一些哌啶衍生物的合成和抗抑郁活性:单胺和阿片能系统的参与

IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Acta poloniae pharmaceutica Pub Date : 2022-11-21 DOI:10.32383/appdr/152631
Ceren Kaya, Nazlı Turan Yücel, Ümmühan Kandemir, Derya Osmaniye, Ö. Can, Ümide Demir Özkay
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引用次数: 0

摘要

本研究旨在合成一些新的哌啶类衍生物并研究其抗抑郁活性。目的化合物是由1-(4-(取代胡椒碱-1-基)苯基)乙二酮和杂环醛在甲醇中反应得到的。利用各种光谱方法(IR, 1H-NMR, 13C-NMR和LCMSMS)确定了合成化合物的结构。通过悬尾和改良强迫游泳试验(MFST)测试化合物(50 mg/kg)的抗抑郁样作用。此外,通过活动笼测量评估小鼠运动活动可能发生的变化。得到的结果表明,化合物2c-2f在两种抗抑郁活性筛选试验中都减少了小鼠的静止时间,表明这些衍生物具有抗抑郁样作用。此外,在MFST中,化合物2c和2e显著增加了游泳次数,而化合物2d和2f显著延长了攀爬时间。对氯苯丙氨酸甲酯(5 -羟色胺消耗剂)预处理可逆转化合物2c和2e的抗抑郁样作用,而α-甲基对酪氨酸甲酯(儿茶酚胺消耗剂)预处理可消除化合物2d和2f的抗抑郁样作用。此外,纳洛酮预处理逆转了这四种衍生物的抗抑郁样作用。所得结果表明,单胺和阿片能系统介导了我们的新型哌啶衍生物的抗抑郁作用。
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Synthesis and antidepressant-like activities of some piperidine derivatives: involvements of monoaminergic and opiodergic systems
It was aimed to synthesize some novel piperidine derivatives and investigate their antidepressant-like activities, in this study. Targeted compounds were obtained by reacting 1-(4-(substitutedpiperidin-1-yl)phenyl)ethan-1-one and heterocyclic aldehydes in methanol. The structures of the synthesized compounds were determined using data from various spectroscopic methods (IR, 1H-NMR, 13C-NMR, and LCMSMS). The compounds (50 mg/kg) were tested for their antidepressant-like effects by tail suspension and modified forced swimming tests (MFST). In addition, possible alterations in locomotor activities of mice were evaluated by activity cage measurements. Obtained results showed that compounds 2c-2f reduced the immobility time of mice in both of the antidepressant activity-screening tests indicating that these derivatives have antidepressant-like effects. Moreover, in MFST, compounds 2c and 2e significantly increased the swimming times, while compounds 2d and 2f significantly prolonged the climbing durations. Antidepressant-like effects of the compounds 2c and 2e was reversed with p-chlorophenylalanine methyl ester (serotonin depleting agent) pre-treatments while the same effect caused by the compounds 2d and 2f was abolished by pretreatment with α-methyl-para-tyrosine methyl ester (catecholamine depleting agent) pre-administrations. Moreover, pre-treatment with naloxone reversed the antidepressant-like effects of these four derivatives. Obtained results indicated that monoaminergic and opioidergic systems mediated the antidepressant-like effects of our novel piperidine derivatives.
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来源期刊
CiteScore
0.80
自引率
0.00%
发文量
74
审稿时长
6-12 weeks
期刊介绍: The international journal of the Polish Pharmaceutical Society is published in 6 issues a year. The journal offers Open Access publication of original research papers, short communications and reviews written in English, in all areas of pharmaceutical sciences. The following areas of pharmaceutical sciences are covered: Analysis, Biopharmacy, Drug Biochemistry, Drug Synthesis, Natural Drugs, Pharmaceutical Technology, Pharmacology and General. A bimonthly appearing in English since 1994, which continues “Acta Poloniae Pharmaceutica”, whose first issue appeared in December 1937. The war halted the activity of the journal’s creators. Issuance of “Acta Poloniae Pharmaceutica” was resumed in 1947. From 1947 the journal appeared irregularly, initially as a quarterly, then a bimonthly. In the years 1963 – 1973 alongside the Polish version appeared the English edition of the journal. Starting from 1974 only works in English are published in the journal. Since 1995 the journal has been appearing very regularly in two-month intervals (six books a year). The journal publishes original works from all fields of pharmacy, summaries of postdoctoral dissertations and laboratory notes.
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