New NO-donors with antithrombotic and vasodilating activities, Part 17. Arylazoamidoximes and 3-arylazo-1,2,4-oxadiazol-5-ones

Seven arylazoamidoximes (3), six phenoxycarbonyl derivatives (4), and six 1,2,4-oxadiazol-5-ones (5) have been prepared and their structure and purity established by spectroscopy and elemental analysis. In the EI mass spectra ready elimination of NO from the title amidoximes was observed. A new addition reaction of 3a with hydrochloric acid to 4-chlorophenylhydro-azoamidoxime 7 is described. The compounds were tested for nitric oxide dependent biological properties, i.e. platelet aggregation, antithrombotic effects, and decrease in blood pressure. In arterioles of rats 5/19 compounds inhibited the formation of thrombi with a laser beam by > or = 20% 2 h after oral administration of 60 mg/kg. Among these are three amidoximes (3a, 3e, 3f), one phenoxycarbonyl derivative (4a), and one oxadiazolone (5a). With the 4-chlorophenylazoamidoxime 3c a long lasting (24 h) decrease of blood pressure in spontaneously hypertensive rats was observed. Microsomal fractions of rat liver oxidize arylazoamidoximes and generate nitric oxide (e.g. 3a and 3b). NO was measured by the oxyhemoglobin assay. The influence of SOD, pretreatment of the rats with dexamethasone, as well as kinetic parameters were determined. Type 3 compounds, therefore, are a new class of NO donors. Type 4 and 5 compounds function as their prodrugs.     

Modelling of long-term diffusion–reaction in a bentonite barrier for radioactive waste confinement

Bentonites have been proposed as buffer material for barriers in geological disposal facilities for radioactive waste. This material is expected to fill up by swelling the void between the canisters containing the waste and the surrounding ground. However, the bentonite barriers may be submitted to changes of humidity, temperature variation, fluid interaction, mass transport, etc. This could modify the physico-chemical performance of the barrier, mainly on the interface with the steel container and with the geological barrier. The engineered barrier development necessitates thus the study of the physico-chemical stability of its mineral component as a function of time under the conditions of the repository in the long-term.The purpose of the present study was two-fold. Firstly, it was hoped to simulate the chemical transformations (geochemical and cation exchange reactions) coupled with diffusion of chemical-elements into the engineered barrier under repository conditions by applying a thermokinetic hydrochemical code (KIRMAT: Kinetic Reactions and Mass transport).Secondly, it was hoped to apply a simplified method to estimate the swelling capacity evolution by a volume balance in the fluid-saturated engineered barrier, considering that the decay of swelling capacity is directly proportional on the volume of transformed montmorillonite and, taking into account that it may be partially compensated by the volume of neo-formed swelling clays.The system modelled herein was considered to consist of 1-m thick zone of water-saturated engineered barrier. This non-equilibrated system was placed in contact with a geological fluid on one side, which was then allowed to diffuse into the barrier, while the other side was kept in contact with a source of metallic iron. Reducing initial conditions(P_O2 0; Eh = − 200 mV) and a constant reaction temperature (100 °C) were considered.The results showed that the EB in contact with the geological fluid was highly transformed after 10,000 years, whereas the most significant chemical processes were illitization, cation exchange and saponization, extending up to 20 cm into the EB. Chemical transformations of minor importance in the EB were identified as well, such as a neo-formation of silicates (quartz, cristobalite), anhydrite, laumontite, magnetite and chlorite in the system.A simplified method based on volume balance showed that the swelling capacity of the bentonite barrier is slightly affected after 10,000 years of diffusion–reaction (D close to 1) because the volume of neo-formed swelling-clays is almost directly proportional to the volume of transformed Na/Ca-montmorillonite, except for a strong illitization and/or neo-formation of non-swelling clays. In the present study, this simple approach predicted that the decay of swelling capacity of the engineered barrier is drastically affected close to the geological barrier-engineered barrier interface. Out this zone the swelling capacity decay lies between 5% and 11%.     

Effects of inhibitory amino acids on the frequency components in sympathetic nerve discharge

The effects of the GABA antagonist picrotoxin and the glycine antagonist strychnine on the frequency components in sympathetic inferior cardiac nerve activity were observed. Picrotoxin (0.03-1.0 mg/kg) increased power in the 10-Hz component of sympathetic activity and produced a dramatic shift in the rhythm to higher frequencies. Only small changes were noted in the 2- to 6-Hz component. Strychnine produced a small generalized increase in power in both frequency bands in sympathetic activity. These data suggest that GABA may play an important role in the generation and maintenance of the 10-Hz rhythm in sympathetic activity while glycine likely inhibits activity at a site of convergence of the two rhythms in sympathetic activity.     

Inferring category characteristics from sample characteristics: Inductive reasoning and social projection.

Inductive reasoning involves generalization from sample observations to categories. This research examined the conditions under which generalizations go beyond the boundaries of the sampled categories. In Experiment 1, participants sampled colored chips from urns. When categorization was not salient, participants revised their estimates of the probability of a particular color even in urns they had not sampled. As categorization became more salient, generalization became limited to the sampled urn. In Experiment 2 the salience of categorization in social induction was varied. When social categorization was not salient, participants projected their own responses to test items to members of a laboratory group even when they themselves did to belong to this group. When salience increased, projection decreased among nonmembers but not among members. In Experiment 3 these results were replicated in a field setting. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Bone size and mechanics at the femoral diaphysis across age and sex

The reasons for the increase in fracture rates with age are not fully understood. It is known that there is a decrease in bone mass with a presumed loss of strength. This decrease may possibly be compensated for by changes in cross-sectional geometry. Previous studies, which have been limited by lack of information on subjects' heights and weights, were not able to resolve this issue. In this study, measurements of cross-sectional geometry (area and second moments of area) from 107 specimens of human femoral diaphysis from subjects aged 21-92 years were analysed. Mathematical models of the variation in bone geometry with age were developed. These models included the effects of sex, height and weight. Values of parameters from these models were then used in a biomechanical analysis of the static stresses at the mid-shaft of the femur. Results indicate that although there was a reduction in cortical area in old age, bone tissue was redistributed so that neither bending stresses in the coronal plane nor torsional stresses were higher in old age than in young adulthood. An additional finding was that at any age women had smaller bones, less cortical bone area and higher bone stresses than men. This finding may have some bearing on the higher fracture incidence seen in older women.     

Functional subcaste discrimination (foragers and brood-tenders) in the antCamponotus vagus scop.: polymorphism of cuticular hydrocarbon patterns

In the antCamponotus vagus, when selected foragers that had been earlier removed from the foraging arena and brood-tenders that had been earlier removed from the nest were placed together in a foraging arena, most of the brood-tenders and only a few of the selected foragers were carried back to the nest by nonselected foragers. We hypothesize that cuticular hydrocarbons serve as a cue that allows foragers to discriminate between members of their own subcaste and brood-tenders. It has been established that the proportions of certain hydrocarbons, which are the same regardless of the colony studied, vary from one worker subcaste to another and thus constitute a specific chemical signature. These hydrocarbons belong to a wide range of chemical families (alkanes, monomethylalkanes, and dimethylalkanes). The greatest differences between the two subcastes were observed on the thorax of workers. Principal component analyses performed on the hydrocarbons (or hydrocarbon combinations) corresponding to the 45 main peaks in the cuticular profiles of the head and thorax of brood-tenders and foragers of several colonies show that there exist quantitative differences between the various signatures that characterize the colony, the worker subcastes, and the various body parts within the same species, which can be classified in a hierarchy where the differences between worker subcastes are less pronounced than those between body parts or between colonies.