gebhart/patrepeval huggingface dataset:
[<sup>125</sup>I]Iodoproxyfan and Related Compounds:  A Reversible Radioligand and Novel Classes of Antagonists with High Affinity and Selectivity for the Histamine H<sub>3</sub>Receptor (1996)

The synthesis and biological evaluation of new histamine H3 receptor antagonists with an iodinated aryl partial structure are described as part of an extensive research program to find model compounds for the development of a new radioligand with high H3 receptor affinity and specific activity. All compounds were tested for their H3 receptor antagonist activity in a [3H]-histamine-release assay with synaptosomes from rat cerebral cortex. The new leads with potent H3 receptor antagonist activity belong to a series of derivatives of 3-(1H-imidazol-4-yl)propanol with carbamate (4-7), ester (8-16), and ether (17-22) as functional groups. Structure-activity relationships are discussed. The most active compound in the functional test (-log Ki = 8.3) and in binding studies with [3H]-(R)-alpha-methylhistamine on rat cerebral cortex (-log Ki = 9.0) in vitro was 3-(1H-imidazol-4-yl)propyl (4-iodophenyl)methyl ether (iodoproxyfan, 19) exhibiting no central H3 receptor antagonist activity in vivo. The potency of iodoproxyfan is more than 300 times lower at H1, H2, alpha1, alpha2, beta1, 5-HT2A, 5-HT3, and M3 receptors than at histamine H3 receptors. Because of the high potency and selectivity of 19, this compound has also been prepared in the [125I]-iodinated form by a nucleophilic halogen exchange reaction using the corresponding bromo derivative 22 as a precursor. The newly prepared [125I]iodoproxyfan (23) possesses advantageous pharmacological properties and fulfills all criteria of a useful radioligand.
42. Attempts to find new antimalarials. Part XXIII. Derivatives of 3 : 4 : 2′ : 3′-pyridoacridine and 1 : 2 : 2′ : 3′-pyridoacridine (1946)

J. Dobson and W. O. Kermack, J. Chem. Soc., 1946, 150 DOI: 10.1039/JR9460000150
Targeted disruption of<i>Slc2a8</i>(GLUT8) reduces motility and mitochondrial potential of spermatozoa (2008)

GLUT8 is a class 3 sugar transport facilitator which is predominantly expressed in testis and also detected in brain, heart, skeletal muscle, adipose tissue, adrenal gland, and liver. Since its physiological function in these tissues is unknown, we generated a Slc2a8 null mouse and characterized its phenotype. Slc2a8 knockout mice appeared healthy and exhibited normal growth, body weight development and glycemic control, indicating that GLUT8 does not play a significant role for maintenance of whole body glucose homeostasis. However, analysis of the offspring distribution of heterozygous mating indicated a lower number of Slc2a8 knockout offspring (30.5:47.3:22.1%, Slc2a8(+/+), Slc2a8(+/-), and Slc2a8(-/-) mice, respectively) resulting in a deviation (p=0.0024) from the expected Mendelian distribution. This difference was associated with lower ATP levels, a reduced mitochondrial membrane potential and a significant reduction of sperm motility of the Slc2a8 knockout in comparison to wild-type spermatozoa. In contrast, number and survival rate of spermatozoa were not altered. These data indicate that GLUT8 plays an important role in the energy metabolism of sperm cells.
Release of Guanylin Immunoreactivity from the Isolated Vascularly Perfused Rat Colon* (2000)

The intestinal peptide guanylin regulates the electrolyte/water transport in the intestinal epithelium. The aim of the present study was to investigate the mechanisms that modulate its secretion in the isolated vascularly perfused rat colon by using a specific guanylin RIA. Intraarterial infusion of bethanechol (10(-4) M) or bombesin (10(-7) M) elicited a significant 6-fold increase in the release of guanylin immunoreactivity (G-IR) in the lumen. Bombesin-stimulated G-IR secretion was strongly reduced by tetrodotoxin, whereas atropine had no effect. VIP (10(-7) M) induced a moderate release of G-IR, whereas substance P, calcitonin gene-related peptide, peptide YY, somatostatin, and neurotensin were without effect. Dimethyl-PGE2 (1.4 x 10(-5) M) or interleukin-1beta (2.5 x 10(-10) M) induced a 3-fold increase in G-IR in the lumen, whereas the degranulator compound bromolasalocid did not stimulate guanylin secretion. Forskolin (10(-5) M) or sodium nitroprusside (10(-4)-10(-3) M) induced a significant release of G-IR. In contrast, PMA (10(-7) M) or ionophore A23187 (10(-6) M) did not modify basal secretion of G-IR. Upon stimulation of guanylin release with bombesin or bethanechol, an increase in G-IR in the portal effluent was also detected. The release of G-IR in the portal effluent was 40-fold lower than that of G-IR into the luminal perfusate. Additionally, analysis with gel chromatography revealed that the immunoreactive material released in the lumen or in the portal effluent coeluted with the 15-amino acid peptide originally isolated from rat intestine. In conclusion, the present data suggest that the enteric nervous system and immune cells may modulate guanylin release from the rat colon. The release of guanylin in the lumen and portal effluent suggests that this peptide may exert both luminal/paracrine and hormonal effects.
Embodying self-compassion within virtual reality and its effects on patients with depression (2016)

© The Royal College of Psychiatrists 2016. This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY) licence.
Experimental resolution measurement in critical dimension scanning electron microscope metrology (2003)

By applying the basic principles of metrology we discuss how to define the standards that any experimental method to measure resolution has to obey. Our results clearly indicate the need to apply a calibration procedure when designing algorithms to estimate resolution to satisfy accuracy requirements. Similarly, the precision of an algorithm has to be clearly specified. We compare here the performances of a variety of commonly used implementations of published methods, with that of an algorithm based on an approach known to be reliable. Our results confirm that when an algorithm is designed with the clear intent of satisfying metrology requirements, it demonstrates excellent accuracy, precision, and lack of sensitivity to the noise level, as is desirable. As a consequence, the algorithm will have the ability to measure accurately the point spread function convoluted in the image, thus paving the way for quantitative deconvolution techniques.
TEACHING INTERCULTURAL SKILLS IN THE MULTICULTURAL CLASSROOM (2004)

This paper evaluates the adaptation of the ExcelL Intercultural Skills Program to an international human resource management course, and critically examines the effectiveness of integrating case study methods with the skills based ExcelL program. The ExcelL program is a theory-driven and evidence-based group program that utilises classroom cultural diversity, student experiences and role-plays to develop specific intercultural skills. The primary purpose of the study was to assess the usefulness of ExcelL within a sample of 85 third-year university business students. Four methodologies were used: (1) questionnaires, (2) case studies, (3) course evaluation survey and (4) focus groups. After completing the program, participants demonstrated improvements in intercultural competencies required in business contexts as well as increased self-confidence and feelings of self-efficacy in cross-cultural situations. Additionally, participants demonstrated improved identification and articulation of cross-cultural business problems and formulation of appropriate intervention strategies to address these problems.
Selecting a two-factor authentication system (2007)

Anyone introducing a secure authentication system beyond basic user name and password authentication faces a variety of choices. Failing to consider all the needs of the authentication system during the decision-making process can prove to be an expensive mistake. It is important to ensure that the system as a whole, not just the choice of technology, continues to meet the needs of the business and its users, both in the short and long term.
A Scalable Near-Memory Architecture for Training Deep Neural Networks on Large In-Memory Datasets (2019)

Most investigations into near-memory hardware accelerators for deep neural networks have primarily focused on inference, while the potential of accelerating training has received relatively little attention so far. Based on an in-depth analysis of the key computational patterns in state-of-the-art gradient-based training methods, we propose an efficient near-memory acceleration engine called NTX that can be used to train state-of-the-art deep convolutional neural networks at scale. Our main contributions are: (i) a loose coupling of RISC-V cores and NTX co-processors reducing offloading overhead by 7 x over previously published results; (ii) an optimized IEEE 754 compliant data path for fast high-precision convolutions and gradient propagation; (iii) evaluation of near-memory computing with NTX embedded into residual area on the Logic Base die of a Hybrid Memory Cube; and (iv) a scaling analysis to meshes of HMCs in a data center scenario. We demonstrate a 2.7 x energy efficiency improvement of NTX over contemporary GPUs at 4.4 x less silicon area, and a compute performance of 1.2 Tflop/s for training large state-of-the-art networks with full floating-point precision. At the data center scale, a mesh of NTX achieves above 95 percent parallel and energy efficiency, while providing 2.1 x energy savings or 3.1 x performance improvement over a GPU-based system.
Design of a programmable slew-rate op amp (1994)

This paper presents the design of a CMOS programmable slew rate operational amplifier. The amplifier proposed in this paper is capable of providing an additional programmable bias current which can be linearly controlled by an external 4 bit digital signal. The circuit designed for slew rate programmability is based upon a newly proposed concept, that is a switched parallel current subtraction circuit with an adaptive biasing technique. By utilizing the newly designed circuit, it was verified that the slew rate was linearly controlled and power dissipation was optimized. If the programmable slew rate amplifier is employed in a data converter, its data conversion time can be easily controlled.
Photonic band structure: the face-centered-cubic case (1990)

We employ the concepts of band theory to describe the behavior of electromagnetic waves in three-dimensionally periodic face-centered-cubic (fcc) dielectric structures. This can produce a “photonic band gap” in which optical modes, spontaneous emission, and zero point fluctuations are all absent. In the course of a broad experimental survey, we have found that most fcc dielectric structures have “semimetallic” band structure. Nevertheless, we have identified one particular dielectric “crystal” that actually has a “photonic band gap.” This dielectric structure consisting of 86% empty space, requires a refractive-index contrast of greater than 3:1, which happens to be readily obtainable in semiconductor materials.
Orthogonal Mirror Telescopes for X-ray Astronomy (1971)

Crossed mirror telescopes are presented as an alternative to the present telescope systems used in x-ray astronomy. These instruments generally have a higher x-ray collecting efficiency but a poorer angular resolution than the more conventional paraboloid-hyperboloid telescopes. They also can be made more easily and quickly as was demonstrated by a recent rocket flight that used a simplified mirror design with only one-dimensional focusing.
Topical Turmeric Microemulgel in the Management of Plaque Psoriasis; A Clinical Evaluation. (2015)

Psoriasis is an autoimmune and recurrent chronic inflammatory skin disease. About 1-3% of the world wide populations are affected. The characteristic features are hyperprolifration of keratinocytes leading to redness, thickening and scaling of epidermis followed with itching and appearance of the lesions which in most cases bother the patients medically and psychologically. Psoriasis is symptomatically treated by the range of oral and topical medications, however, major side effects in some cases are associated with them. Based on several studies, Curcuma longa can inhibit several inflammatory enzymes mainly involved in the inflammatory process of Psoriasis. Therefore, we decided to target this well-known herbal agent with fantastic safety profile to be formulated as a novel topical microemulgel. The clinical and therapeutic benefit of this novel topical formulation was evaluated on 34 patients with mild to moderate plaque psoriasis in a randomized, prospective intra-individual, right-left comparative, placebo-controlled, double-blind clinical trial. The Dermatology Life Quality Index (DLQI) Questionnaire and Psoriasis area & severity index (PASI) score as well as photos before and after treatment was used to evaluate the outcomes. The results show that the clinical and quality of life parameters in treated lesions in comparison with untreated lesions have improved (P<0.05). The reported side effects were also recorded and were trivial. Based on our findings, the proposed microemulgel may well be considered as an alternative in some patients and most likely as an add-on therapeutic option for many patients suffering with plaque psoriasis.
An Octonary Huffman Decoding Method and Its Application to MPEG-4 (2011)

传统的二值Huffman解码方法的解码效率较低。为了提高解码速度，该文提出了一种基于八叉树的Huffman解码方法。该方法将Huffman码表示为八叉树结构，并根据各个节点在树中的位置将码表重建为一维数组。解码时，每次从码流中读取3 bit码元，并使用数值计算代替判断和跳转操作，从而提高了解码效率。将本文方法应用于MPEG-4 VLC和RVLC解码的实验结果表明，该方法在内存增加不大的情况下能大幅度提高Huffman解码效率，其性能优于其它方法。
Discovery of a New Class of Potential Multifunctional Atypical Antipsychotic Agents Targeting Dopamine D<sub>3</sub>and Serotonin 5-HT<sub>1A</sub>and 5-HT<sub>2A</sub>Receptors: Design, Synthesis, and Effects on Behavior (2008)

Dopamine D(3) antagonism combined with serotonin 5-HT(1A) and 5-HT(2A) receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacological features of 5i are a high affinity for dopamine D(3), serotonin 5-HT(1A) and 5-HT(2A) receptors, together with a low affinity for dopamine D(2) receptors (to minimize extrapyramidal side effects), serotonin 5-HT(2C) receptors (to reduce the risk of obesity under chronic treatment), and for hERG channels (to reduce incidence of torsade des pointes). Pharmacological and biochemical data, including specific c-fos expression in mesocorticolimbic areas, confirmed an atypical antipsychotic profile of 5i in vivo, characterized by the absence of catalepsy at antipsychotic dose.
Sky-Scattered Solar Radiation Based Plume Transmissivity Measurement to Quantify Soot Emissions from Flares (2010)

For gas flares typical of the upstream energy industry and similar point sources, most current methods for characterizing soot emissions are based on plume opacity rather than a quantitative measure of mass flux. The absence of more quantitative approaches is indicative of the inherent complexity of soot and the difficulties in characterizing emissions in an unbounded plume. A new experimental approach has been developed for the investigation of soot emissions in industrial plumes. Referred to as sky-LOSA, the diagnostic permits evaluation of 2D spatially resolved monochromatic sky-light transmissivity data over the width of a plume, where sky-light intensities behind the plume are obtained via an interpolation algorithm. By using Rayleigh-Debye-Gans Fractal Aggregate theory to relate transmissivity data to soot concentrations, and with knowledge of the velocity of the plume, it is possible to quantify mass flow rates of soot in a plume. Experiments on an unconfined lab-scale soot plume were used to support a detailed uncertainty analysis under a wide range of conditions and to estimate sensitivity limits of the technique. Results suggest field measurements of soot emission from flare plumes should be possible with overall uncertainties of less than 32%. This represents a significant advancement over existing techniques based on opacity measurements.
On the use of Clocks to Enforce Consistency in the Cloud. (2015)

It is well known that the ability to timestamp events, to keep track of the order in which they occur, or to make sure they are processed in a way that is meaningful to the application, is of paramount importance in a distributed system. The seminal work by Leslie Lamport[30] has laid the foundations to understand the trade-offs associated with the use of physically and logically synchronized clocks for establishing the order of events. Lamport’s original work considered scalar clocks and has later been extended to consider richer forms of logical clocks such as vector clocks and matrix clocks. The purpose of this paper is to revisit these concepts in the concrete setting of developing distributed data store systems for the cloud. We look at how different clock mechanisms have been applied in practice to build different cloud data stores, with different consistency/performance trade-offs. Our goal is to gain a better understating of what are the concrete consequences of using different techniques to capture the passage of time, and timestamp events, and how these choices impact not only the performance of cloud data stores but also the consistency guarantees that these systems are able to provide. In this process we make a number of observations that may offer opportunities to enhance the next generations of cloud
Formal Development of Real-Time Priority-Based Schedulers (2005)

We introduce a deductive method for constructing real-time scheduling programs, based on continuous action systems and the higher-order logic of the refinement calculus. The schedulability goal is a guarantee that all the tasks meet their deadlines, at run-time. This analysis reduces to checking that "always" temporal properties hold on the task set, by enforcing adequate invariance properties. The initial, conjunctive model of the real-time system is further transformed, through refinement, into a program that obeys a specific scheduling policy. We exemplify our method on the Deadline-Monotonic and the Earliest-Deadline-First algorithms.
Synthesis of New Pyridinoazacrown Ethers Containing Aromatic and Heteroaromatic Proton Ionizable Substituents (1995)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of New Pyridinoazacrown Ethers Containing Aromatic and Heteroaromatic Proton Ionizable SubstituentsAndrei V. Bordunov, Paul C. Hellier, Jerald S. Bradshaw, N. Kent Dalley, Xiaolan Kou, Xian Xin Zhang, and Reed M. IzattCite this: J. Org. Chem. 1995, 60, 19, 6097–6102Publication Date (Print):September 1, 1995Publication History Published online1 May 2002Published inissue 1 September 1995https://doi.org/10.1021/jo00124a022RIGHTS & PERMISSIONSArticle Views690Altmetric-Citations29LEARN 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 InReddit PDF (849 KB) Get e-Alerts Get e-Alerts
Continuous Flow <sup>1</sup>H and <sup>13</sup>C NMR Spectroscopy in Microfluidic Stripline NMR Chips (2017)

Microfluidic stripline NMR technology not only allows for NMR experiments to be performed on small sample volumes in the submicroliter range, but also experiments can easily be performed in continuous flow because of the stripline's favorable geometry. In this study we demonstrate the possibility of dual-channel operation of a microfluidic stripline NMR setup showing one- and two-dimensional <sup>1</sup>H, <sup>13</sup>C and heteronuclear NMR experiments under continuous flow. We performed experiments on ethyl crotonate and menthol, using three different types of NMR chips aiming for straightforward microfluidic connectivity. The detection volumes are approximately 150 and 250 nL, while flow rates ranging from 0.5 μL/min to 15 μL/min have been employed. We show that in continuous flow the pulse delay is determined by the replenishment time of the detector volume, if the sample trajectory in the magnet toward NMR detector is long enough to polarize the spin systems. This can considerably speed up quantitative measurement of samples needing signal averaging. So it can be beneficial to perform continuous flow measurements in this setup for analysis of, e.g., reactive, unstable, or mass-limited compounds.
<title>Comparison of reversible methods for data compression</title> (1990)

Widely differing methods for data compression described in the ACR-NEMA draft are used in medical imaging. In our contribution we will review various methods briefly and discuss the relevant advantages and disadvantages. In detail we evaluate 1st order DPCM pyramid transformation and S transformation. We compare as coding algorithms both fixed and adaptive Huffman coding and Lempel-Ziv coding. Our comparison is performed on typical medical images from CT MR DSA and DLR (Digital Luminescence Radiography). Apart from the achieved compression factors we take into account CPU time required and main memory requirement both for compression and for decompression. For a realistic comparison we have implemented the mentioned algorithms in the C program language on a MicroVAX II and a SPARC station 1. 2.
Protective monoclonal antibodies recognize epitopes located on the major outer membrane protein of <i>Chlamydia trachomatis</i>. (1987)

A panel of monoclonal antibodies (MAb) was generated against Chlamydia trachomatis serovar B, an etiologic agent of blinding trachoma. The specificities of MAb were determined by dot blot assay by using viable elementary bodies of 13 C. trachomatis serovars and two C. psittaci strains. The dot blot assay was used to identify those antigens that were unique and immunoaccessible on the chlamydial surface. MAb were identified that recognized bi-specific (serovars B and Ba) or subspecies-specific (various B complex serovars) surface-exposed antigenic determinants that were either resistant or sensitive to heat denaturation (56 degrees C, 30 min). All of the MAb recognized the major outer membrane protein as determined by either immunoblotting or radioimmunoprecipitation. MAb specific for immunoaccessible major outer membrane protein epitopes protected mice from toxic death after i.v. injection of B serovar elementary bodies and neutralized the infectivity of the organism for monkey eyes. In contrast, MAb reactive against non-immunoaccessible subspecies- or species-specific major outer membrane protein epitopes or against an immunoaccessible genus-specific epitope located on chlamydial lipopolysaccharide did not protect mice from toxic death or neutralize infectivity of the parasite for monkey eyes. These data suggest that those major outer membrane protein antigenic determinants that are serovar or serogroup specific and are accessible to antibody on the chlamydial cell surface may be useful as a recombinant subunit vaccine for trachoma.