维拉唑酮、茚丙林和托舒普兰在神经性疼痛大鼠模型中的镇痛作用。

IF 1.8 Q3 PHARMACOLOGY & PHARMACY Turkish Journal of Pharmaceutical Sciences Pub Date : 2022-06-27 DOI:10.4274/tjps.galenos.2021.41514
Levent Hacısüleyman, Bülent Saraç, Ziad Joha
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引用次数: 1

摘要

目的:抑制血清素、去甲肾上腺素和/或多巴胺再摄取的药物被广泛用于治疗抑郁症,并已成为神经性疼痛的有效药物。它们没有实质性的抗伤害性作用,但与加巴喷丁/普瑞巴林一起被认为是神经性疼痛的一线药物。材料与方法:采用热板法和甩尾法研究3种不同剂量的抗抑郁药对神经性疼痛大鼠模型的抗痛觉作用。它们有不同的作用机制;盐酸维拉唑酮是一种选择性血清素抑制剂和5-HT1A部分激动剂;盐酸托舒普兰是一种选择性去甲肾上腺素抑制剂,它对去甲肾上腺素转运蛋白(NET)有很高的亲和力,而盐酸茚他林是一种三重摄取抑制剂,可抑制5-羟色胺(SERT)、多巴胺(DAT)和NET转运蛋白。结果:与假手术组比较,两组实验中所有药物均有抗痛觉作用。对比三种药物的抗痛觉作用,热板试验发现盐酸托舒普兰的效果明显优于其他两种药物。然而,在摇尾测试中,没有统计学上的显著差异。在甩尾试验中,相同剂量的盐酸茚他林比盐酸维拉唑酮更有效。结论:我们的数据表明,三种药物是神经性疼痛大鼠模型的有效镇痛药,抑制去甲肾上腺素再摄取是有效抗抑郁药镇痛机制的基础。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Analgesic Effects of Vilazodone, Indatraline, and Talsupram in a Rat Model of Neuropathic Pain.

Objectives: Drugs that inhibit the reuptake of serotonin, norepinephrine, and/or dopamine are widely used for treating depressive disorders and have emerged as effective drugs for neuropathic pain. They have no substantial anti-nociceptive effects but are considered, with gabapentin/pregabalin, first-line drugs for neuropathic pain.

Materials and methods: In this study, three different antidepressant agents were used in different doses to investigate their anti-hyperalgesic effects in rat models of neuropathic pain using hot plate and tail flick methods. They have different mechanisms of action; vilazodone hydrochloride is a selective serotonin inhibitor and a 5-HT1A partial agonist; talsupram hydrochloride is a selective noradrenaline inhibitor, and it has a high affinity for noradrenaline transporter (NET), whereas indatraline hydrochloride is a triple reuptake inhibitor that inhibits transporters for 5-HT (SERT), dopamine (DAT), and NET.

Results: All the drugs used in the experiment were found to have an anti-hyperalgesic effect in both tests compared to the sham group. When anti-hyperalgesic effects of the three agents were compared to each other, it was found that talsupram hydrochloride was significantly more effective than the two other drugs in hot plate test. However, there was no statistically significant difference in the tail flick test. Indatraline hydrochloride was more effective than vilazodone hydrochloride at the same doses in the tail flick test.

Conclusion: Our data suggest that three drugs are effective analgesics in rat models of neuropathic pain and inhibition of noradrenaline reuptake represents the cornerstone of analgesic mechanisms of effective antidepressants.

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