54 resultados para Synthetic cannabinoids
Resumo:
A near real-time flood detection algorithm giving a synoptic overview of the extent of flooding in both urban and rural areas, and capable of working during night-time and day-time even if cloud was present, could be a useful tool for operational flood relief management. The paper describes an automatic algorithm using high resolution Synthetic Aperture Radar (SAR) satellite data that builds on existing approaches, including the use of image segmentation techniques prior to object classification to cope with the very large number of pixels in these scenes. Flood detection in urban areas is guided by the flood extent derived in adjacent rural areas. The algorithm assumes that high resolution topographic height data are available for at least the urban areas of the scene, in order that a SAR simulator may be used to estimate areas of radar shadow and layover. The algorithm proved capable of detecting flooding in rural areas using TerraSAR-X with good accuracy, and in urban areas with reasonable accuracy. The accuracy was reduced in urban areas partly because of TerraSAR-X’s restricted visibility of the ground surface due to radar shadow and layover.
Resumo:
Removal of silyl protection from D-glucose derived substrate 6 afforded 7, which upon acetonide deprotection followed by reaction with N-benzylhydroxylamine furnished two isomeric isoxazolidinocyclopentane derivatives via spontaneous cyclization of an in situ generated nitrone. The methyl xanthate derivative of the tertiary hydroxyl group of one isomer was isolated and subjected to radical deoxygenation reaction to form epimeric products, while with the other isomer it underwent spontaneous 1,2-elimination to form a mixture of the two possible endocyclic olefins. Hydrogenolytic cleavage of the isoxazolidine rings of the purified products followed by insertion of 5-amino-4-chloropyrimidine moiety and purine ring construction smoothly afforded structurally unique carbanucleoside analogues. Various spectroscopic methods on the synthesized compounds and X-ray analysis on one important intermediate were used to assign the structures and stereochemistry of the products.
Resumo:
A near real-time flood detection algorithm giving a synoptic overview of the extent of flooding in both urban and rural areas, and capable of working during night-time and day-time even if cloud was present, could be a useful tool for operational flood relief management and flood forecasting. The paper describes an automatic algorithm using high resolution Synthetic Aperture Radar (SAR) satellite data that assumes that high resolution topographic height data are available for at least the urban areas of the scene, in order that a SAR simulator may be used to estimate areas of radar shadow and layover. The algorithm proved capable of detecting flooding in rural areas using TerraSAR-X with good accuracy, and in urban areas with reasonable accuracy.
Resumo:
Abstract: Modulation of presynaptic voltage-dependent Ca+ channels is a major means of controlling neurotransmitter release. The CaV 2.2 Ca2+ channel subunit contains several inhibitory interaction sites for Gβγ subunits, including the amino terminal (NT) and I–II loop. The NT and I–II loop have also been proposed to undergo a G protein-gated inhibitory interaction, whilst the NT itself has also been proposed to suppress CaV 2 channel activity. Here, we investigate the effects of an amino terminal (CaV 2.2[45–55]) ‘NT peptide’ and a I–II loop alpha interaction domain (CaV 2.2[377–393]) ‘AID peptide’ on synaptic transmission, Ca2+ channel activity and G protein modulation in superior cervical ganglion neurones (SCGNs). Presynaptic injection of NT or AID peptide into SCGN synapses inhibited synaptic transmission and also attenuated noradrenaline-induced G protein modulation. In isolated SCGNs, NT and AID peptides reduced whole-cell Ca2+ current amplitude, modified voltage dependence of Ca2+ channel activation and attenuated noradrenaline-induced G protein modulation. Co-application of NT and AID peptide negated inhibitory actions. Together, these data favour direct peptide interaction with presynaptic Ca2+ channels, with effects on current amplitude and gating representing likely mechanisms responsible for inhibition of synaptic transmission. Mutations to residues reported as determinants of Ca2+ channel function within the NT peptide negated inhibitory effects on synaptic transmission, Ca2+ current amplitude and gating and G protein modulation. A mutation within the proposed QXXER motif for G protein modulation did not abolish inhibitory effects of the AID peptide. This study suggests that the CaV 2.2 amino terminal and I–II loop contribute molecular determinants for Ca2+ channel function; the data favour a direct interaction of peptides with Ca2+ channels to inhibit synaptic transmission and attenuate G protein modulation. Non-technical summary: Nerve cells (neurones) in the body communicate with each other by releasing chemicals (neurotransmitters) which act on proteins called receptors. An important group of receptors (called G protein coupled receptors, GPCRs) regulate the release of neurotransmitters by an action on the ion channels that let calcium into the cell. Here, we show for the first time that small peptides based on specific regions of calcium ion channels involved in GPCR signalling can themselves inhibit nerve cell communication. We show that these peptides act directly on calcium channels to make them more difficult to open and thus reduce calcium influx into native neurones. These peptides also reduce GPCR-mediated signalling. This work is important in increasing our knowledge about modulation of the calcium ion channel protein; such knowledge may help in the development of drugs to prevent signalling in pathways such as those involved in pain perception.
Resumo:
Mucosa-mimetic polymeric hydrogels have been developed to replace the use of animal tissues as substrates for characterising mucoadhesive properties of drug delivery systems.
Resumo:
The regio- and stereoselective photoinduced addition of N-carbomethoxymethylpyrrolidine to 5(S)-tert-butyldimethylsiloxymethyl-furan-2(5H)-one in the presence of benzophenone yields 3(R)-[N-(diphenylhydroxymethyl)carbo methoxymethylpyrrolidin-2′-yl]-4(S)-tert-butyldimethylsiloxymethyl)-butan-4-olides (epimeric at C-2′), and we report the X-ray structure of the major adduct together with its conversion into the 1-azabicyclo[4.3.0]-nonane ring system.
Resumo:
A new class of carbon structure is reported, which consists of microscale graphitic shells bounded by curved and faceted planes containing two to five layers. These structures were originally found in a commercial graphite produced by the Acheson process, followed by a purification treatment. The particles, which could be several hundreds of nanometres in size, were frequently decorated with nanoscale carbon particles, or short nanotubes. In some cases, nanotubes were found to be seamlessly connected to the thin shells, indicating that the formation of the shells and that of the nanotubes are intimately connected. The structures are believed to form during a purification process which involves passing an electric current through the graphite in the presence of a reactive gas. In support of this, it is shown that similar particles can be produced in a standard carbon arc apparatus. With their extremely thin graphene walls and high surface areas, the new structures may have a range of useful properties.
Resumo:
A near real-time flood detection algorithm giving a synoptic overview of the extent of flooding in both urban and rural areas, and capable of working during night-time and day-time even if cloud was present, could be a useful tool for operational flood relief management. The paper describes an automatic algorithm using high resolution Synthetic Aperture Radar (SAR) satellite data that builds on existing approaches, including the use of image segmentation techniques prior to object classification to cope with the very large number of pixels in these scenes. Flood detection in urban areas is guided by the flood extent derived in adjacent rural areas. The algorithm assumes that high resolution topographic height data are available for at least the urban areas of the scene, in order that a SAR simulator may be used to estimate areas of radar shadow and layover. The algorithm proved capable of detecting flooding in rural areas using TerraSAR-X with good accuracy, classifying 89% of flooded pixels correctly, with an associated false positive rate of 6%. Of the urban water pixels visible to TerraSAR-X, 75% were correctly detected, with a false positive rate of 24%. If all urban water pixels were considered, including those in shadow and layover regions, these figures fell to 57% and 18% respectively.
Resumo:
The different triplet sequences in high molecular weight aromatic copolyimides comprising pyromellitimide units ("I") flanked by either ether-ketone ("K") or ether-sulfone residues ("S") show different binding strengths for pyrene-based tweezer-molecules. Such molecules bind primarily to the diimide unit through complementary π-π-stacking and hydrogen bonding. However, as shown by the magnitudes of 1H NMR complexation shifts and tweezer-polymer binding constants, the triplet "SIS" binds tweezer-molecules more strongly than "KIS" which in turn bind such molecules more strongly than "KIK". Computational models for tweezer-polymer binding, together with single-crystal X-ray analyses of tweezer-complexes with macrocyclic ether-imides, reveal that the variations in binding strength between the different triplet sequences arise from the different conformational preferences of aromatic rings at diarylketone and diarylsulfone linkages. These preferences determine whether or not chain-folding and secondary π−π-stacking occurs between the arms of the tweezermolecule and the 4,4'-biphenylene units which flank the central diimide residue.
Resumo:
Flood extents caused by fluvial floods in urban and rural areas may be predicted by hydraulic models. Assimilation may be used to correct the model state and improve the estimates of the model parameters or external forcing. One common observation assimilated is the water level at various points along the modelled reach. Distributed water levels may be estimated indirectly along the flood extents in Synthetic Aperture Radar (SAR) images by intersecting the extents with the floodplain topography. It is necessary to select a subset of levels for assimilation because adjacent levels along the flood extent will be strongly correlated. A method for selecting such a subset automatically and in near real-time is described, which would allow the SAR water levels to be used in a forecasting model. The method first selects candidate waterline points in flooded rural areas having low slope. The waterline levels and positions are corrected for the effects of double reflections between the water surface and emergent vegetation at the flood edge. Waterline points are also selected in flooded urban areas away from radar shadow and layover caused by buildings, with levels similar to those in adjacent rural areas. The resulting points are thinned to reduce spatial autocorrelation using a top-down clustering approach. The method was developed using a TerraSAR-X image from a particular case study involving urban and rural flooding. The waterline points extracted proved to be spatially uncorrelated, with levels reasonably similar to those determined manually from aerial photographs, and in good agreement with those of nearby gauges.
Resumo:
Stereoscopic white-light imaging of a large portion of the inner heliosphere has been used to track interplanetary coronal mass ejections. At large elongations from the Sun, the white-light brightness depends on both the local electron density and the efficiency of the Thomson-scattering process. To quantify the effects of the Thomson-scattering geometry, we study an interplanetary shock using forward magnetohydrodynamic simulation and synthetic white-light imaging. Identifiable as an inclined streak of enhanced brightness in a time–elongation map, the travelling shock can be readily imaged by an observer located within a wide range of longitudes in the ecliptic. Different parts of the shock front contribute to the imaged brightness pattern viewed by observers at different longitudes. Moreover, even for an observer located at a fixed longitude, a different part of the shock front will contribute to the imaged brightness at any given time. The observed brightness within each imaging pixel results from a weighted integral along its corresponding ray-path. It is possible to infer the longitudinal location of the shock from the brightness pattern in an optical sky map, based on the east–west asymmetry in its brightness and degree of polarisation. Therefore, measurement of the interplanetary polarised brightness could significantly reduce the ambiguity in performing three-dimensional reconstruction of local electron density from white-light imaging.
Resumo:
New bifunctional pyrazole based ligands of the type [C3HR2N2CONR'] (where R = H or CH3; R' = CH3, C2H5, or (C3H7)-C-i) were prepared and characterized. The coordination chemistry of these ligands with uranyl nitrate and uranyl bis(dibenzoyl methanate) was studied with infrared (IR), H-1 NMR, electrospray-mass spectrometry (ES-MS), elemental analysis, and single crystal X-ray diffraction methods. The structure of compound [UO2(NO3)(2)(C3H3N2CON{C2H5}(2))] (2) shows that the uranium(VI) ion is surrounded by one nitrogen atom and seven oxygen atoms in a hexagonal bipyramidal geometry with the ligand acting as a bidentate chelating ligand and bonds through both the carbamoyl oxygen and pyrazolyl nitrogen atoms. In the structure of [UO2(NO3)(2)(H2O)(2)(C5H7N2CON {C2H5}(2))(2)], (5) the pyrazole figand acts as a second sphere ligand and hydrogen bonds to the water molecules through carbamoyl oxygen and pyrazolyl nitrogen atoms. The structure of [UO2(DBM)(2)C3H3N2CON{C2H5}(2)] (8) (where DBM = C6H5COCHCOC6H5) shows that the pyrazole ligand acts as a monodentate ligand and bonds through the carbamoyl oxygen to the uranyl group. The ES-MS spectra of 2 and 8 show that the ligand is similarly bonded to the metal ion in solution. Ab initio quantum chemical studies show that the steric effect plays the key role in complexation behavior.
Resumo:
Small, synthetic peptides based on specific regions of voltage-gated Ca2+ channels (VGCCs) have been widely used to study Ca2+ channel function and have been instrumental in confirming the contribution of specific amino acid sequences to interactions with putative binding partners. In particular, peptides based on the Ca2+ channel Alpha Interaction Domain (AID) on the intracellular region connecting domains I and II (the I-II loop) and the SYNaptic PRotein INTerction (synprint) site on the II-III loop have been widely used. Emerging evidence suggests that such peptides may themselves possess inherent functionality, a property that may be exploitable for future drug design. Here, we review our recent work using synthetic Ca2+ channel peptides based on sequences within the CaV2.2 amino terminal and I-II loop, originally identified as molecular determinates for G protein modulation, and their effects on VGCC function. These CaV2.2 peptides act as inhibitory modules to decrease Ca2+ influx with direct effects on VGCC gating, ultimately leading to a reduction of synaptic transmission. CaV2.2 peptides also attenuate G protein modulation of VGCCs. Amino acid substitutions generate CaV2.2 peptides with increased or decreased inhibitory effects suggesting that synthetic peptides can be used to further probe VGCC function and, potentially, form the basis for novel therapeutic development.
Resumo:
Flooding is a particular hazard in urban areas worldwide due to the increased risks to life and property in these regions. Synthetic Aperture Radar (SAR) sensors are often used to image flooding because of their all-weather day-night capability, and now possess sufficient resolution to image urban flooding. The flood extents extracted from the images may be used for flood relief management and improved urban flood inundation modelling. A difficulty with using SAR for urban flood detection is that, due to its side-looking nature, substantial areas of urban ground surface may not be visible to the SAR due to radar layover and shadow caused by buildings and taller vegetation. This paper investigates whether urban flooding can be detected in layover regions (where flooding may not normally be apparent) using double scattering between the (possibly flooded) ground surface and the walls of adjacent buildings. The method estimates double scattering strengths using a SAR image in conjunction with a high resolution LiDAR (Light Detection and Ranging) height map of the urban area. A SAR simulator is applied to the LiDAR data to generate maps of layover and shadow, and estimate the positions of double scattering curves in the SAR image. Observations of double scattering strengths were compared to the predictions from an electromagnetic scattering model, for both the case of a single image containing flooding, and a change detection case in which the flooded image was compared to an un-flooded image of the same area acquired with the same radar parameters. The method proved successful in detecting double scattering due to flooding in the single-image case, for which flooded double scattering curves were detected with 100% classification accuracy (albeit using a small sample set) and un-flooded curves with 91% classification accuracy. The same measures of success were achieved using change detection between flooded and un-flooded images. Depending on the particular flooding situation, the method could lead to improved detection of flooding in urban areas.