comparison with global CS is presented in the paper.
Ixazomib Improves Bone Remodeling and Counteracts Sonic Hedgehog Signaling Inhibition Mediated by Myeloma Cells (2020)

Multiple myeloma (MM) is a clonal B-cell malignancy characterized by an accumulation of plasma cells (PC) in the bone marrow (BM), leading to bone loss and BM failure. Osteolytic bone disease is a common manifestation observed in MM patients and represents the most severe cause of morbidity, leading to progressive skeletal damage and disabilities. Pathogenetic mechanisms of MM bone disease are closely linked to PCs and osteoclast (OCs) hyperactivity, coupled with defective osteoblasts (OBs) function that is unable to counteract bone resorption. The aim of the present study was to investigate the effects of Ixazomib, a third-generation proteasome inhibitor, on osteoclastogenesis and osteogenic differentiation. We found that Ixazomib was able to reduce differentiation of human monocytes into OCs and to inhibit the expression of OC markers when added to the OC medium. Concurrently, Ixazomib was able to stimulate osteogenic differentiation of human mesenchymal stromal cells (MSCs), increasing osteogenic markers, either alone or in combination with the osteogenic medium. Given the key role of Sonic Hedgehog (SHH) signaling in bone homeostasis, we further investigated Ixazomib-induced SHH pathway activation. This set of experiments showed that Ixazomib, but not Bortezomib, was able to bind the Smoothened (SMO) receptor leading to nuclear translocation of GLI1 in human MSCs. Moreover, we demonstrated that PCs act as GLI1 suppressors on MSCs, thus reducing the potential of MSCs to differentiate in OBs. In conclusion, our data demonstrated that Ixazomib regulates bone remodeling by decreasing osteoclastogenesis and prompting osteoblast differentiation via the canonical SHH signaling pathway activation, thus, representing a promising therapeutic option to improve the complex pathological condition of MM patients.
The North American tree‐ring fire‐scar network (2022)

Abstract Fire regimes in North American forests are diverse and modern fire records are often too short to capture important patterns, trends, feedbacks, and drivers of variability. Tree‐ring fire scars provide valuable perspectives on fire regimes, including centuries‐long records of fire year, season, frequency, severity, and size. Here, we introduce the newly compiled North American tree‐ring fire‐scar network (NAFSN), which contains 2562 sites, &gt;37,000 fire‐scarred trees, and covers large parts of North America. We investigate the NAFSN in terms of geography, sample depth, vegetation, topography, climate, and human land use. Fire scars are found in most ecoregions, from boreal forests in northern Alaska and Canada to subtropical forests in southern Florida and Mexico. The network includes 91 tree species, but is dominated by gymnosperms in the genus Pinus . Fire scars are found from sea level to &gt;4000‐m elevation and across a range of topographic settings that vary by ecoregion. Multiple regions are densely sampled (e.g., &gt;1000 fire‐scarred trees), enabling new spatial analyses such as reconstructions of area burned. To demonstrate the potential of the network, we compared the climate space of the NAFSN to those of modern fires and forests; the NAFSN spans a climate space largely representative of the forested areas in North America, with notable gaps in warmer tropical climates. Modern fires are burning in similar climate spaces as historical fires, but disproportionately in warmer regions compared to the historical record, possibly related to under‐sampling of warm subtropical forests or supporting observations of changing fire regimes. The historical influence of Indigenous and non‐Indigenous human land use on fire regimes varies in space and time. A 20th century fire deficit associated with human activities is evident in many regions, yet fire regimes characterized by frequent surface fires are still active in some areas (e.g., Mexico and the southeastern United States). These analyses provide a foundation and framework for future studies using the hundreds of thousands of annually‐ to sub‐annually‐resolved tree‐ring records of fire spanning centuries, which will further advance our understanding of the interactions among fire, climate, topography, vegetation, and humans across North America.
Mathematical Modeling and Calculation of the Methanol Production Process via Carbon Dioxide Hydrogenation (2020)

This work is devoted to the mathematical modeling and calculation of the hydrogenation reaction of carbon dioxide to produce methanol using kinetic models developed with taking into account different understandings of the reaction mechanism; in particular, the Graaf and Rozovskii–Lin mechanisms are considered. It has been shown that under flow conditions, both models designed for describing the reaction of methanol production from synthesis gas fairly accurately describe the CO2 hydrogenation reaction. Under recycle flow conditions, a more accurate description of the product yield with changes in pressure and temperature can be obtained using a model based on the Graaff mechanism.
Design methodology for accelerating software executions with FPGA (2010)

Reconfigurable logic is a flexible solution for offloading some of computations from a processor. In particular, in applications where small kernels are repeated often, e.g., in DSP. However, the traditional development style for reconfigurable logic is hardware design, while application code for CPU is software, thus there is need for an design methodology for converting software partition to an hardware structure. In this paper, we propose a design method, which can be used to create a FPGA configuration from a software code. The FPGA configuration can be executed in parallel with software execution. The application-specific hardware structures for the FPGA are generated automatically with the required interfaces and device drivers for data transfers.
The privacy challenges of in-depth video analytics (2012)

The increasing need for both automated and privacy-respecting CCTV systems adds many challenges to the tasks of Video Analytics. The growing capabilities of automated surveillance systems lead to the automatic extraction and processing of complex and potentially personal data related to individuals who may not even be aware of it. This paper discusses the issues related to the processing of potentially sensitive information extracted from various computer vision algorithms and techniques such as person tracking, soft biometrics, behaviour analysis or multi-modal person identification, and delivers insights regarding technical solutions and guidelines for achieving a higher level of privacy compliance.
Efficient full-chip yield analysis methodology for OPC-corrected VLSI designs (2002)

Degradation of lithographic pattern fidelity is a major cause of yield loss in VLSl manufacturing. A general methodology for full-chip analysis and improvement of yield loss due to lithographic effects is proposed The approach is based on: a) extraction of pattern fidelity statistics using a full-chip layout engine, b) full-chip optical proximity correction (OPC) to improve pattern reproduction, and c) estimation of yield losses due to line variability, using transistor sensitivity to pattern registration obtained from physical transistor modeling. As a result, yield estimates related to either pattern reproduction fidelity or transistor parametric data variations (such as leakage or drive current) are generated. The method is efficient and well suited for application to modern VLSI designs of memory or logic devices.
Skeletal muscle atrophy and short-term mortality in patients with acute exacerbation of idiopathic pulmonary fibrosis: An observational cohort study (2022)

Abstract Skeletal muscle atrophy often complicates idiopathic pulmonary fibrosis (IPF). IPF patients frequently experience acute exacerbation (AE), but the association between skeletal muscle atrophy and mortality remains unknown in AE-IPF patients. Herein, cross-sectional areas of the erector spinae muscle (ESM CSA ) and the pectoralis muscle (PM CSA ) of AE-IPF patients were analysed via computed tomography. Primary outcome was 90-day mortality. Survival probability was estimated using the Kaplan–Meier method, and the log-rank test was used between the low and high groups of ESM CSA and PM CSA . We used multivariable Cox proportional-hazards models to evaluate the association between ESM CSA and PM CSA and prognosis. Among the 212 patients, 94 (44%) died during the observation period. The low ESM CSA group (&lt; 25.6 cm 2 ) had a significantly worse prognosis than the high group (≥ 25.6 cm 2 ) (hazard ratio (HR) [95% confidence interval (CI)]: 1.52 [1.00–2.33], p = 0.049). Multivariable analyses showed that all-cause mortality was associated with low ESM CSA (model 1, adjusted HR [95% CI]: 1.59 [0.98–2.60]; model 2, 1.55 [0.95–2.56] and model 3, 1.67 [1.00–2.78]). A similar trend was observed between low PM CSA and poor prognosis (HR [95% CI]: 1.39 [0.88–2.20]). In conclusion, low ESM CSA is associated with high 90-day mortality in AE-IPF patients.
Pharmaceutical Applications of Biocatalysis (2004)

Enzyme Inhibition for the Fight against Disease Introduction Procedure for the Development of Pharmacologically Active Compounds Process for the Registration of New Drugs Chiral versus Non-chiral Drugs Enzyme Cascades and Biology of Diseases β-Lactam Antibiotics Inhibition of Cholesterol Biosynthesis (in part after Suckling, 1990) Pulmonary Emphysema, Osteoarthritis: Human Leucocyte Elastase (HLE) AIDS: Reverse Transcriptase and HIV Protease Inhibitors Pharmaceutical Applications of Biocatalysis Antiinfectives Anticholesterol Drugs Anti-AIDS Drugs High Blood Pressure Treatment Applications of Specific Biocatalytic Reactions in Pharma Reduction of Keto Compounds with Whole Cells Applications of Pen G Acylase in Pharma Applications of Lipases and Esterases in Pharma
Transmission network expansion planning consdering pumped-storage unit (2015)

This paper presents, the impact of the pumped-storage (PS) unit on the static transmission network expansion planning problem (STNEP). The aim of this work is to minimize the total cost which is a summation of the transmission line cost, the fuel cost and the load curtailment cost. The load curtailment cost is included in the objective function to avoid the additional artificial generation. The proposed problem is tested on the IEEE 24-bus system and the gbest-guided artificial bee colony (GABC) optimization algorithm is applied to this problem. Also, in order to analyze the load variations on the proposed STNEP problem three different load levels are considered.
Prototype Low Voltage Homopolar Traction Motor (2002)

&lt;div class="htmlview paragraph"&gt;Lower battery voltage enhances electric vehicle safety. A homopolar traction motor operates at low voltage because of its low internal impedance, and delivers torque independent of speed. A 48 VDC multi-pass, iron core homopolar traction motor was designed, fabricated, and tested in the laboratory. A MOSFET pulse width modulated controller was also designed and tested. The motor weighed 227 kg and used solid copper-graphite brushes. Laboratory testing of the motor verified the current-torque characteristic, but high brush wear prevented full speed and power demonstration. System studies show that a hybrid Ward-Leonard drive using a similar motor could yield significant cost and weight savings and improved fault tolerance over a traditional EV architecture.&lt;/div&gt;
Skin Tears: A Literature Review (2007)

Skin tears are reported to be a common occurrence in the elderly because of age related skin changes and associated disease processes. The depth of literature with regard to skin tears is indeed limited, yet skin tears may cause pain and suffering to the individual as well as monetary cost to the individual, hospital and community. In some cases, skin tears may become infected and require surgical intervention, or become chronic wounds and the occurrence of skin tears may present as an indicator of the quality of care in healthcare facilities. However, there is no consensus for the prevention and management of skin tears, and evidence based protocols are limited, with many of the existing protocols generated by dressing product manufacturers.This literature review was conducted to identify the scope and management of these wounds in relation to a hospital based investigation into skin tear occurrence. The review concludes that, to optimise outcomes, it becomes the responsibility of healthcare providers to educate, prevent, protect and treat individuals at risk of skin tears.