U-49900 (3,4-二氯-N-(2-(二乙基氨基)环己基)-N-甲基苯甲酰胺)对成年斑马鱼的镇静作用

T. Kolesnikova, Vadim Shevyrin, S. L. Khatsko, Allan Kalueff
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引用次数: 0

摘要

U-49900 是一种选择性 μ 阿片受体激动剂 U-47700 的化学类似物。尽管包括 U-49900 在内的合成阿片类药物被越来越多地滥用,但人们对其精神药理学和毒理学特征仍然知之甚少。斑马鱼(Danio rerio)是神经科学领域一种前景广阔的模式生物,经常被用于神经刺激药物的精神药理学评估。在此,我们以成年斑马鱼为研究对象,在新型水槽试验中以 1、5、10 和 25 毫克/升(浸水)的剂量对 U-49900 进行了精神药理学评估。浓度为 25 毫克/升、持续 20 分钟的 U-49900 会减少斑马鱼在新水箱试验中的行进距离和顶入次数(与对照组相比,p0.001),但不会改变该试验中的其他参数。总之,斑马鱼对 U-49900 等合成非芬太尼类阿片的敏感性表明,有可能开发出高通量筛选平台,为合成阿片引起的病症找到有效的治疗方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
SEDATIVE EFFECT OF U-49900 (3,4-DICHLORO-N-(2-(DIETHYLAMINO)CYCLOHEXYL)-N-METHYL-BENZAMIDE) IN ADULT ZEBRAFISH
U-49900 is a chemical analogue of a selective μ-opioid receptor agonist U-47700. Despite the growing abuse of synthetic opioids, including U-49900, its psychopharmacological and toxicological profiles remain poorly understood. The zebrafish (Danio rerio) is a promising model organism in neuroscience, and is often used for the psychopharmacological evaluation of neurotropic drugs. The psychopharmacological profile of U-49900 was evaluated here in adult zebrafish at 1, 5, 10 and 25 mg/l (water immersion) tested in the novel tank test. U-49900 at 25 mg/l for 20 min reduces the distance traveled and the number of top entries in the novel tank test (p0.001 vs. control group), but unalters other parameters in this test. Overall, the sensitivity of zebrafish to synthetic non-fentanyl opioids like U-49900 suggests the possibility of developing high-throughput screening platforms for finding effective therapies for pathological conditions caused by synthetic opioids.
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