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Population analysis to assess the influence of age and body weight on pharmacokinetics and pharmacodynamics of dexmedetomidine in New Zealand White rabbits
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Acute and subacute (28-Day) toxicity studies of ionic liquid, didecyldimethyl ammonium acesulfamate, in rats
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The pharmacokinetics of propofol in ICU patients undergoing long-term sedation
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The quantification of reticulocyte maturation and neocytolysis in normal and erythropoietin stimulated rats
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Protective Effect of Aronia Melanocarpa Polyphenols on Cadmium Accumulation in the Body: A Study in a Rat Model of Human Exposure to this Metal
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Aqueous Extracts of Selected Potentilla Species Modulate Biological Activity of Human Normal Colon Cells
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New Insights into Dietary Supplements Used in Sport: Active Substances, Pharmacological and Side Effects
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Complexation of Bioelements and Toxic Metals by Polyphenolic Compounds - Implications for Health
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Antioxidants as a Potential Preventive and Therapeutic Strategy for Cadmium
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Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: implications for clinical use.
PublikacjaThe acridinone derivates C-1305 and C-1311 are promising antitumor agents with high activity against several experimental cellular and tumor models and which are under evaluation in pre-clinical and early phase clinical trials. Recent evidence from our laboratories has indicated that both compounds were conjugated by several UGT isoforms with the most active being extrahepatic UGT1A10. The present studies were designed to test...
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Role of Human UDP-Glucuronosyltransferases in the Biotransformation of the Triazoloacridinone and Imidazoacridinone Antitumor Agents C-1305 and C-1311 : Highly Selective Substrates for UGT1A10
Publikacja5-Diethylaminoethylamino-8-hydroxyimidazoacridinone, C-1311 (NSC-645809), is an antitumor agent shown to be effective against breast cancer in phase II clinical trials. A similar compound, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, shows high activity against experimental tumors and is expected to have even more beneficial pharmacological properties than C-1311. Previously published studies showed that these...
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The role of intestine and liver in glucuronidation of the imidazo- and triazoloacridinone antitumor agents, C-1311 and C-1305: High affinity substrates for UGT1A10
PublikacjaCelem przeprowadzonych badań było określenie roli poszczególnych izoform UDP-glukuronylotransferazy (UGT)oraz mikrosomów jelita(HIM)i wątroby (HLM) wyizolowanych od różnych pacjentów w metabolizmie pochodnych akrydonu, związków C-1311 i C-1305. Wykazano, że rodziną UGT katalizującą przemiany C-1305 i C-1311 jest UGT1A, z najwyższą aktywnością wykazywaną przez pozawątrobowy izoenzym UGT1A10. Rozkład aktywności frakcji mikrosomalnych...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublikacjaZwiązki oznaczone symbolami JWH-018 i JWH-073 są syntetycznymi pochodnymi kanabinoidów, obecnymi w preparatach o działaniu psychoaktywnym (K2/Spice). Wcześniejsze badań wykazały, że u osób przyjmujących tzw. ''legalną marihuanę'', głównymi produktami biotransformacji obecnymi w moczu były hydroksylowe pochodne obu związków, jak również ich glukuronidy. W związku z tym celem prowadzonych badań było określenie roli poszczególnych...
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublikacjaA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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In silico design of telomerase inhibitors.
PublikacjaTelomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms...
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Targeting shelterin proteins for cancer therapy.
PublikacjaAs a global health challenge, cancer prompts continuous exploration for innovative therapies that are also based on new targets. One promising avenue is targeting the shelterin protein complex, a safeguard for telomeres crucial in preventing DNA damage. The role of shelterin in modulating ataxia- telangiectasia mutated (ATM) and ataxia-telangiectasia and Rad3-related (ATR) kinases, key players in the DNA damage response (DDR),...
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Human carnosinases: A brief history, medicinal relevance, and in silico analyses
PublikacjaCarnosine, an endogenous dipeptide, has been found to have a plethora of medicinal properties, such as antioxidant, antiageing, and chelating effects, but with one downside: a short half-life. Carnosinases and two hydrolytic enzymes, which remain enigmatic, are responsible for these features. Hence, here we emphasize why research is valuable for better understanding crucial concepts like ageing, neurodegradation, and cancerogenesis,...
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The Comparison of the Web GIS Applications Relevant for 4D Models Sharing
PublikacjaThe paper presents results of the project: Cultural Heritage Through Time (CHT 2, http://cht2-project.eu) realized accomplished within the framework of the “Joint Programming Initiative in Cultural Heritage” JPI-CH (http://www.jpi-culturalheritage.eu) by an international consortium: Politecnico di Milano (IT), Newcastle University (UK), Salamanca University (ES), and Stanislaw Staszic Scientific Association SSSA (a non-profit...
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Calibration of acoustic vector sensor based on MEMS microphones for DOA estimation
PublikacjaA procedure of calibration of a custom 3D acoustic vector sensor (AVS) for the purpose of direction of arrival (DoA) estimation, is presented and validated in the paper. AVS devices working on a p-p principle may be constructed from standard pressure sensors and a signal processing system. However, in order to ensure accurate DoA estimation, each sensor needs to be calibrated. The proposed algorithm divides the calibration process...
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An attempt to create a digital reconstruction of the Copper Ship = Próba cyfrowej rekonstrukcji kadłuba wraku Miedziowca
PublikacjaThis study presents an attempt to create a digital reconstruction of the W-5 shipwreck (the Copper Ship) based on data acquired by 3D scanning of structural components held at the National Maritime Museum in Gdańsk and on a physical reconstruction model of the ship’s hull. A digital reconstruction would facilitate analysis of various possible options for the structural design of the hull, and would enable the preparation of a model for...
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Comprehensive thermodynamic analysis of steam storage in a steam cycle in a different regime of work: A zero-dimensional and three-dimensional approach
PublikacjaDue to the current trends aiming to reduce carbon dioxide emissions by increasing the use of renewable energy sources, changes are required in the operation of coal-fired steam units. The unstable nature of renewable energy sources, depending on weather conditions, means that the amount of energy produced varies and is not always in line with peak demand. To ensure the security and stability of energy supplies in the energy system,...
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Spin-Resolved Band Structure of Hoffman Clathrate [Fe(pz)2Pt(CN)4] as an Essential Tool to Predict Optical Spectra of Metal–Organic Frameworks
PublikacjaParamount spin-crossover properties of the 3D-Hoffman metalorganic framework (MOF) [Fe(pz)2Pt(CN)4] are generally described on the basis of the ligand field theory, which provides adequate insight into theoretical and simulation analysis of spintronic complexes. However, the ligand field approximation does not take into account the 3D periodicity of the actual complex lattice and surface effects and therefore cannot predict a full-scale...
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Impact of selected drugs and their binary mixtures on the germination of Sorghum bicolor (sorgo) seeds
PublikacjaThe aim of this study was to assess the toxicological potential of binary drug mixtures and individual drugs under different pH conditions with different inorganic ion additions on the germination of Sorghum bicolor (sorgo) seeds. To assess whether the given drug mixtures were more phytotoxic than the individual compounds, concentration addition (CA) and independent action (IA) approaches were applied to estimate the predicted...
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Człowiek zanurzony w rzeczywistości wirtualnej na przykładzie Laboratorium Zanurzonej Wizualizacji Przestrzennej
PublikacjaArtykuł opisuje Laboratorium Zanurzonej Wizualizacji Przestrzennej (LZWP), które umożliwia swobodną podróż w czasie i przestrzeni. Jego podstawowym wyposażeniem jest jaskinia rzeczywistości wirtualnej, czyli pomieszczenie o ścianach, suficie i podłodze stanowiących ekrany projekcyjne, wyświetlające generowane komputerowo obrazy 3D, tworzące spójny widok jednej sceny. Człowiek znajdujący się w takiej jaskini jest zatem zanurzony...
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Problem of aggregation in dye-DNA interaction, calorimetry studies
PublikacjaNucleic acids are the biological target for many antimicrobial, antitumor and antiviral drugs. Ligand-DNA interactions can be classified into two major categories: 1. covalent binding, which can provide to intermolecular adducts, 2. physico-chemical interactions, which can be divided into intercalation (e.g. adriamycin) or groove binding (e.g. dystamycin). There are several methods to investigate interactions between drug and DNA....
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4D Models in World Wide Web
PublikacjaThe paper presents some results of research curried out within the framework of the European project named "Cultural Heritage Through Time" (CHT2). One of the main project aims were to develop a methodology for sharing multi-temporal information via the Internet (webGIS) for remote analysis of structures and landscapes over time. Reported in this paper results are focused on testing two technologies (Hexagon and Esri) for online...
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Electronic structure and time-dependent description of rotational predissociation of LiH
PublikacjaThe adiabatic potential energy curves of the ^1Sigma+ and ^1Pi states of the LiH molecule were calculated. They correlate asymptotically to atomic states, such as 2s + 1s, 2p + 1s, 3s + 1s, 3p + 1s, 3d + 1s, 4s + 1s, 4p + 1s and 4d + 1s. A very good agreement was found between our calculated spectroscopic parameters and the experimental ones. The dynamics of the rotational predissociation process of the 1^1Pi state were studied...
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Comparative analysis of numerical with optical soliton solutions of stochastic Gross–Pitaevskii equation in dispersive media
PublikacjaThis article deals with the stochastic Gross–Pitaevskii equation (SGPE) perturbed with multiplicative time noise. The numerical solutions of the governing model are carried out with the proposed stochastic non-standard finite difference (SNSFD) scheme. The stability of the scheme is proved by using the Von-Neumann criteria and the consistency is shown in the mean square sense. To seek exact solutions, we applied the Sardar subequation...
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Sensitivity analysis of a composite footbridge
PublikacjaThis work include an example of sensitivity analysis for the design of a composite footbridge. A sandwich structure is used, consisting two high-strength skins separated by a core material. The analysis was conducted for two numerical models. The first one is a simple, single-span beam of a composite cross-section (laminate and foam), with different Young’s modulus for each material. Calculations were made by means of a MATLAB-based...
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Processing of Hydroacoustic and LiDAR Data for Three-dimensional Surface Reconstruction
PublikacjaThe technologies of sonar and laser scanning are commonly used for obtaining spatial information about underwater and over ground environments in the form of point clouds. Since this data model has known disadvantages, a more practical solution of visualising such data involves the creation of solid three-dimensional meshes composed of edges and facets. In this paper, several methods for 3D shape reconstruction of data obtained...
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Application of Fast Cameras to String Vibrations Recording
PublikacjaA hardware and software solution for guitar string vibration measurement by fast cameras is described. Orthogonal setup for 3D image acquisition is proposed capable to capture several thousand image frames per second. Dedicated image processing algorithm was developed and described in the paper, aimed at tracking the movement of some selected points along the string. Fast and accurate tracking results provided a detailed information...
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Quaternion encryption methods for multimedia transmission, a survey of existing approaches
PublikacjaIn this paper we review quaternion encryption methods for multimedia transmission. We explain their weak and strong properties as well as suggest possible modifications. Our main focus is an algorithm QFC presented in paper by Dzwonkowski et al. (2015). All encryption methods, presented in this paper, use special properties of quaternions to perform rotations of data sequences in 3D space. Each method uses a common key generation...
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KTaO3-based nanocomposites for air treatment
PublikacjaA series of single semiconductors and their nanocomposites combination (such as KTaO3 + CdSe + SrTiO3; KTaO3 + CdS +WO3; KTaO3 + CdS + MoS2) were prepared using hydrothermal route. Photocatalytic activity of as-prepared nanocomposites was estimated by photocatalytic degradation of toluene in the gas phase using light-emitting diodes (LEDs, 375 nm) in four subsequent cycles. The nanocomposites were characterized by scanning electron...
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Microstructure–Property Relationship of Polyurethane Foams Modified with Baltic Sea Biomass: Microcomputed Tomography vs. Scanning Electron Microscopy
PublikacjaIn this paper, novel rigid polyurethane foams modified with Baltic Sea biomass were compared with traditional petro-based polyurethane foam as reference sample. A special attention was focused on complex studies of microstructure, which was visualized and measured in 3D with high-resolution microcomputed tomography (microCT) and, as commonly applied for this purpose, scanning electron microscopy (SEM). The impact of pore volume,...
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The Effect of Protrusions on the Initiation of Partial Discharges in XLPE High Voltage Cables
PublikacjaThis paper is focusing on 3D Finite Elements Analysis (FEA) based modelling of protrusions as defects or imperfections in the XLPE high voltage cable. This study is aiming to examine the impact protrusions have on the initiation of partial discharges. Spherical and ellipsoidal protrusions with different sizes at the conductor screen of the high voltage cable is an essential content of this paper. In addition, a spherical gas-filled...
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A three-dimensional meso-scale approach to concrete fracture based on combined DEM with x-ray micro-CT images
PublikacjaArtykuł omawia wyniki numeryczne uzyskane stosując 3-wymiarowy mezoskopowy model do opisu pękania w betonie na poziomie kruszywa w belce z nacięciem podczas zginania. Do obliczeń użyto metodę elementów dyskretnych. Beton został opisany jako materiał 4-fazowy złożony z kruszywa, zaprawy, makro-porów i stref przejściowych miedzy kruszywem a zaprawą. Kształt i położenia kruszywa przyjęto na podstawie skanów z mikro-tomografu. Uzyskano...
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Data regarding a new, vector-enzymatic DNA fragment amplification-expression technology for the construction of artificial, concatemeric DNA, RNA and proteins, as well as biological effects of selected polypeptides obtained using this method
PublikacjaApplications of bioactive peptides and polypeptides are emerging in areas such as drug development and drug delivery systems. These compounds are bioactive, biocompatible and represent a wide range of chemical properties, enabling further adjustments of obtained biomaterials. However, delivering large quantities of peptide derivatives is still challenging. Several methods have been developed for the production of concatemers –...
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Tyre/road noise reduction of poroelastic road surface tested in a laboratory
PublikacjaA so-called poroelastic road surface (PERS) is being developed in Europe. This contains a large percentage of rubber particles mixed with hard aggregate (stone and sand) and bound with polyurethane. This gives high air void content (around 30 %), high elasticity and smooth texture, all of which should give low noise properties. Inthis experiment anominally 30 mm thick sample of PERS was mounted on a steel drum. Various car tyres...
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Ipertrofan Revisited—The Proposal of the Complete Stereochemistry of Mepartricin A and B
PublikacjaBeing a methyl ester of partricin, the mepartricin complex is the active substance of a drug called Ipertrofan (Tricandil), which was proven to be useful in treatment of benign prostatic hyperplasia and chronic nonbacterial prostatitis/chronic pelvic pain syndrome. Nevertheless, no direct structural evidence on the stereochemistry of its components has been presented to date. In this contribution, we have conducted detailed, NMR-driven...
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Nowe substancje psychoaktywne CZ. II. SYNTETYCZNE KANNABINOIDY - CHARAKTERYSTYKA, METODY OZNACZANIA I WYZWANIA ANALITYCZNE
PublikacjaDo nielegalnego obrotu co roku trafiają nowe związki o działaniu psychoaktywnym. Dostęp do takich substancji nie jest trudny, gdyż są one łatwo dostępne w wielu krajach, głównie w sklepach internetowych. Ponadto, organy ścigania i wymiar sprawiedliwości nie nadążają z wprowadzaniem tych substancji na listy substancji zakazanych przez co ich kontrola jest bardzo utrudniona. Syntetyczne kannabinoidy to grupa związków chemicznych,...
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Solvent effects on fluorescence properties of protochlorophyll and its derivatives with various porphyrin side chains
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Protochlorophyll complexes with similar steady-state fluorescence characteristics can differ in fluorescence lifetimes. A model study in Triton X-100
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Trust Models for Community- Aware Identity Managment. [....]
PublikacjaArtykuł przedstawia możliwości budowania zaufania pomiędzy członkami społecznych sieci współpracujacych w Internecie. Przedstawiono system informatyczne wykorzystującyna współczesą wiedzę z zakresu psychologi społecznej, umozliwiajacy tworzenie sieci społecznych w internecie.
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Study on 19th-century cast iron columns from the former financial office building in Kwidzyn
PublikacjaThe article presents the results for cast iron columns used as floor supports in the former financial office building in Kwidzyn (Poland).The stocktaking drawings provided the general and detailed data about the 19th century designer’s decisions. During the research, architectural and structural analysis was carried out. The graphics were used as a starting material for preparing 3D calculation models. The FEM-based numerical simulations...
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4D Reconstruction and Visualisation of Krakow Fortress
PublikacjaThe specific aim of the European project named "Cultural Heritage Through Time" (CHT2) and reported in this paper is to fully integrate the fourth dimension (4D) into Cultural Heritage studies for analysing structures and landscapes over time. Krakow-the Fortress City (Poland) is the one of four case studies of the CHT2, which are used for the time varying reconstruction, analysis, visualization, and preservation. The goal of...
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Nonlinear viscoelasticity in Three Dimensional filler reinforced rubber composites and nanocomposites
PublikacjaThis chapter describes the influence of three-dimensional nanofillers used in elastomers on the nonlinear viscoelastic properties. In particular, this part focuses and investigates the most important three-dimensional nanoparticles, which are used to produce rubber nanocomposites. The rheological and the dynamic mechanical properties of elastomeric polymers, reinforced with spherical nanoparticles, like POSS, titanium dioxide and...
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Wizyjny system monitoringu stanu nakładek ślizgowych odbieraków prądu
PublikacjaEksploatowane do niedawna w Polsce nakładki kolejowych odbieraków prądu były wykonywane w postaci styków miedzianych. Na początku 2011 r. przeprowadzono kompleksową zmianę typu nakładek stykowych z miedzianych na metalizowane węglowe.Wraz z wprowadzeniem nakładek węglowych istnieje potrzeba opracowania nowych metod diagnostyki tego istotnego elementu toru zasilania pojazdu. Celem diagnostyki jest wykrycie uszkodzonych i nadmiernie...
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A Conception of Pairwise Comparisons Model for Selection of Appropriate Body Surface Area Calculation Formula
PublikacjaBody surface area (BSA) may be computed using a variety of formulas, but the computed BSA differs from real BSA values for particular subjects. This is presented in the paper by computing BSA values for selected subject and comparing them to the real BSA value obtained with the use of a 3D body scanner. The results show inequalities in the relevant BSA computing formulas. Hence, there is a need to determine a method that will allow...
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Influence of Dielectric Overlay Permittivity on Size and Performance of Miniaturized ESPAR Antenna
PublikacjaIn this paper, influence of dielectric overlay permittivity on miniaturized ESPAR antenna parameters is presented. ESPAR antenna is a low-cost and energy-efficient way to implement beam steering capability to a node and improve network performance. The antenna size reduction is obtained by embedding its active and passive elements in ABS based materials of relative permittivity equal to 4, 5.5 and 7.5 in order to achieve network...