Resume. It is 41 years in 2018 since Braestrup and Squires opened translocator protein 18 kDa TSPO, known until 2006 as the peripheral benzodiazepine receptor (PBR). The functions of this receptor, which is one of the most important component of the outer mitochondrial membrane, have been studied in detail during this time. One of the key functions of TSPO is the transfer of cholesterol from the outer to the inner membrane of mitochondria, which is the limiting step in the synthesis of neurosteroids. In addition, TSPO is involved in porphyrin transport, mitochondrial respiration, the opening of mitochondrial pores, apoptosis and cell proliferation. This review presents the modern views on the structure of TSPO, the mechanism of it participation in neurosteroidogenesis and the endogenous and synthetic ligands of TSPO. Particular emphasis is placed on the analysis of approaches to the design of synthetic ligands and their neuropsychotropic activity in vitro and in vivo. This review demonstrates the prospects of new neuropsychotic drugs design among TSPO ligands.

Resume. TThe preparation "Antarite” is a combination of magaldrate (antacid of a new generation) with simethicone (antifoam component to reduce flatulence). The antacid effect of the drug develops quickly (1-2 minutes) and lasts for a long time (up to 3 hours). Magaldrat is antacid of multitarget effect, exhibiting a pronounced cytoprotective effect on the gastric mucosa. When the galdrate is dissolved in the hydrochloric acid of the stomach, the crystal structure of this substance causes the formation of tightly packed aluminum hydroxide particles. These particles envelop the area of ulceration, and the size of these particles (2 microns) is such that it facilitates the migration of epithelial cells and fibroblasts in the process of repair of the stomach wall. Additional curative effects of magaldrate are associated with the gradual secretion of magnesium and aluminum ions (hexa-aluminum), which help to maintain optimal concentrations of these ions. The biological effects of aluminum ions are accomplished by activating G-proteins and inhibiting adenylate cyclases. As a result, the metabolism of prostaglandins is modulated, the levels of the vasodilator of nitric oxide (NO) increase, and antihistamine effects are manifested - important components of the multitarget action of magaldrate.

Resume. Actuality. Dimeric dipeptide mimics of the nerve growth factor ( NGF) and brain derived neurotrophic factor (BDNF), respectively GK-2 and GSB-106, were created in the V.V. Zakusov Institute of pharmacology. The similarity of GK-2 and GSB-106 to the corresponding full-sized neurotrophins by the mechanism of action and pharmacological properties, including pronounced neuroprotective activity in vitro and in vivo, has been established. The purpose of this study was to obtain additional data on the cytoprotective properties of GK-2 and GSB-106 using Paramecium caudatum. Methods. Oxidative stress in the Paramecium caudatum was induced by adding heavy metal salts (cadmium chloride, lead acetate, copper sulfate, zinc sulfate) to the medium at a final concentration of 10 |jM. GK-2 or GSB-106 in concentrations from 10^-5 to 10^-8 M was added into the medium with experimental cells 45 minutes before introducing the oxidative stress initiator. Results. Dipeptides GK-2 and GSB-106 in all studied concentrations protected cells from death. The maximum neuroprotective effect of the dipeptides showed in a concentration of 10^-8 M, completely preventing the death of ciliates. Conclusion. GK-2 and GSB-106, at a concentration of 10^-8M, completely protect against the death Paramecium caudatum under conditions of oxidative stress caused by heavy metal salts.

Resume. Lithium ascorbate is a highly digestible and low-toxic lithium salt. In stis study patients with stenosing arteriosclerosis of brachiocephalic arteries were under observation (n = 70, mean age 52 years, 50 % men). In group A (n = 30), participants received standard therapy and lithium ascorbate (0.78 mg/day of elemental lithium, 8 weeks), in group B (n = 40, control) - only the standard therapy. Effects of the lithium ascorbate on the results of neuropsychological testing (Luria's technique, Schulte tables, MMSE and BDI scales, visual-spatial gnosis), levels of BDNF and the levels of trace elements in hair have been established. Lithium ascorbate contributed to a significant improvement in work capacity, mood, a decrease in the proportion of patients with 20 % cerebral stenosis, increased levels of BDNF and a decrease in the levels of toxic trace elements in the hair.

Resume. The results of a studying the pharmacokinetics of the anti-tuberculosis drug Biomayrin in experimental animals (rats) after oral administration were presented. A comparative analysis of the pharmacokinetic parameters of Biomayrin with a comparing drug (a mixture of rifampicin, ethambutol and isoniazid) showed that the bioavailability of isoniazid increased four times as a part of Biomayrin, the ethambutol and rifampicin three times compared to the comparing drug, thereby showing a prolonged effect. It should also be noted that the introduction of isoniazid into the polysaccharide matrix retards its metabolism to the therapeutically inactive acetylisoniazid.

Resume. The article describes the experience of using the immunohistochemical method of analysis with anti-insulin monoclonal antibodies to assess the cytoprotective effect of lithium salts (carbonate and chloride) on pancreatic p-cells. The main advantage of this method over the classical staining methods, which reveal all types of Langerhans' cells, is selective insulin-producing p-cells identification. On the model of streptozotocin-induced type 2 diabetes in Wistar rats, a significant reduction in the p-cells number and a violation of their morphological structure was shown. Both lithium salts are known to be the GSK-3P inhibitors. Our experiments revealed the pronounced cytoprotective activity, consisting in restoring of the insulinocytes' morphological characteristics, increasing the p-cells absolute and relative quantity and the percentage of small and medium-sized islets. A satisfactory correlation between the degree of the lithium salts cytoprotective effect and their hypoglycemic activity has been revealed.