Novel selective antagonist radioligands for the pharmacological study of A2B adenosine receptors

The adenosine A2B receptor is the least well characterized of the four adenosine subtypes due to the lack of potent and selective agonists and antagonists. Despite the widespread distribution of A2B receptor mRNA, little information is available with regard to their function. The characterization of A2B receptors, through radioligand binding studies, has been performed, until now, by using low-affinity and non-selective antagonists like 1,3-dipropyl-8-cyclopentylxanthine ([3H]DPCPX),(4-(2-[7-amino-2-(2-furyl)-[1,2,4]triazolo-[2,3-a][1,3,5]triazin-5-ylamino]ethyl)-phenol ([3H]ZM 241385) and 3-(3,4-aminobenzyl)-8-(4-oxyacetate)phenyl-1-propyl-xanthine ([125I]ABOPX). Recently, high-affinity radioligands for A2B receptors, [N-(4-cyanophenyl)-2-[4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)-phenoxy]acetamide ([3H]MRS 1754), N-(2-(2-Phenyl-6-[4-(2,2,3,3-tetratritrio-3-phenylpropyl)-piperazine-1-carbonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-ethyl)-acetamide ([3H]OSIP339391) and N-benzo[1,3]dioxol-5-yl-2-[5-(1,3-dipropyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy]-acetamide] ([3H]MRE 2029F20), have been introduced. This minireview offers an overview of these recently developed radioligands and the most important applications of drugs towards A2B receptors

Oil generation potential of the Permian deposits of Tatarstan based on the content, structure and thermal stability of organic matter in rocks

© SGEM2016.With the use of thermal analysis and Rock-Eval, as well as on the basis of changes in the content and features of the group and the hydrocarbon composition of organic matter in samples of oil and bitumen-containing rocks of Permian deposits in Tatarstan, according to their mineral composition, evaluated the types of hydrocarbon fluids and oil generation potential of the rocks

New 2,6,9-trisubstituted adenines as adenosine receptor antagonists: a preliminary SAR profile

A new series of 2,6,9-trisubstituted adenines (5–14) have been prepared and evaluated in radioligand binding studies for their affinity at the human A1, A2A and A3 adenosine receptors and in adenylyl cyclase experiments for their potency at the human A2B subtype. From this preliminary study the conclusion can be drawn that introduction of bulky chains at the N6 position of 9-propyladenine significantly increased binding affinity at the human A1 and A3 adenosine receptors, while the presence of a chlorine atom at the 2 position resulted in a not univocal effect, depending on the receptor subtype and/or on the substituent present in the N6 position. However, in all cases, the presence in the 2 position of a chlorine atom favoured the interaction with the A2A subtype. These results demonstrated that, although the synthesized compounds were found to be quite inactive at the human A2B subtype, adenine is a useful template for further development of simplified adenosine receptor antagonists with distinct receptor selectivity profiles

Aquathermolysis of High-Viscosity Oil in the Presence of an Oil-Soluble Iron-Based Catalyst

© 2017, Springer Science+Business Media, LLC, part of Springer Nature. A synthetic oil-soluble iron-based catalyst was studied experimentally. A physical model of the catalytic transformation of high-viscosity oil at 200°C was developed. The composition and physicochemical and rheological characteristics of the thermocatalysis products were studied. IR spectroscopy found that the compositions of individual fractions changed. It was shown that the fraction of high-molecular-mass components could be substantially reduced by using the synthetic catalyst in combination with a hydrogen donor. This reduced the viscosity and; therefore, increased the degree of oil extraction

Conversion of Heavy Oil with Different Chemical Compositions under Catalytic Aquathermolysis with an Amphiphilic Fe-Co-Cu Catalyst and Kaolin

© 2018 American Chemical Society. The physical simulation of heavy oil catalytic aquathermolysis with different chemical compositions from deposits located in the Tatarstan Republic, Russia (Ekaterinovsky oil, B2 type, and Olimpiadovsky oil, A1 type), was designed. The catalytic aquathermolysis processes were conducted at a temperature of 300 °C in the presence of a rock-forming additive - kaolin (the content of montmorillonite was 44%), and catalysts composed of transition metal (Fe, Co, and Cu) carboxylates. The environment of the processes was a mixture of carbon dioxide and water vapor. The distinctive features of hydrothermal-catalytic conversion of various oil types are evaluated by fractional, structural-group, microelement compositions, and H:C ratio changes. These variations are due to initial properties of crude oils and the activation degree of destruction reactions on C-C, C-N, C-O, and C-S bonds leading to different levels of increase of saturated fractions content and decrease of resins and asphaltenes content in the products of experiments. By the thermal analysis method, the assessment of potential content of the oil on a solid sorbent before and after experiments was carried out. The high-molecular-weight components of the naphthene-aromatic B2 type oil revealed greater adsorption capacity to the rocks, in comparison with the oil of the A1 type. Therefore, the adsorption of catalyst components on rocks is also greater

Professional-Pedagogical Staff: New Training Techniques

The article deals with the issues of training professional and pedagogical personnel for the system of vocational education, analyzes the methods used to attract teaching staff in the USSR in the 1970s–1980s and in the system of intra-company corporate training in the modern period. Determining potential candidates for involvement in teaching activities in technical schools and colleges of the country, special emphasis is proposed to be placed on employees of industrial enterprises as well as winners and prizewinners of professional skills championships. The involvement of such categories of personnel requires the development of innovative education techniques that allow to eliminate professional deficits in the field of pedagogical and psychological knowledge effectively and in the shortest possible time. The personalized learning model is presented.Рассмотрены вопросы подготовки профессионально-педагогических кадров для системы профессионального образования, проанализированы используемые методы привлечения педагогического персонала в СССР в 1970–1980 гг. и в системе внутрифирменного корпоративного обучения в современный период. При определении потенциальных кандидатов для привлечения к педагогической деятельности в техникумах и колледжах страны особый акцент предлагается делать на работников производственных предприятий, а также победителей и призеров чемпионатов по профессиональному мастерству. Обозначена проблема привлечения таких категорий работников, требующая разработки инновационных образовательных технологий, которые позволяют эффективно и в максимально короткие сроки устранят профессиональные дефициты в области педагогического и психологического знания. Приведена модель персонализированного обучения

Composition and physico-chemical properties of aqueous extracts of lydites of the North Onega synclinorium in Karelia

Relevance. The need to obtain reliable information on chemical composition of aqueous extracts of lydites. There is lack of such information, but it is so important both for understanding dispersion of elements and their impact on natural waters of a region. It is necessary to study the composition of aqueous extracts as a result of water–rock interaction to determine possible sources of water pollution with toxic elements. Mineral composition of lydites of the North Onega synclinorium contains organic carbon and mist pyrite, which may contain increased concentrations of trace elements "harmful" for drinking water. To determine the ability of such elements to pass into a dissolved state, it is necessary to study aqueous extracts of lydites. Aim. To determine trace element composition and physico-chemical properties of aqueous extracts of lydites selected from two districts of the North Onega synclinorium to assess their environmental hazard. Objects. Geological section of the shungite-lidite-dolomite complex of the Zaonezhskaya formation of the Paleoproterozoic age of the North Onega synclinorium. Samples of lidites were taken at the Tetyugino (LT) and Shunga (LSh) sites of the Medvezhyegorsk district of the Republic of Karelia. Methods. Field studies, including investigation of stratigraphic position of lydites in geological sections of the Tetyugino and Shunga sites and sampling, laboratory experiment, aqueous extraction, scanning electron microscopy, Raman spectroscopy, X-ray fluorescence analysis, Inductively Coupled Plasma Mass Spectrometry (ICP-MS). Results. Mineralogical composition of the lydites of both sites is similar. Taking into account high content of SiO2 and negligible content of other petrogenic oxides in chemical composition of lydites, it is possible to consider them as a source for obtaining pure quartz raw materials. The structure of lydites is clot-cryptocrystalline and clot-globular. Lydite extracts environment acidity depends on the totality of the minerals extracted from it, either basic (dolomite) or acidic (pyrite oxidation products). This factor is decisive in formation of chemical composition of lydite extracts, regardless of the location of the samples within a given geological object. Many elements extracted by water from the lydite samples of two regions under consideration are characterized by varying degrees of their extraction from the massive and veined parts of the sample. The cure coefficients of chemical elements in the form of the ratio of element average concentrations in the extract and lydite solid phase show the predominant intake of Cd, Mn, Mo, Sr, Rb, Li, Ni, Co, Li from Tetyugino lydites into water. Mo, Sb and W are predominantly extracted into the solution from the Shunga lydites. Average concentrations of most elements of the extracts of the Shunga samples satisfy the requirements for drinking water and, unlike shungite, they are not sources of harmful components in water. Therefore, it is advisable to carry out work on the possibility of their use for water purification for drinking purposes

Structural changes of heavy oil in the composition of the sandstone in a catalytic and non-catalytic aquathermolysis

© 2016,International Journal of Pharmacy and Technology. All rights reserved.Currently in connection with exhaustion of actively developed resources of light crude and the increasing consumption of energy carriers the development task solution of scavenger oil which will soon become the most important resource of stabilization and increase of oil production is relevant. The share of scavenger oil which,in particular,treatsuperviscous heavy oil steadily grows in overall balance therefore in the next years the gain of oil extraction will be provided at the expense of such naptha. It is accepted to call these resources of hydrocarbons non-conventional as their extraction requires application of the technologies and methods different from traditional methods of light oil production. One of such methods is steam impact on the layer which is characterized by downloading settlement volume of the heat carrier through delivery wells,creation of a thermal fringe and its subsequent advance by not heated water on layer towards production wells. At the same time use of various additional receptions,in particular,forcing of catalytic systems will allow to increase energy efficiency and to intensify process of heavy oil extraction. Relevance of such researches does not raise doubts. In this work the heavy native oil structural changes are studied; they lie in a sample of petrosaturated sandstone of the Volga-Ural province,being impacted by process of catalytic and not catalytic aquathermolysis

Chronotope of Engineering and Pedagogical Thinking

The article is devoted to engineering and pedagogical thinking as a kind of professional thinking that exists due to specific reasons and necessary and sufficient conditions. The “assembly” of these causes and conditions takes place in a certain time-and-place (chronotope), the conceptual reconstruction of which opens the way to overcoming the traditions of haphazard enumerative descriptions of various properties that have developed in the literature and to reaching the construction of the theory of engineering and pedagogical thinking, which, in turn, will help to reasonably update the content and organization of training engineers-teachers, on whom a lot depends in the near technological future of Russia. A review of the characteristics of engineering-pedagogical and related engineering and pedagogical thinking presented in scientific publications is proposed. It shows the need for greater certainty in understanding the nature, foundations, essence and features of heterogeneous engineering and pedagogical thinking. Heterogeneity requires actualization of the potential not only of pedagogy and technical sciences, but also of philosophy, cultural studies, sociology, and psychology. Such actualization shows the heuristic of the communicative interpretation of the nature and essence of thinking. In its light, engineering-pedagogical thinking appears simultaneously as an articulated and unarticulated, discrete and continuous communication of engineers-teachers with students, within which the competencies required by the profession and the impulse developing engineering and technical flair and ingenuity are transmitted, “infecting” (V. Shklovsky2) and charging them, thanks to which communication overcomes the boundaries of the chronotope, gaining continuum features, demonstrating its pulsating situational-suprasituative (corpuscular-wave) dualism. The scientific novelty lies in the justification, by the example of advancing to the theory of engineering and pedagogical thinking, of supplementing the competence approach with consideration of no less significant cultural and subcultural factors, including latent ones, which sometimes manifest themselves in very weak signals about the features of the chronotope of training engineers and technicians by engineers–teachers, not so much by virtue of official regulations as by virtue of singular acts of everyday life communication