Synthesis,Pharmacological Evaluation,and Docking Studies of Novel Pyridazinone‐Based Cannabinoid Receptor Type 2 Ligands

In recent years, cannabinoid type 2 receptors (CB₂R) have emerged as promising therapeutic targets in a wide variety of diseases. Selective ligands of CB₂R are devoid of the psychoactive effects typically observed for CB₁R ligands. Based on our recent studies on a class of pyridazinone 4‐carboxamides, further structural modifications of the pyridazinone core were made to better investigate the structure–activity relationships for this promising scaffold with the aim to develop potent CB₂R ligands. In binding assays, two of the new synthesized compounds [6‐(3,4‐dichlorophenyl)‐2‐(4‐fluorobenzyl)‐cis‐N‐(4‐methylcyclohexyl)‐3‐oxo‐2,3‐dihydropyridazine‐4‐carboxamide ( 2 ) and 6‐(4‐chloro‐3‐methylphenyl)‐cis‐N‐(4‐methylcyclohexyl)‐3‐oxo‐2‐pentyl‐2,3‐dihydropyridazine‐4‐carboxamide ( 22 )] showed high CB₂R affinity, with K_i values of 2.1 and 1.6 nm , respectively. In addition, functional assays of these compounds and other new active related derivatives revealed their pharmacological profiles as CB₂R inverse agonists. Compound 22 displayed the highest CB₂R selectivity and potency, presenting a favorable in silico pharmacokinetic profile. Furthermore, a molecular modeling study revealed how 22 produces inverse agonism through blocking the movement of the toggle‐switch residue, W6.48.     

Motion retargeting and evaluation for VR-based training of free motions

Virtual reality (VR) has emerged as one of the important and effective tools for education and training. Most VR-based training systems are situation based, where the trainees are trained for discrete decision making in special situations presented by the VR environments. In contrast, this paper discusses the application of VR to a different class of training, for learning free motion, often required in sports and the arts. We propose a VR-based motion-training framework that contains an intuitive motion-guiding interface, posture-oriented motion retargeting, and an evaluation and advice scheme for corrective feedback. Applications of the proposed framework to simple fencing training and a dance imitation game are demonstrated.     

Filtering for bilinear systems with a lipschitz nonlinearity using LPV approach

This paper deals with the H _?? filtering problem for a class of nonlinear systems. This class of nonlinear systems is composed of a bilinear part and of a lipschitzian one. The use of an unbiasedness condition for the bilinear part (called quasi unbiasedness condition) permits to parameterize the filter matrices through a single gain. Two LPV (Linear Parameter Varying) extensions of the bounded real lemma are used to solve the filtering problem. This approach reduces the conservatism inherent to the boundedness of the inputs. Then the filtering solution is expressed in terms of LMI (Linear Matrix Inequality) to be verified at the vertices of a polytope. A numerical example is finally given to illustrate our approach.     

GearBi: Towards an online arbitration environment based on the design principles simplicity,awareness, orientation,and timeliness

Arbitration is a preferred method for the resolution of international business disputes. As of yet, most publications on online arbitration deal with legal issues. In this paper, we present an Online arbitration environment that we believe facilitates the participants in a meaningful way. Our assumption is that an ODR service should be easy to use (convenient), and at the same time provide meaningful support. More specifically we have paid attention to four criteria that we believe are important, viz. simplicity, awareness, orientation and timeliness. The online arbitration service is called GearBi.     

Performance control for interconnection of identical systems: Application to PLL network design

In this paper, the problem of the control law design for interconnected identical systems ensuring the global stability and the global performance properties is under consideration. Inspired by the decentralized control law design methodology using the dissipativity input–output approach, the problem is reduced to the problem of satisfying two conditions: (i) the condition on the interconnection and (ii) the condition on the local subsystem dynamics. Both problems are efficiently solved applying a (quasi‐) convex LMI optimization and standard H_∞ synthesis. The proposed design methodology is applied to the control law design of a synchronous PLL network. Copyright © 2014 John Wiley & Sons, Ltd.     

An Experimental Economics Investigation of Shipper-carrier Interactions in the Choice of Mode and Shipment Size in Freight Transport

The paper discusses the theoretical and empirical evidence on the subject and concludes that freight mode choice can be best understood as the outcome of interactions between shippers and carriers, and that mode choice depends to a large extent on the shipment size that results from shipper-carrier interactions. These conclusions are supported by economic experiments designed to test the hypothesis of cooperative behavior. This was accomplished by conducting two sets of experiments (ones with the shipper playing the lead role in selecting the shipment size; and others in which the shipment size decision was left to the carriers), and by comparing their results to the ones obtained numerically under the assumption of perfect cooperation. The comparison of results indicated that the experiments converged to the perfect cooperation case. This is in line with the conclusion from game theory that indicates that under typical market conditions the shipper and carrier would cooperate. These results also imply that it really does not matter who “makes” the decision about the shipment size and mode to be used at a given time period, as over time the shipper—that is the customer—ends up selecting the bids more consistent with its own interest. In other words, these results do not support the assumption that freight mode choice is solely made by the carriers.     

INTAMAP: The design and implementation of an interoperable automated interpolation web service

INTAMAP is a Web Processing Service for the automatic spatial interpolation of measured point data. Requirements were (i) using open standards for spatial data such as developed in the context of the Open Geospatial Consortium (OGC), (ii) using a suitable environment for statistical modelling and computation, and (iii) producing an integrated, open source solution. The system couples an open-source Web Processing Service (developed by 52°North), accepting data in the form of standardised XML documents (conforming to the OGC Observations and Measurements standard) with a computing back-end realised in the R statistical environment. The probability distribution of interpolation errors is encoded with UncertML, a markup language designed to encode uncertain data. Automatic interpolation needs to be useful for a wide range of applications and the algorithms have been designed to cope with anisotropy, extreme values, and data with known error distributions. Besides a fully automatic mode, the system can be used with different levels of user control over the interpolation process.     

Augmented reality-based remote coaching for fast-paced physical task

Virtual Reality - One popular application of augmented reality (AR) is the real-time guidance and training in which the AR user receives useful information by a remote expert. For relatively...     

Electrical characterization and modelling of top‐emitting PIN‐OLEDs

Abstract— Positively doped, intrinsic, negatively doped organic light‐emitting diodes (PIN‐OLEDs) have been shown to exhibit high efficiency and a long lifetime compared to conventional small‐molecule OLEDs (SM‐OLEDs). The improved performance of PIN‐OLEDs makes them attractive for use in display applications. Knowledge of the electrical load exhibited by these devices is used to develop an equivalent electrical‐circuit model. Such models are used by circuit designers to assist with the precise design of active‐matrix‐display driver circuits used in such applications. In this paper, the development of a SPICE model for a top‐emitting PIN‐OLED stack is reported.     

The development and maturation of humanitarian psychology.

Humanitarian psychological support as an organized field is relatively young. Pioneers in the field were involved primarily in providing psychological support to refugees and internally displaced persons in conflict and nonconflict situations. This article describes basic principles for the design of psychological support programs and interventions. The International Federation of Red Cross and Red Crescent Societies (IFRC) began a psychological support program in 1991. The IFRC chose psychological first aid as its model for implementation in developing countries. Psychological first aid fits all the principles for psychological support program design and is adapted to individual communities. The first generation of psychological support programs differed dramatically depending on the countries in which they were developed. A second generation of psychological support programs evolved in response to the earthquake/tsunami of December 26, 2004. The Inter-Agency Standing Committee international guidelines consolidated the advances of second-generation programs and provided a clear indication of the wide acceptance of the importance of psychological support. A glimpse is provided of the third generation of psychological support programs, and an admonition is made for a more empirical evaluation of the effectiveness of interventions. (PsycINFO Database Record (c) 2010 APA, all rights reserved)