Azotetrazolylfurazan and Nitrogenous Salt Derivatives

The synthesis of (E)‐1,2‐bis(4‐(1H‐tetrazol‐5‐yl)‐1,2,5‐oxadiazol‐3‐yl)diazene (AzTF) and its high nitrogen salts is described. Compounds were tested for sensitivity to impact, spark, and friction and heats of formation were determined through bomb calorimetry. The calorimetry results coupled with density measurements by gas pychnometry were used to predict explosive output using the Cheetah thermochemical code. Of the four compounds tested AzTF itself has the most promise as an explosive due to TATB‐like performance and high thermal stability, while the triaminoguanidinium salt (TAG₂AzTF) may find favor as a high‐nitrogen gas generant in regard to the low overall sensitivity and very high nitrogen content of the molecule.     

Do small lapses predict relapse to smoking behavior under bupropion treatment?

Although bupropion is known to be an effective aid to smoking cessation, little is known about its mode of action. In the present study we tested the hypothesis that bupropion reduces the likelihood that a smoking lapse, or slip, leads to a subsequent relapse. This hypothesis was tested in the context of a clinical trial of bupropion as a smoking cessation aid, using Cox regression and representing lapse history as a discrete time-varying covariate. Bupropion treatment reduced the probability of relapse during the treatment phase (hazard ratio, or HR=.421, p< or =.000) but not during the follow-up phase (end of treatment to 6 months, HR=.896, p< or=.67). As anticipated, having small lapses during treatment contributed to or predicted subsequent relapse, both during treatment (HR=2.897, p< or =.000) and during follow-up (HR=2.320, p< or=.008). Although an interaction was found between drug treatment and lapse history in predicting subsequent failure during the treatment phase, the finding suggested that drug slightly increased the effect of lapse on eventual failure during treatment (HR=1.706, p相似文献   

Probabilistic model of fatigue fracture of carbon nanostructures

Presented evaluation of risk of fatigue fracture of carbon nanostructures (CN) is based on: (a) the criterion of the threshold of the dissipated energy of tensile stresses, and (b) simulation of stochastic character of fracture by the failures in queueing system. The assessments of probability of fatigue fracture of CN in conditions of uniaxial tension, plane torsion and uniaxial compression are done.     

Yield,development, and weight of Cadra cautella (Walker) and Plodia interpunctella (Hübner) on twenty-one diets derived from natural products

Both Cadra (Ephestia) cautella (Walker) and Plodia interpunctella (Hübner) produced more adult progeny, developed faster, and weighed more when reared in a standard moth medium than in any other of 21 natural product diets. Whole cereals and whole soybeans were poor diets, it being assumed that the hard seed coats prevented the larvae from penetrating to the food. Cracked and ground foods were generally more favorable for growth and development and for production of adult progeny. However, ground peanuts caused the death of the seeding adults and offspring of P. interpunctella and also were very unfavorable for C. cautella.     

Characterization of binding properties to human P-glycoprotein: development of a [3H]verapamil radioligand-binding assay

Interaction with the exsorptive transporter P-glycoprotein (P-gp) is a possible source of peculiarities in drug pharmacokinetics, including dose-dependent absorption, drug-drug interactions, intestinal secretion, and limited permeability of the blood-brain barrier. Among the established in vitro methods of the analysis of drug interactions with P-gp, none directly quantifies the affinity of ligands with P-gp. Instead, they measure the result of a membrane permeation and a receptor-binding process; this may lead to difficulties in the interpretation of results. An assay for quantification of drug affinity to the transporter is presented on the basis of the radioligand-binding assay principle. This has the advantage of directly quantifying the interaction between drugs and P-gp. Because of the reversible and competitive interaction of numerous substrates with P-gp, a radioligand-binding assay was developed by taking [3H]verapamil and [3H]vinblastine as radioligands and the human intestinal Caco-2 cells, overexpressed with P-gp by culturing in the presence of vinblastine or transfecting with multidrug resistance gene MDR-1 as receptor preparation. The assay was performed in 96-well plates and has the potential to be used as a high-throughput method. A clear induction of the expression of P-gp was demonstrated in the Caco-2 cells grown in the presence of vinblastine, as well as in the transfected cells, although to a lesser extent. Both radioligands were shown to bind to P-gp. Verapamil was the radioligand of choice for further investigations due to its lower nonspecific binding to the transporter preparation. Kinetics as well as specificity of the binding of verapamil to the P-gp preparation were demonstrated. A two-affinity model was found to adequately describe the data derived from saturation as well as from competition experiments, in accordance with previous findings on two exsorption sites for P-gp. The binding properties of [3H]verapamil and [3H]vinblastine to a P-gp preparation derived from induced Caco-2 cells are described. The concentration-dependent displacement of the radioligand by nonlabeled substrates for P-gp should be a suitable principle for the determination of drug affinity to the respective binding sites at the human intestinal multidrug transporter P-gp.     

The sympathetic nervous system''s role in regulating blood pressurevariability

This article focuses on how sympathetic nerve activity (SNA) contributes to the variability seen in blood pressure. Specifically, it examines the following questions: why do oscillations occur at certain frequencies, why do only certain frequencies of oscillations in SNA induce oscillations in the vasculature, and what may be the functional purpose of these oscillations