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  • 1
    In: Advances in nano research, Techno-Press, Vol. 4, No. 3 ( 2016-09-25), p. 167-179
    Type of Medium: Online Resource
    ISSN: 2287-237X
    Language: English
    Publisher: Techno-Press
    Publication Date: 2016
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  • 2
    In: Medical academic journal, ECO-Vector LLC, Vol. 19, No. 4 ( 2020-04-03), p. 103-108
    Abstract: Objective. The article is devoted to study the anti-hypoxemic properties of new coumarin derivatives in the models of hypoxemic hypoxia with hypercapnia, hemic hypoxia and histotoxic hypoxia. Materials and methods. Нypoxemic hypoxia with hypercapnia was modeled as follows: mice were placed in hermetic 200 cm3 jars one in a jar. Hemic hypoxia was reproduced in mice by single subcutaneous introduction of sodium nitrite in a dose of 230 mg/kg. Histotoxic hypoxia was caused in mice by intraperitoneal introduction of sodium nitroprusside in a dose of 20 mg/kg. Coumarin derivatives under lab codes IEM-2266 and IEM-2267 were dissolved in distilled water with addition of twin-80, and then a single intraperitoneal infusion of them in doses 25 and 50 mg/kg was made 45 minutes before placing to the model conditions. Increased life time of an animal compared with the control served the criterion of anti-hypoxemic effect of the studied substances. Results. In hypoxemic hypoxia with hypercapnia test compound under IEM-2267 in doses of 25 and 50 mg/kg increased mice life time by 26 and 34% respectively in comparison with control. In hemic hypoxia model, the positive effect was seen with IEM-2266 compound in a dose of 50 mg/kg which increased life time of animals by 45% in comparison with control. In histotoxic hypoxia model, at preventive introduction of IEM-2266 compound in a dose of 25 mg/kg and IEM-2267 in a dose of 50 mg/kg life time increased up to 117% and 123% respectively. Conclusion. The coumarin derivatives IEM-2266 and IEM-2267 relieved the course of acute hypoxia and increased life time of animals in the models of hypoxemic hypoxia with hypercapnia, hemic hypoxia and histotoxic hypoxia.
    Type of Medium: Online Resource
    ISSN: 2687-1378 , 1608-4101
    URL: Issue
    Language: Unknown
    Publisher: ECO-Vector LLC
    Publication Date: 2020
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  • 3
    Online Resource
    Online Resource
    ECO-Vector LLC ; 2020
    In:  Reviews on Clinical Pharmacology and Drug Therapy Vol. 18, No. 1 ( 2020-05-13), p. 37-42
    In: Reviews on Clinical Pharmacology and Drug Therapy, ECO-Vector LLC, Vol. 18, No. 1 ( 2020-05-13), p. 37-42
    Abstract: Introduction. A study of the effects of coumarins has not received widespread use in medicine, largely due to the lack of optimal dosage forms, the creation of which is complicated by their poor solubility in water. Currently, studies are underway on the synthesis of macromolecules, combining various structural fragments, which will lead to increased biological activity of the synthesized coumarin derivatives compared to natural coumarins. The aim of this work was to study the central effect of new coumarin-based compounds: IEM-2262, IEM-2263, IEM-2266, IEM-2267 on emotional and research behavior in rats. Methods. Studies have been carried out using battery of tests that are commonly used to study emotional and exploratory behavior: an open field test and an elevated plus maze in rats. The neuroprotector mexidol (200 mg/kg i.p., Farmasoft, Russia) was used as a reference substance. Results. Coumarins (1050 mg/kg ip) have been shown to have a mild psychotropic, predominantly anti-anxiety and sedative effect. 7-Alkoxycoumarins (IEM-2262 and IEM-2266) and 4-aminocoumarins (IEM-2263 and IEM-2267) have different sensitivity in the open field compared with the effects in the elevated plus maze. Anxiolytic properties appeared in the elevated plus maze after the administration of 4-aminocoumarins (IEM-2263 and IEM-2267). The number of defecation boluses in the open field decreased as a result of the administration of 7-alkoxycoumarins (IEM-2262), which was associated not only with fear of novelty, but to a greater extent with anti-stress action. Thus, the new coumarin derivatives have mild tranquilizing and anti-stress effects and can be used in the future for post-traumatic stress disorders with panic attacks.
    Type of Medium: Online Resource
    ISSN: 2542-1875 , 1683-4100
    URL: Issue
    Language: Unknown
    Publisher: ECO-Vector LLC
    Publication Date: 2020
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  • 4
    Online Resource
    Online Resource
    ECO-Vector LLC ; 2018
    In:  Reviews on Clinical Pharmacology and Drug Therapy Vol. 16, No. 3 ( 2018-12-15), p. 25-31
    In: Reviews on Clinical Pharmacology and Drug Therapy, ECO-Vector LLC, Vol. 16, No. 3 ( 2018-12-15), p. 25-31
    Abstract: Aim. The antihypoxic properties of uridine and uridine-5'-monophosphate (UMP), which are the metabolic precursors of the natural activator of mitochondrial ATP-dependent K+ channels (mitoKATP channels) uridine diphosphat were investigated on the models of hypoxic hypoxia with hypercapnia (HHH), hemic hypoxia and local circulatory hypoxia. Methods. HHH was created in males and females white mice weighing 28-30 g. The animals were placed one by one in hermetically closed container and the duration of their life was determined. The antihypoxic activity of the substances was compared with the reference anthypoxant amtizole (50 mg/kg). Hemic hypoxia was caused in Wistar rats weighing 350-370 g by the injection of sodium nitrite (intramuscularly, 100 mg/kg). Uridine or UMP 30 mg/kg was injected intraperitoneally 30 minutes before the onset of HHH and hemic hypoxia. Local circulatory hypoxia was modeled in male Wistar rats weighing 250-300 g. Acute coronary occlusion lasting 60 min was reproduced by legation of descending branch of the left coronary artery (LCA). Uridine or UMP (30 mg/kg) was administered intravenously 5 minutes prior to LCA occlusion. Selective blocker of mitoKATP channels 5-hydroxydecanoate (5 mg/kg, intravenously, 5 minutes prior uridine or UMP) was used to determine the role of these channels in the mechanism of antihypoxic action of the studied drugs. The volume of the damaged myocardium was used as the marker of antihypoxic activity of uridine and UMP. Results. Different resistance to hypoxia in female and male mice was observed in HHH. The female mice were more resistant, their life duration was 43% more than the males. Uridine and UMP displayed antihypoxic activity only in male mice, increasing their life duration by 25% and 20% respectively. This effect was 2 times less than that of amtisol. In similar conditions in females mice the preparations did not show a protective effect. In hemic hypoxia the life duration of rats treated with uridine and UMP did not differ from the control values. Circulatory hypoxia, caused by occlusion of the LCA, led to the formation of a local zone of myocardial damage. Uridine or UMP decreased the damage zone in 2 and 3,5 times respectively. The inhibitor of mitoKATP channels blocked the protective effect of these compounds. Conclusion. Uridine and UMP have a distinct antihypoxic effect in HHH and a marked protective effect in local circulatory hypoxia. The antihypoxic activity of druges in HHH is manifested differently in female and male mice. It may be due to sexual differences in the resistance to hypoxia. The maximum effect is observed in male who have initially low resistance to oxygen deficiency. The mechanism of the protective action of uridine and UMP in the circulatory hypoxia is associated with the activation of mitoKATP channels.
    Type of Medium: Online Resource
    ISSN: 2542-1875 , 1683-4100
    URL: Issue
    Language: Unknown
    Publisher: ECO-Vector LLC
    Publication Date: 2018
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