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利帕林 A 在小鼠模型中的抗抑郁活性。

Antidepressant activity of Riparin A in murine model.

机构信息

Department of Biotechnology.

School of Medicine, University of Ribeirão Preto, Ribeirão Preto, Brazil.

出版信息

Behav Pharmacol. 2021 Oct 1;32(7):599-606. doi: 10.1097/FBP.0000000000000654.

Abstract

Depression and anxiety are common neuropsychiatric disorders that usually appear as comorbidities. The development of new drugs is crucial for safer and more effective clinical management of both disorders. Riparin A is a synthetic chemical analog of riparins that naturally occur in several medicinal plants. Marked pharmacological effects such as anxiolytic and antidepressant properties characterize this class of compounds. However, little is known about the potential anxiolytic and antidepressant effects of Riparin A. In this work, we showed that, unlike other riparins, Riparin A exerts only a very mild anxiolytic-like effect as demonstrated by the results of classical behavioral tests such as the elevated plus-maze, light-dark box and open-field tests in rats. However, all doses of Riparin A (2.5; 5.0 and 10 mg/kg; intraperitoneal) have shown significant antidepressant activity in rats submitted to forced swimming test. In addition to this interesting pharmacological property, Riparin A did not promote any important alterations in the locomotor performance of the animals as specifically demonstrated by the rotarod test. Furthermore, Riparin A did not induce sedation in treated animals; instead, this compound appears to increase the animal's state of alertness as measured by the latency time to loss of reflexes and time to recovery from sleep in rats submitted to the pentobarbital-induced sleep time test. The present results point to an antidepressant effect of Riparin A and reinforce the pharmaceutical interest in the group of riparins, particularly their high potential for use in new studies investigating the structure-activity relationships between member compounds.

摘要

抑郁和焦虑是常见的神经精神疾病,通常表现为共病。开发新药对于这两种疾病的安全有效的临床治疗至关重要。Riparin A 是一种天然存在于几种药用植物中的 Riparin 的合成化学类似物。该类化合物具有明显的药理学作用,如抗焦虑和抗抑郁作用。然而,关于 Riparin A 的潜在抗焦虑和抗抑郁作用知之甚少。在这项工作中,我们表明,与其他 Riparin 不同,Riparin A 仅表现出非常温和的类似抗焦虑作用,这可以从经典行为测试(如高架十字迷宫、明暗箱和旷场测试)的结果中得到证明。然而,所有剂量的 Riparin A(2.5;5.0 和 10 mg/kg;腹腔内注射)在强迫游泳试验中均显示出对大鼠的显著抗抑郁活性。除了这种有趣的药理学特性外,Riparin A 没有促进动物的运动表现发生任何重要变化,这可以通过旋转棒测试具体证明。此外,Riparin A 没有在治疗动物中引起镇静作用;相反,与戊巴比妥诱导的睡眠时间试验中大鼠的反射潜伏期和睡眠恢复时间的测量结果一致,该化合物似乎增加了动物的警觉状态。目前的结果表明 Riparin A 具有抗抑郁作用,并增强了人们对 Riparin 组的药物兴趣,特别是它们在研究成员化合物之间的结构-活性关系的新研究中的高应用潜力。

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