The screening study of the effects of several new diethylamino- and dimethylaminoethanol fumaric esters with Krebs cycle intermediates on the physical performance of male mice in the forced swimming test have been conducted. The compounds: Fumarate-DMAE-Fumarate at a dose of 75 mg/kg and Fumarate-DEAE-Succinate at a dose of 10 mg/kg, as well as Diethylaminoethanol (DEAE base) at a dose of 50 mg/kg. The study has shown that their effect on physical performance surpassed the comparison drug, deanol aceglumate, used at the optimal dose of 50 mg/kg. The latter provided a 74% increase in the maximum swimming time of animals, while the studied compounds showed +175%, +162%, +121% results compared to control. The actoprotective activity of the compounds Fumarate-DMAE-Fumarate (75 mg/kg dose) and Fumarate-DEAE-Succinate (FDES) (10 mg/kg dose) is comparable to the effect of ethylthiobenzimidazole hydrochloride (25 mg/kg dose).
The effect of succinic salt of diethylethanolamine fumaric ester on the cognitive abilities of male CBA mice and outbred male rats was studied. It was found that the test substance at doses of 10 and 75 mg/kg in the “Extrapolation escape task” test has a positive effect on the short-term and long-term memory of animals, contributing to the preservation and reproduction of the information received. In the “T-maze” test, the succinic salt of diethylethanolamine fumaric ester in both doses was superior, and in the “Extrapolation escape task” test, it had a comparable effect with the reference drug piracetam (dose 900 mg/kg).
Diethylethanolamine derivative tablets, manufactured by direct compression, do not possess adequate quality attributes. Granulation of excipients makes it possible to improve the fluidity of the mixture and increase the shelf-life of tablets, however the organization of the technological process in production is expensive. Melt extrusion makes it possible to increase the stability of the substance and obtain high-quality tablets with a shelf-life of 2 years. This technological approach is preferred for obtaining granulates from a hygroscopic substance of a diethylethanolamine derivative.
The pathophysiological features of the development of maladjustment under mountain-cold conditions as a manifestation of the syndrome of mutual burdening are considered. In this study, contents of various literary sources, characterizing a persons resistance to the effects of a complex of factors under high mountains and polar zones conditions, were analyzed. With the simultaneous exposure to hypoxia and hypothermia from a pathophysiological point of view, intersecting links of terminological paths, often having diametrically opposite dynamics of changes in the characterized concepts, will be significant. Thus, in the terminological mitochondrial pathway of energy metabolism, uncoupling proteins are present, which, to increase the resistance to hypothermia, should be activated to switch the energy metabolism to predominantly use fatty acids. However, hypoxic conditions should be suppressed to maintain the level of adenosine triphosphate acid available for cells. In the terminological tract of compensatory reactions in response to hypoxemia, the volume of pulmonary ventilation is released, which must increase to improve tolerance to hypoxia, which, under mountain-cold conditions, increased heat loss and promote the deterioration of the condition, i.e., tolerance to low temperatures. Under hypoxic and hypothermic conditions, a synergistic interaction can form, which can be manifested by the development of a syndrome of mutual burdening, which will result in a significant decrease in the functional capabilities of the body, result, and productivity. Maladjustment to mountain cold, with maximum probability, will manifest as disorders of the central nervous system, decreased physical performance, depletion of the functional and regulatory reserves of the body, functional immunodeficiency, decreased regenerative potential, and development of endogenous intoxication. With a high degree of probability, a significant synergistic interaction of hypoxia and hypothermia can be found in relation to the indicators of pulmonary ventilation, blood gases (hypercapnia), acidbase balance (gas alkalosis and lactic acidosis), heart rate (tachycardia), blood pressure (hypotension), central venous pressure (increase), blood viscosity (increase) and its coagulability (hypercoagulation), peroxide and free radical oxidation (activation), and protein catabolism (increase). These changes will negatively affect the functional state of specialists performing complex professional tasks in polar latitudes.
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