Molecular structure and stereoelectronic properties of sarmazenil--a weak inverse agonist at the omega modulatory sites (benzodiazepine receptors): comparison with bretazenil and flumazenil

X-ray diffraction and ab initio MO theoretical calculations were used in order to investigate the structural and electronic properties of sarmazenil, a weak inverse agonist at the omega modulatory sites (benzodiazepine receptors). This compound was compared to bretazenil, a partial agonist, and to the antagonist flumazenil on the basis of structural and electronic data. The conformational and theoretical properties (interatomic pi overlap populations, molecular electrostatic potential (MEP), the topology of frontier orbitals, and proton affinity) of these three imidazobenzodiazepinones were determined in order to analyse the stereoelectronic properties in relation with their distinct intrinsic efficacies at the omega modulatory sites.     

Non-functional variants of yeast mitochondrial ATP synthase subunit 8 that assemble into the complex

Myocardial and pulmonary beta-adrenoceptors can be imaged with 2-(S)-(-)-(9H-carbazol-4-yl-oxy)-3-[1-(fluoromethyl)ethyl]amino-2- propanol (S-1'-[18F]fluorocarazolol, I). Quantification of unmodified fluorocarazolol in plasma is necessary for analysis of PET images in terms of receptor densities. We have determined I and its radioactive metabolites in rat, sheep and human plasma, using (1) solid-phase extraction (C18) followed by reversed-phase HPLC and (2) direct injection of untreated plasma samples on an internal-surface reversed-phase (ISRP) column. The two methods were in good agreement. Unmodified I decreased from over 99% initially to less than 5%, 5-10% and 20% at 60 min post-injection in rats, sheep and human volunteers, respectively. Protein binding in sheep and human plasma was determined by ultrafiltration. The fraction of total plasma radioactivity bound to protein and the fraction representing unmodified radioligand were linearly correlated, suggesting that fluorocarazolol was more than 70% protein-bound, whereas its metabolites showed negligible protein binding. Direct injection of plasma on an ISRP column seems a convenient method for quantification of lipophilic radioligands such as fluorocarazolol.     

Batch-means control charts for autocorrelated data

Modern statistical process control must often cope with large quantities of highly autocorrelated data. Alwan and Radson (1992) proposed the monitoring of autocorrelated processes by plotting the averages of small batches of data separated by skipping observations. Using results for the AR(1) process, we show that generally better performance can be achieved with no skipping and much larger batch sizes. The resulting batch-means charts derive from methods used in simulation output analysis and can be implemented easily with common digital control systems.     

Sub-optimal solutions to track detection problem using graph theoretic concepts

This paper demonstrates how the problem of tracking targets, which appear as either straight or curved lines in two-dimensional display images (or data images) can be formulated in terms of a directed weighted graph model and how dynamic programming techniques can be efficiently applied to reach an optimal or sub-optimal solution. In general, track detection algorithms providing optimal solutions have good detective ability, but most of them suffer from the inability to detect discontinuous lines or to resolve efficiently pairs of crossing lines. A sub-optimal solution is provided that efficiently overcomes these weaknesses. We focus on modeling the track detection problem in terms of a graph, formulating fast sequential/parallel sub-optimal track detection algorithms and testing them on simulated data in order to show their detective ability. Moreover, we specify the conditions under which sub-optimal algorithms can perform at least as well as their corresponding optimal algorithms. This is significant for the track detection problem where fast, accurate and real-time detection is considered a necessity.     

The TSIMMIS Approach to Mediation: Data Models and Languages

TSIMMIS—The Stanford-IBM Manager of Multiple InformationSources—is a system for integrating information. It offers a datamodel and a common query language that are designed to support thecombining of information from many different sources. It also offerstools for generating automatically the components that are needed tobuild systems for integrating information. In this paper we shalldiscuss the principal architectural features and their rationale.     

A new efficient dcvs circuit synthesis technique used for an improved implementation of a serial/parallel multiplier

This paper describes an efficient technique for the design of fault-secure VLSI circuits based on differential cascode voltage switch (DCVS) logic. We propose a new synthesis method for constructing DCVS circuits with a near-optimal transistor count based on binary decision diagrams (BDDs). the time and memory resources required are very low, making the technique practical even for PC-based synthesis tools. This method is the basis for a CAD tool that allows automatic synthesis of fault-secure circuits based on the DCVS technology. We finally present an improved design and implementation of a 2's complement serial/parallel multiplier as an application of the proposed technique and algorithm.