Study of analgesic activity and effects of new dipharmacophores – nebracetam and cyclooxygenase-2 inhibitors derivatives on the cognitive abilities of rats

Q3 Pharmacology, Toxicology and Pharmaceutics Research Results in Pharmacology Pub Date : 2021-12-16 DOI:10.3897/rrpharmacology.7.78463
V. S. Slyusarenko, I. S. Koklin, S. Kovalenko, V. Chuev, Alexey A. Shabalin, V. Gureev, M. Korokin
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Abstract

Introduction: The aim of the present study was to research the analgesic activity and effect of new dipharmacophore compounds consisting of substances with proven therapeutic activity, namely nebracetam–ibuprofen (NRIP), nebracetam–dexibuprofen (NRDIP), nebracetam–niflumic acid (NRNFA), and nebracetam–mefenamic acid (NRMFA), on the cognitive abilities of rats. Materials and methods: The experimental study was performed in 110 Wistar rats (male/female ratio 50/50%), weighing 180–200 g, and 50 laboratory mice (male/female ratio 50/50%) weighing 18–22 g. The study of the analgesic activity was carried out using the acetic acid writhing test and the hot plate test. The effect on the cognitive abilities of rats was studied using the pattern recognition test in a model of neurotrauma caused by a drop-weight. Results and discussion: It has been shown that the administration of dipharmacophores nebracetam–ibuprofen (NRIP), nebracetam–dexibuprofen (NRDIP), nebracetam–niflumic acid (NRNFA) as well as nebracetam–mefenamic acid (NRMFA) in the tested dosages leads to a statistically significant (p<0.05) analgesic action in acetic acid writhing tests and hot plate tests. At the same time, the analgesic activity of the compounds has been shown to conjoin with a statistically significant influence on cognitive functions in the experimental animal groups after simulating a neurotrauma. Conclusion: The dipharmacophore compounds studied in the present research, having analgesic and nootropic effects, can be used as effective and safe analgesics and can also be used for the treatment and prevention of pain syndrome, enhancing the cognitive abilities of healthy people in complicated professional conditions.
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新型双药效团奈布西坦及环氧化酶-2抑制剂衍生物对大鼠认知能力的影响及镇痛活性研究
前言:本研究的目的是研究由已证实具有治疗活性的物质组成的新型双药效团化合物,即nebracetam-ibuprofen (NRIP)、nebracetam-dexibuprofen (NRDIP)、nebracetam - nifluic acid (NRNFA)和nebracetam - mefinamic acid (NRMFA)对大鼠认知能力的镇痛活性和影响。材料与方法:实验选用Wistar大鼠110只(雌雄比50/50%),体重180-200 g,实验小鼠50只(雌雄比50/50%),体重18-22 g。采用醋酸扭体法和热板法对其镇痛活性进行了研究。采用模式识别试验方法,在落锤损伤大鼠模型上研究了其对认知能力的影响。结果与讨论:在醋酸扭体试验和热板试验中,双药效团纳布拉西坦-布洛芬(NRIP)、纳布拉西坦-地苯洛芬(NRDIP)、纳布拉西坦-尼氟酸(NRNFA)和纳布拉西坦-甲氧胺酸(NRMFA)在试验剂量下的镇痛作用有统计学意义(p<0.05)。同时,在模拟神经损伤后的实验动物组中,化合物的镇痛活性已被证明与统计上显著的认知功能影响相结合。结论:本研究所研究的双药效团化合物具有镇痛和益智作用,可作为安全有效的镇痛药,也可用于治疗和预防复杂职业条件下的疼痛综合征,提高健康人的认知能力。
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来源期刊
Research Results in Pharmacology
Research Results in Pharmacology Medicine-Pharmacology (medical)
CiteScore
1.50
自引率
0.00%
发文量
32
审稿时长
12 weeks
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