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二烷基-[2-(1-氧杂-3,4,9-三氮杂-芴-2-基甲氧基)乙基]胺对生物胺的影响:新型潜在抗抑郁药。

Effect of dialkyl- [2-(1-oxa-3,4,9-triaza-fluoren-2-yl-methoxy)ethyl] amines on biogenic amines: new potential antidepressants.

机构信息

University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh, India.

出版信息

Can J Physiol Pharmacol. 2012 Dec;90(12):1585-90. doi: 10.1139/y2012-139. Epub 2012 Nov 26.

DOI:10.1139/y2012-139
PMID:23210437
Abstract

A thorough survey of the literature has revealed that indole derivatives have shown various central nervous system activities. This study aims to evaluate the antidepressant activity of the newly synthesized dialkyl- [2-(1-oxa-3,4,9-triaza-fluoren-2-yl-methoxy)ethyl] amines and their effect on biogenic amines. In this study, the synthesized compounds were assessed by in-vivo antidepressant models, by forced swim test and tail suspension test in mice and effect of synthesized compounds on biogenic amines in brain in a chronic unpredictable stress model. The test compounds have demonstrated significant (P < 0.05) reduced immobility duration in mice when compared with the control group animals. The reduced immobility displayed by mice indicates potential antidepressant activity. In this study, chronic unpredictable stress led to decreased monoamine levels in the cortex and hippocampus regions of the brain. With chronic administration of the investigated compounds there is an increased in monoamines in the brain, in the chronic unpredictable stress model. Decreased levels of monoamines induced by the chronic unpredictable stress induced model of depression, were normalized by treatment with the test compounds, which indicates potential antidepressant activity.

摘要

文献综述表明,吲哚衍生物具有多种中枢神经系统活性。本研究旨在评估新合成的二烷基-[2-(1-氧杂-3,4,9-三氮杂-芴-2-基甲氧基)乙基]胺类化合物的抗抑郁活性及其对生物胺的影响。在这项研究中,通过体内抗抑郁模型,即强迫游泳试验和小鼠悬尾试验,以及合成化合物对慢性不可预测应激模型中脑内生物胺的影响来评估合成化合物。与对照组动物相比,测试化合物显著(P<0.05)降低了小鼠的不动时间。小鼠表现出的不动时间减少表明具有潜在的抗抑郁活性。在这项研究中,慢性不可预测应激导致大脑皮层和海马区的单胺水平降低。在慢性给予研究化合物的情况下,在慢性不可预测应激模型中,大脑中的单胺增加。用测试化合物治疗后,由慢性不可预测应激诱导的抑郁症模型引起的单胺水平降低得到了正常化,这表明具有潜在的抗抑郁活性。

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