Identification of potent P2Y-purinoceptor agonists that are derivatives of adenosine 5'-monophosphate

1. A series of chain-extended 2-thioether derivatives of adenosine monophosphate were synthesized and tested as agonists for activation of the phospholipase C-linked P2Y-purinoceptor of turkey erythrocyte membranes, the adenylyl cyclase-linked P2Y-purinoceptor of C6 rat glioma cells, and the cloned human P2U-receptor stably expressed in 1321N1 human astrocytoma cells. 2. Although adenosine monophosphate itself was not an agonist in the two P2Y-purinoceptor test systems, eleven different 2-thioether-substituted adenosine monophosphate analogues were full agonists. The most potent of these agonists, 2-hexylthio AMP, exhibited an EC50 value of 0.2 nM for activation of the C6 cell receptor. This potency was 16,000 fold greater than that of ATP and was only 10 fold less than the potency of 2-hexylthio ATP in the same system. 2-hexylthio adenosine was inactive. 3. Monophosphate analogues that were the most potent activators of the C6 cell P2Y-purinoceptor were also the most potent activators of the turkey erythrocyte P2Y-purinoceptor. However, agonists were in general more potent at the C6 cell receptor, and potency differences varied between 10 fold and 300 fold between the two receptors. 4. Although 2-thioether derivatives of adenosine monophosphate were potent P2Y-purinoceptor agonists no effect of these analogues on the human P2U-purinoceptor were observed. 5. These results support the view that a single monophosphate is sufficient and necessary for full agonist activity at P2Y-purinoceptors, and provide insight for strategies for development of novel P2Y-purinoceptor agonists of high potency and selectivity.     

Value-based transmission planning and the effects of network models

A value-based automated transmission system planning model is presented in this paper and the impact of the various network representations on the results of the model is discussed. Value-based integrated resource planning provides a “societal cost” (utility operation and investment costs plus customer outage costs) minimizing composite generation-transmission system expansion plan. The model trades-off and compares the costs and benefits of alternative generation and transmission resources using a consistent economic and engineering criterion in order to determine an “optimal” resource expansion plan. The generalized Benders decomposition algorithm with “importance sampling” used to solve the problem enables the model to estimate certain average information about scenarios or contingencies by examining only a very small fraction of all the scenarios or contingencies. The impacts of system resources upon both real and reactive power can be analyzed when using the AC power flow equations. It is concluded that for transmission system planning where reactive power flows and voltage constraints are important, it is imperative that an AC power flow model be used. The combination of AC power flow and linearized power flow models, with linearization about the solution of the AC power flow model, was found to be a promising compromise between accuracy and computation time     

Optimal and Suboptimal Quadriphase Sequences Derived from Maximal Length Sequences over Z _{{\bf 4}}

The paper presents families of quadriphase sequences derived from maximal length sequences over having good correlation properties. These are: (i) families of quadriphase sequences of period from maximal length sequences over ; each family consisting of sequences, (ii) families of quadriphase sequences of period from interleaved maximal length sequences over ; each family consisting of sequences. Such sequences are of interest in quadriphase modulated code division multiple access communication systems, where it is desirable to have large sets of sequences that possess low value of , the maximum magnitude of the periodic crosscorrelation and out of phase auto-correlation values. The sequences over are viewed as trace functions of appropriately chosen unit elements of Galois extension rings of . Quadriphase sequences are then obtained from sequences, by a quadriphase mapping, , from to roots of unity, given by, ; where and . Periodic correlation properties (correlation values and their distribution) of the quadriphase sequences are obtained by using an Abelian association scheme on the elements of the corresponding Galois extension ring of . The majority of the families of sequences derived are optimal with respect to the Welch lower bound on ; the rest being suboptimal with bounded by , where is the period\newpage of the sequences. However nearly half of the sequences in these families are balanced. Received July 18, 1995; revised version November 29, 1996     

Effect of Li<Subscript>2</Subscript>O on the Refractive Index and Optical Band Gap of Cadmium Phosphate Glasses

A series of lithium cadmium phosphate glasses having composition (mol %) xLi₂O-(50 ? x)CdO-50P₂O₅ were prepared in a platinum crucible by the melt quenching technique. The quantity x varies in the range 0–40. The mass density and refractive index of these glasses were found in the ranges 3.95–2.89 g/cm₃ and 1.55–1.40, respectively. The optical absorbance studies were also carried out on these glasses to measure their energy gaps. The absorption spectra of these glasses were recorded in the UV-visible range. No sharp edges were found in the optical spectra, which verifies the amorphous nature of these glasses. The optical band gap energies for these glasses were found to be in the range 2.58–3.5 eV. It was observed that the density, the refractive index, and the optical band gap energy decrease with increasing amount of lithium oxide. The band tailing, worked out from the Urbach plots, shows an increase with increasing Li₂O content and lies in the range 0.47–0.78 eV. The absorption coefficient is observed to show an exponential dependence on the photon energy.     

Removal of partial occlusion from single images

This paper examines large partial occlusions in an image which occur near depth discontinuities when the foreground object is severely out of focus. We model these partial occlusions using matting, with the alpha value determined by the convolution of the blur kernel with a pinhole projection of the occluder. The main contribution is a method for removing the image contribution of the foreground occluder in regions of partial occlusion, which improves the visibility of the background scene. The method consists of three steps. First, the region of complete occlusion is estimated using a curve evolution method. Second, the alpha value at each pixel in the partly occluded region is estimated. Third, the intensity contribution of the foreground occluder is removed in regions of partial occlusion. Experiments demonstrate the method's ability to remove the effects of partial occlusion in single images with minimal user input.     

Towards quality requirements via animated formal specifications

Assuring a high quality requirements specification document involves both an early validation process and an increased level of participation. An approach and its supporting environment which combines the benefits of a formal system specification and its subsequent execution via a rapid prototype is reported. The environment assists in the construction, clarification, validation and visualisation of a formal specification. An illustrative case study demonstrates the consequences of assertions about system properties at this early stage of software development. Our approach involves the pragmatic combination of technical benefits of formal systems engineering based techniques with the context‐sensitive notions of increased participation of both developer and user stakeholders to move us closer towards a quality requirements specification document.     

Magnetron sputtered Dy_2O_3 with chromium and copper contents for antireflective thin films with enhanced absorption

Dy_2O_3 is a rare earth oxide having a number of advanced applications in various fields including protective or antireflective coatings, Main objective of this novel research work is to check the effect of Cr and Cu addition on different properties of Dy_2O_3 and achievement of antireflective thin films with enhanced abso rption. Thin films of these materials we re deposited using DC magnetron with reactive cosputtering. XRD studies reveals the crystalline nature of thin films having Dy_2O_3(222) reflection in all samples with Cr_2O_3(116) and CuO(111) reflections in Cr and Cu containing compositions. Field emission scanning electron microscopy demonstrates the homogeneous deposition of thin films with uniform shape, size and distribution of grains. Refractive index, extinction coefficient and absorption coefficient significantly increase while optical reflectance decreases with Cr and Cu mediation corroborating an improved antireflective mechanism. The imaginary part of dielectric constant is found to increase slightly with low tangent loss for Cr containing composition co nsidered favorable for energy storage applications.     

Study on the preparation and properties of novel block copolymeric materials based on structurally modified organometallic as well as organic polyamides and polydimethylsiloxane

Some novel ferrocene‐containing polyamide‐based block copolymer materials with telechelic polydimethylsiloxane oligomer and their organic analogues were prepared by solution‐phase polycondensation of ferrocene‐based organometallic and terephthaloyl‐ as well as isophthaloyl‐based organic acyl chlorides with a series of semi‐aromatic diamines having ether linkages together with variable aliphatic character. The corresponding polyamides of the synthesized materials, without polydimethylsiloxane segment, were also prepared for comparison of physicochemical properties. None of the synthesized organometallic and organic block copolymers along with their respective polyamides melted below 300 °C and their structural features were confirmed by their physical properties and spectroscopic studies. The weight‐average molecular weights and molecular parameters of all these materials were determined by the static laser light scattering technique. The materials were soluble in sulfuric acid and partially soluble in common organic solvents, and yet became readily soluble upon N‐trifluoroacetylation. The synthesized materials were further characterized by their water absorption characteristics, X‐ray diffraction studies and surface morphology (SEM and AFM) and thermal (DSC and TG) analyses, and their structure–property relationships were elucidated from these studies. The energies of pyrolysis for these materials were calculated by the Horowitz and Metzger method. © 2012 Society of Chemical Industry