Miracle-dz/UniFAR-FTUs huggingface dataset:
Structure–Activity Relationships of New 1‐substitutedmethyl‐4‐[5‐(N‐methyl‐N‐propylamino)pentyloxy]piperidines and Selected 1‐[(N‐substituted‐N‐methyl)‐3‐propyloxy]‐5‐(N‐methy‐l‐N‐propyl)‐pentanediamines as H3‐Antagonists

Novel, potent non‐imidazole histamine H3 receptor antagonists have been prepared and in vitro tested as H3‐receptor antagonists (the electrically evoked contraction of the guinea‐pig jejunum). The present compounds contain a 4‐hydroxypiperidine core, which behaves as a conformationally restricted version of the 3‐amino‐1‐propanol moiety common to the many previously described non‐imidazole H3 ligands. Detailed structure‐activity studies revealed that 1‐(2‐benzofuranylmethyl)‐ 5c (pA2 = 8.47 ± 0.05) and 1‐(3‐benzofuranylmethyl)‐4‐[5‐(N‐methyl‐N‐propyl)pentyloxy]piperidine 5d (pA2 = 8.15 ± 0.07) exhibit high potency for the H3 histamine receptor. In addition, the potency of selected 1‐[(N‐substituted‐N‐methyl)‐3‐propyloxy]‐5‐(N‐methyl‐N‐propyl)pentanediamines as antagonist of the H3 histamine receptor was also evaluated. Replacement of the 4‐hydroxypiperidine of the leads 7 and 5c by a highly flexible 3‐(methylamino)propyloxy chain yields compounds 6a (pA2 = 8.02) and 6b (pA2 = 6.23) with higher and lower potency than their piperidine analogues (7, pA2 = 7.79; 5c, pA2 = 8.47), respectively. The histaminergic H1 antagonism of selected compounds 5c, 5d and 6a has been established on the isolated guinea‐pig ileum by conventional methods; the pA2 values have compared with the potency of pyrilamine. None of them showed any H1‐antagonistic activity (pA2 < 4; for pyrilamine pA2 = 8.5).
The Efficiency of Histogram-like Techniques for Database Query Optimization

One of the most difficult tasks in modern day database management systems is information retrieval. Basically, this task involves a user query, written in a high-level language such as the Structured Query Language, and some internal operations, which are transparent to the user. The internal operations are carried out through very complex modules that decompose, optimize and execute the different operations. We consider the problem of Query Optimization which consists of the system choosing, among many different query evaluation plans (QEPs), the most economical one. Since the number of QEPs increases exponentially as the number of relations involving the query increases, query optimization is a very complex problem. Many estimation techniques have been developed in order to approximate the cost of a QEP. Histogram-based techniques are the most used methods in this context. In this paper, we discuss the efficiency of some of these methods: Equi-width, Equi-depth, the Rectangular Attribute Cardinality Map (R-ACM) and the Trapezoidal Attribute Cardinality Map (T-ACM). These methods are used to estimate the cost of the different QEP, whence they attempt to determine the optimal one. It has been shown that the errors of the estimates from R-ACM and T-ACM are significantly less than the corresponding errors obtained from Equi-width and Equi-depth. This fact has been formally demonstrated using reasonable statistical distributions for the cost of a QEP, the doubly exponential distribution and the normal distribution. For the empirical analysis, we have developed a formal, rigorous prototype model used to analyze these methods on random databases. Our empirical results demonstrate that R-ACM chooses a superior QEP more than two times as often as Equi-width and Equi-depth. Similar results have been obtained for T-ACM when compared to the traditional methods. Indeed, in the most general scenario, we analytically provethat undercertain models thebetter theaccuracy of an estimation technique, the greater the probability of choosing the most efficient QEP.
Loopy Belief Propagation Algorithm in Distributed Wireless Cooperative Spectrum Sensing

Considering the date fusion in distributed cognitive radio networks, this paper studies the loopy belief propagation (LBP) algorithm to make the data fusion in distributed network with loops, and also gives a weighted modified LBP. This paper considers the effect of a shadow fading in the wireless channel model, and also exists malicious nodes, which may give the false result. The key idea is to model the network of secondary users as Markov random fields and to apply the loopy belief propagation algorithm or the weighted loopy belief propagation algorithm to facilitate decision fusion in a distributed manner. The paper shown that weighted LBP can solve the deep shadow fading and malicious nodes more effectively. Finally, a simulation with MATLAB has been done and verifies the results.
Autonomous e-coaching in the wild: empirical validation of a model-based reasoning system

Autonomous e-coaching systems have the potential to improve people's health behaviors on a large scale. The intelligent behavior change support system eMate exploits a model of the human agent to support individuals in adopting a healthy lifestyle. The system attempts to identify the causes of a person's non-adherence by reasoning over a computational model (COMBI) that is based on established psychological theories of behavior change. The present work presents an extensive, monthlong empirical validation study (N=82) of eMate in which participants were coached in their everyday life -- using a mobile app and a website -- towards taking the stairs more often. The eMate reasoning mechanism is evaluated on its accuracy and its ability to promote behavior change. Results show that eMate (i) identifies and accurately targets the problematic constructs for an individual and (ii) positively affects aspects of behavior change through tailored interventions.
Challenges for Industrial-Strength Information Retrieval on Databases

Implementing keyword search and other IR tasks on top of relational engines has become viable in practice, especially thanks to high-performance column-store technology. Supporting complex combinations of structured and unstructured search in real-world heterogeneous data spaces however requires more than “just” IR-on-DB. In this work, we walk the reader through our industrial-strength solution to this challenge and its application to a real-world scenario. By treating structured and unstructured search as first-class citizens of the same computational platform, much of the integration effort is pushed from the application level down to the data-management level. Combined with a visual design environment, this allows to model complex search engines without a need for programming.
Collaboration and Shared Reflections in the Classroom

This article describes a comprehensive model of professional collaboration that developed in an inner-city community school as teachers and administrators sought to address the needs of their economically disadvantaged students. Two certified teachers in each classroom (the basic team) share all teaching and planning responsibilities for their students and consult with the extended team of administrators, parents and colleagues at all grade levels to create an enriched, integrated curriculum. Our teachers find pervasive collaboration and continual self-reflection to be professionally rewarding. However, working in teams challenges professional relationships and requires new approaches in teaching, planning and organizing teaching practice. Communicating openly, taking risks, planning, and scheduling are a few of the collaborative processes developed and presented here.
Perspectives in Diabetes Therapeutic Strategies Based on Glucagon-Like Peptide 1

Glucagon-like peptide (GLP)-1 is an incretin hormone with potent glucose-dependent insulinotropic and glucagonostatic actions, trophic effects on the pancreatic -cells, and inhibitory effects on gastrointestinal secretion and motility, which combine to lower plasma glucose and reduce glycemic excursions. Furthermore, via its ability to enhance satiety, GLP-1 reduces food intake, thereby limiting weight gain, and may even cause weight loss. Taken together, these actions give GLP-1 a unique profile, considered highly desirable for an antidiabetic agent, particularly since the glucose dependency of its antihyperglycemic effects should minimize any risk of severe hypoglycemia. However, its pharmacokinetic/pharmacodynamic profile is such that native GLP-1 is not therapeutically useful. Thus, while GLP-1 is most effective when administered continuously, single subcutaneous injections have short-lasting effects. GLP-1 is highly susceptible to enzymatic degradation in vivo, and cleavage by dipeptidyl peptidase IV (DPP-IV) is probably the most relevant, since this occurs rapidly and generates a noninsulinotropic metabolite. Strategies for harnessing GLP-1’s therapeutic potential, based on an understanding of factors influencing its metabolic stability and pharmacokinetic/pharmacodynamic profile, have therefore been the focus of intense research in both academia and the pharmaceutical industry. Such strategies include DPP-IV–resistant GLP-1 analogs and selective enzyme inhibitors to prevent in vivo degradation of the peptide. Diabetes 53:2181–2189, 2004
Neutrophil accumulation in experimental myocardial infarcts: relation with extent of injury and effect of reperfusion.

The effects of reperfusion on the myocardial accumulation of neutrophils and their role in the extent of injury were investigated in a canine preparation with a 3 hr coronary occlusion followed by 21 hr of reperfusion. The left anterior descending coronary artery (LAD) was permanently occluded in group 1 and reperfused after 3 hr in four others (groups 2 to 5). All but group 5 received lidocaine (1 mg/min over 8 hr). A critical stenosis was produced and left in place at reperfusion only in group 2. In groups 1 and 2, 111In-labeled autologous neutrophils were injected at the time of coronary occlusion. Group 4 animals were rendered leukopenic 2 hr before the coronary ligature and throughout the experiment by injection of an antineutrophil rabbit serum. Quantification of the radioactivity by digitized scintigraphy of the heart slices revealed an 80% (p less than .05) increase in neutrophil accumulation in the infarct region after reperfusion (group 2) as compared with permanent occlusion (group 1). Gamma counting of myocardial tissue samples showed that the neutrophil accumulation ratio in the subendocardial central zone of the infarct was increased five times (p less than .05) by reperfusion, whereas no difference was evident in the subepicardium. Infarct size and myocardial area at risk were not statistically different among the five groups. However LAD flow in the leukopenic group (group 4) was significantly higher (p less than .05) 30 min after reperfusion (40.0 +/- 5 ml/min) when compared with the preocclusion value (21.7 +/- 4 ml/min). In contrast, in a parallel experiment without leukopenia (group 3), LAD flow after reperfusion did not differ from the preocclusion value. (ABSTRACT TRUNCATED AT 250 WORDS)
Time-Lapse Imaging Time-Lapse Imaging

By their very nature, biological systems are dynamic, and a proper understanding of the cellular and molecular processes underlying living organisms and how to manipulate them is a prerequisite to combat diseases and improve human health care. One of the major challenges of current biomedical research, therefore, is to unravel not just the spatial organization of these complex systems, but their spatiotemporal relationships [142,42]. Catalyzed by substantial improvements in optics hardware, electronic imaging sensors, and a wealth of fluorescent probes and labeling methods, light microscopy has, over the past decades, matured to the point that it enables sensitive time-lapse imaging of cells and even single molecules [150,93,166,100]. These developments have had a profound impact on how research is currently being conducted in the life sciences.
Memory design for selective error protection

Memory error protection is increasingly important as memory density and capacity continue to scale. This paper presents a memory SEP (Selective Memory Protection) design that enables SEP for commodity memory modules, with no change to the modules or devices. Memory error protection is provided through embedded ECC, a recently proposed, energy-efficient ECC memory organization. The memory SEP design splits the physical memory address space into two memory regions of adjustable sizes, one with error protection and one without. With this support, the OS can adjust the size ratio of the protected region and non-protected region based on the needs of applications. In this scheme, the mapping from a physical memory address to memory device addresses is no longer power-of-two based. New and efficient address mapping schemes based on the Chinese Remainder Mapping are proposed to avoid the use of complex Euclidean division. The simulation results show that the memory SEP design may retain memory performance and cut memory power increase, while providing the ECC protection to commodity memory modules.
A Wikipedia-based approach to conceptual indexing and retrieval of documents

This paper describes a support system helping archivists in indexing and retrieving documents. Our method is based on the Wikipedia category network as a conceptual taxonomy. A directed acyclic graph (DAG) is built for each document by mapping terms (one or more words) to a concept in the Wikipedia category network. Properties of the graph are used to weight these concepts. According to the so–called important concepts, topics and keywords are proposed. Conceptual indexing consists in finding the relevant Wikipedia papers and categories, which can be used to describe the text. Conceptual retrieval consists in using these papers and categories to return the relevant documents for a user query. Finally, a proof–of–concept prototype is presented.
A Critical Review of the Ontological Assumptions of Actor-Network Theory for Representing e-Government Initiatives

The potential contribution of Actor-Network Theory ANT for representing e-government initiative flows from its ontological assumptions. However, these assumptions have never been critically reviewed using real e-government cases. Using two e-government cases in Indonesia, the paper tries to provide real evidence on how meaningful are all ontological assumptions of ANT for representing e-government.
Distinguishable Patterns of Competition, Collusion, and Parallel Action

Alternative market structures are distinguishable by the degree of parallel action exhibited by producers. We show that the correlation between output levels varies systematically with the degree of interdependence among firms, and establish an ordering among alternative behavioral hypotheses (Cournot, Stackelberg, Edgeworth/Bertrand, collusion, and perfect competition). Because the ordering is invariant to the values of background parameters, statistical tests of market conduct may be possible even when the slopes of the demand curve and marginal cost curves are unknown. An application to the world oil market finds strong evidence of collusive behavior among OPEC members, but not elsewhere.
Brain and arterial abnormalities following prenatal X‐ray irradiation in mice assessed by magnetic resonance imaging and angiography

The present study aimed to quantitatively characterize changes in the whole brain and arterial morphology in response to prenatal ionizing irradiation. Magnetic resonance imaging (MRI) and angiography (MRA) were used to evaluate brain and arterial abnormalities in 8‐week‐old male mice prenatally exposed to X‐ray radiation at a dose of 0.5 or 1.0 Gy on embryonic day (E) 13. Irradiated mice demonstrated decreased brain volume, increased ventricular volume, and arterial malformation. Additionally, MRA signal intensity and arterial thickness in the anterior cerebral artery, middle cerebral artery, and basilar artery were lower in radiation‐exposed mice than in control mice. MRI and MRA are useful tools for assessing brain and arterial abnormalities after prenatal exposure to radiation.
Contribution of ATM and ATR to the Resistance of Glioblastoma and Malignant Melanoma Cells to the Methylating Anticancer Drug Temozolomide

The major cytotoxic DNA adduct induced by temozolomide and other methylating agents used in malignant glioma and metastasized melanoma therapy is O6-methylguanine (O6-MeG). This primary DNA damage is converted by mismatch repair into secondary lesions, which block replication and in turn induce DNA double-strand breaks that trigger the DNA damage response (DDR). Key upstream players in the DDR are the phosphoinositide 3-kinases ataxia telangiectasia mutated (ATM) and ataxia telangiectasia and Rad3 related (ATR). Here, we addressed the question of the importance of ATM and ATR in the cell death response following temozolomide. We show that (i) ATM- and ATR-mutated cells are hypersensitive to temozolomide, (ii) O6-MeG triggers ATM and ATR activation, (iii) knockdown of ATM and ATR enhances cell kill in gliobalstoma and malignant melanoma cells with a stronger and significant effect in ATR knockdown cells, (iv) ATR, but not ATM, knockdown abolished phosphorylation of H2AX, CHK1, and CHK2 in glioma cells, and (v) temozolomide-induced cell death was more prominently enhanced by pharmacologic inhibition of CHK1 compared with CHK2. The data suggest that ATM and, even better, ATR inhibition is a useful strategy in sensitizing cancer cells to temozolomide and presumably also other anticancer drugs. Mol Cancer Ther; 12(11); 2529–40. ©2013 AACR.
Antibodies Against the First Ig-Like Domain of Human Platelet Endothelial Cell Adhesion Molecule-1 (PECAM-1) That Inhibit PECAM-1-Dependent Homophilic Adhesion Block In Vivo Neutrophil Recruitment1

Platelet endothelial cell adhesion molecule (PECAM-1), a member of the Ig superfamily, is found on endothelial cells and neutrophils and has been shown to be involved in the migration of leukocytes across the endothelium. Adhesion is mediated, at least in part, through binding interactions involving its first N-terminal Ig-like domain, but it is still unclear which sequences in this domain are required for in vivo function. Therefore, to identify functionally important regions of the first Ig-like domain of PECAM-1 that are required for the participation of PECAM-1 in in vivo neutrophil recruitment, a panel of mAbs against this region of PECAM-1 was generated and characterized in in vitro adhesion assays and in an in vivo model of cutaneous inflammation. It was observed that mAbs that disrupted PECAM-1-dependent homophilic adhesion in an L cell aggregation assay also blocked TNF-α-induced intradermal accumulation of neutrophils in a transmigration model using human skin transplanted onto SCID mice. Localization of the epitopes of these Abs indicated that these function-blocking Abs mapped to specific regions on either face of domain 1. This suggests that these regions of the first Ig-like domain may contain or be close to binding sites involved in PECAM-1-dependent homophilic adhesion, and thus may represent potential targets for the development of antiinflammatory reagents.
Anxiety and depression among Nigerian patients with asthma; Association with sociodemographic, clinical, and personality factors

ABSTRACT Objective: To estimate the rate of anxiety and depression in adult asthma patients and examine the possible association with sociodemographic, clinical and other significant variables. Methods: Adult asthmatics (n = 203) were recruited from the asthma outpatient clinic and assessed for sociodemographic and clinical profiles, their levels of disability, social support, asthma treatment stigma and personality traits. The Mini International Neuropsychiatric Interview (M.I.N.I) was used to assess for the diagnosis of Anxiety and Depression in comparison with matched healthy controls (n = 205). Results: Seventy (34.5%) of the patients with asthma have a diagnosis of Anxiety or Depression compared with 15 (7.3%) of matched healthy controls and the difference was significant (OR 6.67, 95% CI 3.58–13.04). Although older age, lower income, use of oral corticosteroid, patients perceived severity of asthma, disability, social support and personality traits were initially significant in univariate analysis, a subsequent logistic regression analysis revealed that only disability scores above the group mean (OR 4.50, 95% CI 2.28–8.87) and not having a strong social support (OR 2.88, 95% CI 1.443–5.78) were the only variables independently associated with diagnosis of Anxiety and Depression in the group of patients with asthma. Conclusion: Anxiety and depression are significantly more common in adult outpatients with asthma when compared with healthy control in Nigeria and was significantly associated with levels of disability and social support. These factors should be considered while formulating predictive models for management of psychosocial problems in asthma in this environment.
Colored Petri Net Based Automatic Service Composition

Service composition is an effective method to achieve flexible pervasive application. According to the relationship of messages and behaviors, we define a message oriented activity based Petri net (Moap) model to describe service, which supports concurrent processes and the reuse of composite service. And user's loose requirement is denoted as goal which is composed of expected input, output and key behaviors. Based on Moap, an automatic service composition algorithm autoSC is proposed to automatically create a specification of composite process to achieve goal. Finally, we analyze the effectiveness of autoSC and give a detailed comparison with other methods.
Model Checking for Generation of Test Suites in Software Unit Testing

Model checking is a technique for exhaustively searching the model’s state space for possible errors. Testing is a common method for enhancing the quality of a software product by checking for errors in program executions sampled according to some criterion called coverage criterion. Testing is a costly process especially if it is not supported by an appropriate method (and tool) for generating test suites, i.e. sets of test cases that fulfil a specific coverage criterion. This work introduces a method based on model checking, that supports generation of test cases for coverage based unit testing. As a proof of concept, we provide results obtained from the developed prototype tool support. Our method relies on automatically deriving from the source code a SPIN model with injected breakpoints. Test cases are obtained as counterexamples of violated Linear Temporal Logic (LTL) formulae that are automatically produced based on the selected coverage criterion. Keywords—Software testing, Model Checking, Unit Testing, Coverage Criteria.
Towards Integrated Acoustic Models for Speech Synthesis

All Statistical Parametric Speech Synthesizers consist of a linear pipeline of components. This view means that the synthesizer consists of a top-down structure where data fed into the synthesizer goes to front-end, then to the prediction algorithm, then to the waveform generation, and so on until the speech is finally constructed. Each component in this pipeline naïvely receives a stream of numbers from the preceding component, and spits out a stream of numbers for the next one in line, with little to no knowledge of what happens in the larger scheme of the pipeline. In this thesis, I argue against this “Markovian” structure, and instead propose the idea of an Integrated structure. In an integrated structure, every component in the system influences, and is in turn influenced by every other component in the system. This thesis describes four sets of experiments that move towards this idea. The first involves using lexical information to improve waveform generation algorithms. The second tries to increase the interaction between prediction algorithms and waveform generation. The third is an attempt to derive phonemes and phonetic information automatically from the speech rather than from the text. The last, and probably hardest, describes an idea for an evaluation metric that pays attention to multiple components of the synthesizer, rather than focusing on just a single one.