THE SEARCH FOR NEUROPROTECTIVE COMPOUNDS AMONG NEW ETHYLTHIADIAZOLE DERIVATIVES

R. F. Cherevatenko, O. V. Antsiferov, S. Skachilova, M. Pokrovsky, V. Gureev, I. I. Banchuk, A. Banchuk, M. I. Golubinskaya, A. A. Syromyatnikova, I. S. Rozhkov, A. A. Mostovykh
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引用次数: 2

Abstract

The aim of the study is to search compounds with neuroprotective properties among new ethylthiadiazole derivatives in simulated traumatic brain injury.Materials and methods. The experiment was carried out on 78 white male rats 270±20 g line “Wistar” 5–6 months of age and 120 outbred sexually mature mice weighing 20±2 grams. The article describes the search for compounds with neuroprotective properties among new ethylthiadiazole derivatives under the codes LKHT 4–15, LKHT 10–18, LKHT 11–18, and LKHT 12–18 in experimental traumatic brain injury in rats. Acute toxicity of the compounds was studied. Pharmacological screening was performed using behavioral and neurological research methods. The McGraw stroke score scale modified by I.V. Gannushkina and the mNSS psychometric scale were used in the study. The open field and Rota-rod tests were used to assess the behavioral status of the animals.Results. The compound-LKHT 12–18 at a dose of 50 mg/kg was detected as a leader. In pharmacological correction of pathology, this compound had the lowest percentage of fatality among the studied compounds (8%), the severity of neurological deficit was significantly reduced, the lowest scores and a higher level of motor activity of the limbs were registered. The number of rearing in the group of animals receiving the compound LKHT 12–18 at the dose of 50 mg/kg increased by 1.5 times, statistically significant (p<0.05) in comparison with the control group. Based on the results of the “Rota-rod” test, the total time of holding animals on the rod for 3 attempts was statistically significantly different in the groups administered with LKHT 12–18 derivatives (1.5 times longer) at the dose of 50 mg/kg compared with the control (p<0.05).Conclusion. Based on the results obtained in this study, it is planned to study in more detail the compound LKHT 12–18 at the dose of 50 mg/kg.
在新的乙基噻二唑衍生物中寻找神经保护化合物
本研究的目的是在新的乙基噻二唑衍生物中寻找具有神经保护作用的化合物,以模拟创伤性脑损伤。材料和方法。实验选用5 ~ 6月龄270±20 g“Wistar”系白种雄性大鼠78只和体重20±2 g的远交性成熟小鼠120只。本文描述了在LKHT 4-15、LKHT 10-18、LKHT 11-18和LKHT 12-18的新乙基噻二唑衍生物中寻找具有神经保护作用的化合物对实验性创伤性脑损伤大鼠的影响。研究了化合物的急性毒性。采用行为学和神经学研究方法进行药理学筛选。采用I.V. Gannushkina改良的McGraw脑卒中评分量表和mNSS心理测量量表。采用空地法和Rota-rod法对大鼠的行为状态进行评价。化合物lkht12 - 18在剂量为50 mg/kg时被检测为先导。在病理药理学校正中,该化合物在所研究的化合物中具有最低的致死率(8%),神经功能缺陷的严重程度显着降低,记录了最低分数和较高水平的肢体运动活动。复方LKHT 12-18 50 mg/kg剂量组的饲养数量比对照组增加了1.5倍,差异有统计学意义(p<0.05)。根据“旋转杆”试验结果,在50 mg/kg剂量下,LKHT 12-18衍生物给药组动物在杆上停留3次的总时间(1.5倍)与对照组相比差异有统计学意义(p<0.05)。根据本研究结果,拟对化合物LKHT 12-18在50 mg/kg剂量下进行更详细的研究。
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