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Search results for: UGT-MODULATED PHARMACOKINETICS
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Copper(I) halide cluster-based coordination polymers modulated by chiral ditopic dithiodianthranilide ligands: synthesis, crystal structure and photoluminescence
PublicationReaction of copper(I) halides with chiral dithiodianthranilidesmdtaandbdtaafforded polymeric complexeswhere polynuclear CuX clusters were linked together by ditopic bridging ligands into 1D chains or 2D layerstructures. In the case of racemic ligands double stranded chain polymers were formed where the Cu4X4(X = I or Br) cores are connected by enantiomeric pairs of the ditopic ligands. In contrast, a homochiralmdtaligand created...
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<p>In vivo Studies on Pharmacokinetics, Toxicity and Immunogenicity of Polyelectrolyte Nanocapsules Functionalized with Two Different Polymers: Poly-L-Glutamic Acid or PEG</p>
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Systemic modulation of stress and immune parameters in patients treated for prostate adenocarcinoma by intensity-modulated radiation therapy or stereotactic ablative body radiotherapy
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Diverging frequency-modulated 50-kHz vocalization, locomotor activity and conditioned place preference effects in rats given repeated amphetamine treatment
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Inter-individual diversity and intra-individual stability of amphetamine-induced sensitization of frequency-modulated 50-kHz vocalization in Sprague–Dawley rats
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Rats showing low and high sensitization of frequency-modulated 50-kHz vocalization response to amphetamine differ in amphetamine-induced brain Fos expression
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Diverging changes in rat striatal extracellular dopamine and DOPAC levels and in frequency-modulated 50-kHz ultrasonic vocalizations rate during repeated amphetamine treatment
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Pulse-Modulated Radio-Frequency Alternating-Current-Driven Atmospheric-Pressure Glow Discharge for Continuous-Flow Synthesis of Silver Nanoparticles and Evaluation of Their Cytotoxicity toward Human Melanoma Cells
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Efficacy, pharmacokinetics, and safety of the biosimilar CT-P10 compared with rituximab in patients with previously untreated advanced-stage follicular lymphoma: a randomised, double-blind, parallel-group, non-inferiority phase 3 trial
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Glukuronidacja leków przeciwnowotworowych – detoksyfikacja, mechanizm oporności czy sposób na formę proleku?*
PublicationKsenobiotyki podlegają w organizmie biotransformacji I i II fazy, której celem jest ich detoksyfikacja i ułatwienie wydalania. UDP-glukuronylotransferazy (UGT) – enzymy należące do II fazy metabolizmu katalizują przyłączenie kwasu glukuronowego do lipofilowego substratu zawierającego nukleofilową grupę funkcyjną. Nadrodzina UGT składa się z izoenzymów o różnej swoistości substratowej oraz odmiennym profilu ekspresji w poszczególnych tkankach....
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Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublicationBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
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Drug-drug interaction potential of antitumor acridine agent C-1748: The substrate of UDP-glucuronosyltransferases 2B7, 2B17 and the inhibitor of 1A9 and 2B7
PublicationBackground The compound 9-(2′-hydroxyethylamino)-4-methyl-1-nitroacridine (C-1748), the promising antitumor agent developed in our laboratory was determined to undergo phase I metabolic pathways. The present studies aimed to know its biotransformation with phase II enzymes – UDP-glucuronosyltransferases (UGTs) and its potential to be engaged in drug-drug interactions arising from the modulation of UGT activity. Methods UGT-mediated...
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UDP-glukuronylotransferazy - białka siateczki śródplazmatycznej. Struktura i mechanizm działania
PublicationIzoenzymy UDP-glukuronylotransferazy (EC. 2.4.1.17), UGT, katalizują w organizmach ssaków reakcję koniugacji grupy glikozylowej pochodzącej z nukleotydu UDPGA z aglikonem. UDPGA jest przyłączany do odpowiedniej grupy funkcyjnej metabolitu I fazy, rzadziej związku wyjściowego, przez co polarność aglikonu i zdolność jego wydalania z komórki zwiększa się, a to w konsekwencji obniża efekt toksyczny.Struktura UGT zawiera 2 domeny. Domena...
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Population Pharmacokinetic Modelling of Filgrastim in Healthy Adults following Intravenous and Subcutaneous Administrations
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Human UDP-Glucuronosyltransferases: Effects of altered expression in breast and pancreatic cancer cell lines.
PublicationIncreased aerobic glycolysis and de novo lipid biosynthesis are common characteristics of invasive cancers. UDP-glucuronosyltransferases (UGTs) are phase II drug metabolizing enzymes that in normal cells possess the ability to glucuronidate these lipids and speed their excretion; however, de-regulation of these enzymes in cancer cells can lead to an accumulation of bioactive lipids, which further fuels cancer progression. We hypothesize...
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Review on Current Status of Echinocandins Use
PublicationFungal infections are rising all over the world every year. There are only five medical compound classes for treatment: triazoles, echinocandins, polyenes, flucytosine and allylamine. Currently, echinocandins are the most important compounds, because of their wide activity spectrum and much lower sides effects that may occur during therapy with other drugs. Echinocandins are secondary metabolites of fungi, which can inhibit the...
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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
PublicationCelem 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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Characterization of corrosion in reinforced concrete beams using destructive and non-destructive tests
PublicationThe paper presents both non-destructive and destructive experimental tests on steel-reinforced concrete beams subjected to electrochemical corrosion. To examine the condition and behavior of the specimens, destructive tests were carried out, i.e., a three-point bending together with a modulated ultrasonic wave test. In addition, a series of non-destructive experiments were conducted, such as the potential measurement method, low-frequency...
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Age-structured population model of cell survival
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Assessing circadian rhythms in propofol PK and PD during prolonged infusion in ICU patients
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UDP-glukuronylotranferazy w metabolizmie detoksykacyjnym i aktywacyjnym związków endogennych oraz ksenobiotyków
PublicationGlukuronidacja jest główną drogą koniugacji w szlakach metabolizmu i wydalania związków endogennych oraz ksenobiotyków. Reakcja ta jest katalizowana przez UDP-glukuronylotransferazy, UGT, dla których substratami są bilirubina, hormony steroidowe, tyroidowe i kwasy żółciowe, oraz związki egzogenne, w tym leki, związki kancerogenne, chemiczne zanieczyszczenia środowiska i składniki żywności. Z terapeutycznego punktu widzenia szczególnie...
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The II phase metabolism of endogenous and exogenous compounds, including antitumor chemotherapeutics
PublicationThe II phase metabolism, it is a set of metabolism and excretion pathways of endogenous as well as exogenous compounds including xenobiotics. UDP-glucuronyltransferases (UGTs; EC 2.4.1.17) are the most crucial representatives of II phase enzymes, which are responsible for the transformation of bilirubine and bile acids, steroids and thyroid hormones and lipids. Exogenous compounds, including drugs, carcinogens, environmental pollutants...
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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.
PublicationThe 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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GAS SENSORS WITH TEMPERATURE MODULATION – AN OVERVIEW
PublicationAlthough different methods of improving semiconductor gas sensor properties have been proposed, a technique involving temperature modulation seems to be the most promising. Semiconductor gas sensors working with modulated temperature can be more stable and are more selective comparing with sensor working at one temperature. In this paper, various approaches to temperature modulation are reviewed.
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Determination of the shape of the CFGFT cylindrical column based on laboratory tests
PublicationAnalyses were carried out on glass-fibre-reinforced polymer tube columns with reference to laboratory tests. The angles of the glass fibre beams were 20◦, 55◦ and 85◦. The study employed non-classical operational calculus. Various modulated harmonic signal shapes were considered for columns and tubes at buckling. The buckling loads were assessed and compared for different models.
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Pomiar odpowiedzi impulsowej kanału radiowego na obszarze morskim i przybrzeżnym
PublicationW artykule zaprezentowano wyniki pomiarów odpowiedzi impulsowej kanału radiowego na obszarze morskim i przybrzeżnym. Pomiary przeprowadzono na częstotliwości 1457 MHz a sygnałem sondującym był sygnał o paśmie 10 MHz z modulacją BPSK i pseudoprzypadkową zawartością binarną. Odbierane sygnały były rejestrowane przez dwie stacje ruchome, zainstalowane w samolocie i na łodzi patrolowej. Podczas późniejszej obróbki danych zastosowano...
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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
Publication5-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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A novel method of local chirp-rate estimation of LFM chirp signals in the time-frequency domain
PublicationIn the paper, novel dynamic representations of a complex signal in the time-frequency domain are introduced. The proposed approach is based on using the gradient of the short-time Fourier transform complex phase. A channelized instantaneous complex frequency (CICF) and a complex local group delay (CLGD) are included in the presented signal representations. An application of the newly-introduced distributions is demonstrated by...
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A method for testing the wide-sense stationary uncorrelated scattering assumption fulfillment for an underwater acoustic channel
PublicationWide-sense stationary and uncorrelated scattering (WSSUS) assumptions are often applied for the statistical description of wireless communication channels. However, in the case of underwater acoustic channels the WSSUS model is of limited value. The degree of similarity of in-phase and quadrature components of the channel impulse response, measured with the use of bandpass modulated signals, can be used as an indicator of WSSUS...
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Non-Linear Interaction of Harmonic Waves in a Quasi-Isentropic Flow of Magnetic Gas
PublicationThe diversity of wave modes in the magnetic gas gives rise to a wide variety of nonlinear phenomenaassociated with these modes. We focus on the planar fast and slow magnetosound waves in the geometryof a flow where the wave vector forms an arbitrary angleθwith the equilibrium straight magnetic field.Nonlinear distortions of a modulated signal in the magnetic gas are considered and compared to thatin unmagnetised gas. The case of...
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237Np Mössbauer effect study on NpFeAsO
PublicationWe report 237Np Mössbauer measurements on NpFeAsO. The Np atoms were found to occupy only one crystallographic site. The value of the isomer shift (δ ∼ 9.1 mm s−1 versus NpAl2) indicates a 5f4 electronic configuration (Np3+ ions). The magnetic ordering of the Np sublattice below 60 K is established and the saturated ordered magnetic moment is determined to be 1.73μB at 3.6 K. The unique set of hyperfine parameters exclude a modulated...
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Distance measurement errors in silent FM-CW sonar with matched filtering
PublicationThe secretiveness of sonar operation can be achieved by using continuous frequency-modulated sounding signalswith reduced power and significantly prolonged repeat time. The application of matched filtration in the sonarreceiver provides optimal conditions for detection against the background of white noise and reverberation, and avery good resolution of distance measurements of motionless targets. The article shows that target...
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Biotransformation of abused synthetic cannabinoids, JWH-018 and JWH-073, by human cytochromes P450 and UDP-glucuronosyltransferases
PublicationZwiązki 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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The Imidazoacridinone Antitumor Drug, C-1311, Is Metabolized by Flavin Monooxygenases but Not by Cytochrome P450s.
PublicationPrezentowane w publikacji wyniki badań mają na celu wyjaśnienie roli enzymów wątrobowych w metabolizmie przeciwnowotworowych pochodnych C-1311 oraz C-1330. Oba związki inkubowane były z frakcją mikrosomalną oraz enzymami rekombinantowymi należącymi do grypy cytochromu P450, FMO oraz UGT. Badania wykazały, że oba związki są metabolizowane przez enzymy frakcji mikrosomalnej, ale nie przez enzymy cytochromu P450. Aktywność enzymatyczna...
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Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals
PublicationAntifungal polyene macrolide antibiotics Amphotericin B (AmB) and Nystatin (NYS) were conjugated through the ω-amino acid linkers with diwalled “molecular umbrellas” composed of spermidine-linked deoxycholic or cholic acids. The presence of “umbrella” substituents modulated biological properties of the antibiotics, especially their selective toxicity. Some of the AmB-umbrella conjugates demonstrated antifungal in vitro activity...
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Shallow Water Experiment of OFDM Underwater Acoustic Communications
PublicationThe large variability of communication properties of underwater acoustic channels, and especially the strongly varying instantaneous conditions in shallow waters, is a challenge for the designers of underwater acoustic communication (UAC) systems. The use of phase modulated signals does not allow reliable data transmission through such a tough communication channel. However, orthogonal frequency-division multiplexing (OFDM), being...
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Chirp Rate and Instantaneous Frequency Estimation: Application to Recursive Vertical Synchrosqueezing
PublicationThis letter introduces new chirp rate and instantaneous frequency estimators designed for frequency-modulated signals. These estimators are first investigated from a deterministic point of view, then compared together in terms of statistical efficiency. They are also used to design new recursive versions of the vertically synchrosqueezed short-time Fourier transform, using a previously published method (D. Fourer, F. Auger, and...
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Examining Acoustic Emission of Engineered Ultrasound Loudspeakers
PublicationMeasurement results of the sound emitted from an ultrasound custom-made system with high spatial directivity are presented. The proposed system is using modulated ultrasound waves which demodulate in nonlinear medium resulting in audible sound. The system is aimed at enhancing the users’ personal audio space, therefore the measurements are performed using the Head and Torso Simulator which provides the realistic reproduction of...
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Investigation of the temperature modulation parameters on semiconductor gas sensor response
PublicationIn this work we present the results of the investigation of the sensing properties of semiconductor gas sensors with a sinusoidally modulated temperature in the presence of synthetic air (SA) and three volatile air pollutants, i.e. NH3, NO2 and SO2. The measurements were performed for different average sensor heater temperatures and the amplitude of the modulation signal. In addition, the extraction of features from the sensor...
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Measurements and Simulations of Engineered Ultrasound Loudspeakers
PublicationSimulation and measurement results of the sound emitted from an ultrasound custom-made system with high spatial directivity are presented. The proposed system is using modulated ultrasound waves which demodulate in nonlinear medium resulting in audible sound. The system is aimed at enhancing the users’ personal audio space, therefore the measurements are performed using the Head and Torso Simulator which provides realistic reproduction...
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Digital microcontroller for sonar waveform generator
PublicationGenerating sounding signals is essential for the operation of active sonar. The system should be highly reliable. This can be achieved through architecture, communication between the devices, and a well-designed and self–testing software. The system presented in the article is responsible for the generation of hydroacoustic sounding signals, and ensures proper interaction between power amplifiers and power supplies. Thanks to its...
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Audio codec employing frequency-derived tonality measure
PublicationA transform codec employing efficient algorithm for detection of spectral tonal components is presented. The tonality measure used in MPEG psychoacoustic model is replaced with the method providing adequate tonality estimates even if the tonal components are deeply frequency modulated. The reliability of hearing threshold estimated using psychoacoustic model with standardized tonality measure and the proposed one is investigated...
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Frequency measurement research with weight averaging of pulse output signal of voltage-to-frequency converter
PublicationThe paper presents the essence and investigation of the efficiency of weight averaging of a pulse output signal of voltage-to-frequency converter. The effect of counting and the influence of interference on the result of weight averaging of frequency modulated pulses are analyzed. It is shown that from the point of view of counting error reduction, the best are polynomial weight functions. In the case of high interferences whose...
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New approaches for improving selectivity and sensitivity of resistive gas sensors: A review
PublicationResistive gas sensors are very popular and reliable but suffer from low selectivity and sensitivity. Various methods have been suggested to improve both features without increasing the number of sensors in gas detection systems. Fluctuation enhanced gas sensing was proposed to improve gas detection efficiency by analyzing low-frequency resistance fluctuations, and noise parameters can be more informative than the single DC resistance...
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Company versus consumer performance: does brand community identification foster brand loyalty and the consumer’s personal brand?
PublicationThis study investigates the effect of community identification in building brand loyalty (attitudinal and behavioural) and a personal brand via social networks. The proposed model explained the main community identification antecedents and how identification can lead to enhanced company and consumer performance. This study adopts the theoretical lens of uses and gratifications theory and identifies three motivational drivers of...
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Investigation of the Combustion Processes in the Gas Turbine Module of an FPSO Operating on Associated Gas Conversion Products
PublicationIn this paper, we consider the issue of thermo-chemical heat recovery of waste heat from gas turbine engines for the steam conversion of associated gas for offshore vessels. Current trends in the development of offshore infrastructure are identified, and the composition of power plants for mobile offshore drilling units and FPSO vessels is analyzed. We present the results of a comparison of power-to-volume ratio, power-to-weight...
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Modeling the impact of rotor movement on non-linearity of motor currents waveforms in high-speed PMSM drives
PublicationMotor current measurement techniques as well as predictive control algorithms for electric drives rely on an assumption of linear motor currents changes resulting from constant inverter output voltages. Recent research has reported that this assumption does not hold in motors with short electrical time constant, and in drives whose rotor position advances substantially during a control period. This paper proposes a simulation model...
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Low cost microwave X-band generator
PublicationA low cost microwave X-band generator for educational purposes was designed and built. Its simple construction and user's interface makes it suitable for a student laboratory.The generator is based on a single frequency conversion concept. It uses a digitally tunable PLL chip for intermediate frequency generation and an active frequency multiplier for frequency conversion. The generator covers 9,7 - 11 GHz part of the X frequency...
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Profile irregularities of turned surfaces as a result of machine tool interactions
PublicationThe paper describes the influence of the machining operation on a surface, which disturbs the projection of the tool profile in the form of its relative movements with respect to the object. The elements of the machine tool undergo constant wear during the machining process, it is therefore important to recognize the effects of their influence on the surface's irregularities. Amplitude-frequency analysis of lateral profiles has...
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Study of probe signal bandwidth influence on estimation of coherence bandwidth for underwater acoustic communication channel
PublicationA signal transmitted in a shallow Underwater Acoustic Communication (UAC) channel suffers from time dispersion due to the multipath propagation and the refraction phenomena. This causes intersymbol interference of the received signal and frequency-selective fading observed in its spectrum. Coherence bandwidth is one of the key transmission parameters used for designing the physical layer of a data transmission system to minimise...