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叔丁基 4-((1-苯基-1H-吡唑-4-基)甲基)哌嗪-1-羧酸酯(LQFM104)-一种具有抗焦虑和抗抑郁样作用的新型哌嗪衍生物:5-羟色胺能系统的推测作用。

Tert-butyl 4-((1-phenyl-1H-pyrazol-4-yl) methyl) piperazine-1-carboxylate (LQFM104)- New piperazine derivative with antianxiety and antidepressant-like effects: Putative role of serotonergic system.

机构信息

Department of Pharmacology, Institute of Biological Sciences, Federal University of Goiás, Goiânia, GO, Brazil.

Chemistry Institute, Laboratory of Chromatography and Mass Spectrometry, Federal University of Goiás, Goiânia, GO, Brazil.

出版信息

Biomed Pharmacother. 2018 Jul;103:546-552. doi: 10.1016/j.biopha.2018.04.077. Epub 2018 Apr 24.

DOI:10.1016/j.biopha.2018.04.077
PMID:29677541
Abstract

The piperazine derivatives correspond to an extensive chemical class of compounds with numerous neuropharmacological activities, including antidepressant (e.g., nefazodone, trazodone) and anxiolytic (e.g., buspirone) properties. Therefore, aiming to identify a new antidepressant and antianxiety lead-compound, our group designed, synthesized, and investigated the effects of a new piperazine compound, namely, LQFM104, on the behavior of mice. Male albino Swiss mice were treated with LQFM104 prior to predictive behavioral tests as open field (OFT), elevated plus maze (EPM), forced swimming (FST), and tail suspension tests (TST). The participation of the serotonergic system was evaluated by pretreatment with a 5-HT1A antagonist receptor (WAY100635) and serotonin (5-HT) synthesis inhibitor (p-chlorphenylalanine, pCPA) before oral administration of LQFM104 and behavioral tests. The treatment with LQFM104 did not interfere with locomotor activity but revealed suggestive data of anxiolytic-like effects by the increase in the time spent in the center of the OFT. This activity was confirmed by the results obtained in the EPM, and it was abolished after pretreatment with WAY100635 and pCPA. The immobility time decreased in both the FST and TST. The antidepressant-like activity was completely abolished after WAY100635 pretreatment. Altogether, these data revealed that LQFM104 possesses anxiolytic and antidepressant-like properties in behavioral tests on mice, and these activities are possibly mediated, directly and/or indirectly, by serotonergic pathways.

摘要

哌嗪衍生物属于广泛的化学类化合物,具有许多神经药理学活性,包括抗抑郁(如奈法唑酮、曲唑酮)和抗焦虑(如丁螺环酮)特性。因此,为了寻找一种新的抗抑郁和抗焦虑先导化合物,我们小组设计、合成并研究了一种新的哌嗪化合物 LQFM104 对小鼠行为的影响。雄性白化瑞士小鼠在进行预测性行为测试(如旷场测试、高架十字迷宫测试、强迫游泳测试和悬尾测试)之前,用 LQFM104 进行预处理。通过在口服 LQFM104 之前用 5-HT1A 拮抗剂受体(WAY100635)和 5-HT 合成抑制剂(对氯苯丙氨酸,pCPA)预处理,评估了 5-HT 能系统的参与。LQFM104 的治疗并未干扰运动活动,但在旷场测试的中心停留时间增加方面显示出类似抗焦虑的效果。这一活动在高架十字迷宫测试中得到了证实,并且在 WAY100635 和 pCPA 预处理后被消除。在强迫游泳测试和悬尾测试中,不动时间减少。在 WAY100635 预处理后,抗抑郁样活性完全被消除。总的来说,这些数据表明 LQFM104 在小鼠行为测试中具有抗焦虑和抗抑郁样特性,这些活性可能直接和/或间接通过 5-HT 能途径介导。

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