A new EPOR/CD131 heteroreceptor agonist EP-11-1: a neuroprotective effect in experimental traumatic brain injury

Q3 Pharmacology, Toxicology and Pharmaceutics Research Results in Pharmacology Pub Date : 2021-10-09 DOI:10.3897/rrpharmacology.7.75301
O. V. Antsiferov, R. F. Cherevatenko, M. Korokin, V. Gureev, A. V. Gureeva, M. Zatolokina, E. V. Avdeyeva, L. A. Zhilinkova, I. Kolesnik
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Abstract

Introduction: EP-11-1 (UEHLERALNSS) is a short-chain erythropoietin derivative without have erythropoietic activity. It was created by modifying a peptide mimicking the spatial structure of the erythropoietin a-helix B pHBSP. One of the promising directions of its administration is the correction of morphofunctional disorders that occur in traumatic brain injury (TBI). Materials and methods: The study was performed in 160 male Wistar rats, weighing 180–200 g.TBI was simulated using the drop-weight method. To assess the emerging morphofunctional disorders and a degree of their correction, we used the severity of neurological deficit, indicators of locomotor activity and exploration, a marker of brain injury S100B and morphological examination. Results and discussion: The combined administration of a new EPOR/CD131 heteroreceptor agonist EP-11-1 with citicoline and trimetazidine led to a more pronounced correction of the neurological deficit when compared not only to the group of the ”untreated” animals, but also to the groups of animals to which these drugs had been administered as monotherapy (p < 0.05). The same tendency was also observed in the study of locomotor activity and exploration. A biochemical study showed that the administration of all three combinations led to a statistically significant (p < 0.05) decrease in the S-100B concentration compared not only to the group of “untreated” animals, but also to the groups of animals to which these drugs had been administered as a monotherapy. Conclusion: The results of the conducted experiments prove the most pronounced positive dynamics in the combined administration of the new EPOR/CD131 heteroreceptor agonist EP-11-1with citicoline and trimetazidine.
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一种新的EPOR/CD131异受体激动剂EP-11-1:实验性创伤性脑损伤的神经保护作用
简介:EP-11-1(UEHLERALNSS)是一种不具有红细胞生成活性的短链红细胞生成素衍生物。它是通过修饰一种模拟红细胞生成素a螺旋B pHBSP空间结构的肽而产生的。其给药的一个有希望的方向是纠正创伤性脑损伤(TBI)中发生的形态功能紊乱。材料和方法:本研究在160只雄性Wistar大鼠中进行,体重180–200 g。采用失重法模拟TBI。为了评估新出现的形态功能障碍及其矫正程度,我们使用了神经功能缺损的严重程度、运动活动和探索指标、脑损伤S100B的标志物和形态学检查。结果和讨论:新的EPOR/CD131异受体激动剂EP-11-1与胞磷胆碱和曲美他嗪的联合给药不仅与“未治疗”动物组相比,但也适用于这些药物作为单一疗法给药的动物组(p<0.05)。在运动活动和探索的研究中也观察到了同样的趋势。一项生物化学研究表明,与“未经治疗”的动物组相比,所有三种组合的给药均导致S-100B浓度显著下降(p<0.05),而且与这些药物作为单一疗法给药的动物组也存在统计学差异。结论:所进行的实验结果证明,新的EPOR/CD131异受体激动剂EP-11-1与胞磷胆碱和曲美他嗪联合给药具有最显著的正动力学。
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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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