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2
3,4-Methylenedioxypyrovalerone prevents while methylone enhances methamphetamine-induced damage to dopamine nerve endings: β-ketoamphetamine modulation of neurotoxicity by the dopamine transporter.3,4-亚甲二氧基吡咯戊酮可预防而甲酮会增强甲基苯丙胺对多巴胺神经末梢的损伤:多巴胺转运体对β-酮苯丙胺神经毒性的调节作用。
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Dopaminergic Effects of Major Bath Salt Constituents 3,4-Methylenedioxypyrovalerone (MDPV), Mephedrone, and Methylone Are Enhanced Following Co-exposure.主要浴盐成分 3,4-亚甲二氧基吡咯戊酮(MDPV)、氯胺酮和甲基酮的多巴胺能效应在共同暴露后增强。
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Psychoactive "bath salts": not so soothing.精神活性“浴盐”:并非那么舒缓。
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Comparative neuropharmacology of three psychostimulant cathinone derivatives: butylone, mephedrone and methylone.三种致幻苯丙胺衍生物:丁基酮、 甲卡西酮和甲基酮的比较神经药理学研究。
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"Polytox" synthetic cathinone abuse: A potential role for organic cation transporter 3 in combined cathinone-induced efflux.“聚毒”合成卡西酮滥用:有机阳离子转运蛋白 3 在联合卡西酮诱导外排中的潜在作用。
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Pharmacokinetics of Synthetic Cathinones Found in Bath Salts in Mouse Brain and Plasma Using High-Pressure Liquid Chromatography-Tandem Mass Spectrometry.使用高压液相色谱-串联质谱法测定浴盐中合成卡西酮在小鼠脑和血浆中的药代动力学
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Metabolites of the ring-substituted stimulants MDMA, methylone and MDPV differentially affect human monoaminergic systems.取代苯丙胺类兴奋剂 MDMA、甲基酮和 MDPV 的代谢物对人单胺能系统有不同的影响。
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Bath salts, mephedrone, and methylenedioxypyrovalerone as emerging illicit drugs that will need targeted therapeutic intervention.浴盐、甲麻黄碱和亚甲基二氧吡咯戊酮作为新兴的非法药物,将需要有针对性的治疗干预。
Adv Pharmacol. 2014;69:581-620. doi: 10.1016/B978-0-12-420118-7.00015-9.

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本文引用的文献

1
Atypical dopamine efflux caused by 3,4-methylenedioxypyrovalerone (MDPV) via the human dopamine transporter.3,4-亚甲基二氧吡咯戊酮(MDPV)通过人多巴胺转运体引起的非典型多巴胺流出。
J Chem Neuroanat. 2017 Oct;83-84:69-74. doi: 10.1016/j.jchemneu.2017.01.004. Epub 2017 Feb 3.
2
Methamphetamine, 3,4-methylenedioxymethamphetamine (MDMA) and 3,4-methylenedioxypyrovalerone (MDPV) induce differential cytotoxic effects in bovine brain microvessel endothelial cells.甲基苯丙胺、3,4-亚甲基二氧甲基苯丙胺(摇头丸)和3,4-亚甲基二氧基吡咯戊酮(MDPV)在牛脑微血管内皮细胞中诱导不同的细胞毒性作用。
Neurosci Lett. 2016 Aug 26;629:125-130. doi: 10.1016/j.neulet.2016.06.029. Epub 2016 Jun 16.
3
Editor's Highlight: Characterization of Hepatotoxicity Mechanisms Triggered by Designer Cathinone Drugs (β-Keto Amphetamines).编辑推荐:新型卡西酮类药物(β-酮基苯丙胺)引发的肝毒性机制的特征分析
Toxicol Sci. 2016 Sep;153(1):89-102. doi: 10.1093/toxsci/kfw105. Epub 2016 Jun 2.
4
3,4-Methylenedioxypyrovalerone (MDPV): in vitro mechanisms of hepatotoxicity under normothermic and hyperthermic conditions.3,4-亚甲二氧基吡咯戊酮(MDPV):在常温及高热条件下的肝毒性的体外机制。
Arch Toxicol. 2016 Aug;90(8):1959-73. doi: 10.1007/s00204-015-1653-z. Epub 2015 Dec 16.
5
Synthetic cathinones and their rewarding and reinforcing effects in rodents.合成卡西酮及其在啮齿动物中的奖赏和强化作用。
Adv Neurosci (Hindawi). 2014 Jun 4;2014:209875. doi: 10.1155/2014/209875.
6
Proactive forensic science: a novel class of cathinone precursors.主动式法医学:一类新型的卡西酮前体。
Forensic Sci Int. 2014 Sep;242:219-227. doi: 10.1016/j.forsciint.2014.06.020. Epub 2014 Jul 5.
7
Awash in a sea of 'bath salts': implications for biomedical research and public health.深陷“浴盐”之海:对生物医学研究和公共卫生的影响
Addiction. 2014 Oct;109(10):1577-9. doi: 10.1111/add.12601. Epub 2014 Jul 1.
8
Bath salts, mephedrone, and methylenedioxypyrovalerone as emerging illicit drugs that will need targeted therapeutic intervention.浴盐、甲麻黄碱和亚甲基二氧吡咯戊酮作为新兴的非法药物,将需要有针对性的治疗干预。
Adv Pharmacol. 2014;69:581-620. doi: 10.1016/B978-0-12-420118-7.00015-9.
9
"Deconstruction" of the abused synthetic cathinone methylenedioxypyrovalerone (MDPV) and an examination of effects at the human dopamine transporter.滥用的合成卡西酮甲撑二氧吡咯戊酮(MDPV)的“解构”及对人多巴胺转运体的作用研究。
ACS Chem Neurosci. 2013 Dec 18;4(12):1524-9. doi: 10.1021/cn4001236. Epub 2013 Oct 31.
10
The mixture of "ecstasy" and its metabolites is toxic to human SH-SY5Y differentiated cells at in vivo relevant concentrations.“摇头丸”及其代谢物混合物在体内相关浓度下对人 SH-SY5Y 分化细胞有毒性。
Arch Toxicol. 2014 Feb;88(2):455-73. doi: 10.1007/s00204-013-1120-7. Epub 2013 Oct 8.

卡西酮邻苯二甲酰亚胺诱导的单胺能毒性:一项体外研究。

Monoaminergic toxicity induced by cathinone phthalimide: An in vitro study.

作者信息

Lantz Susan M, Rosas-Hernandez Hector, Cuevas Elvis, Robinson Bonnie, Rice Kenner C, Fantegrossi William E, Imam Syed Z, Paule Merle G, Ali Syed F

机构信息

Neurochemistry Laboratory, Division of Neurotoxicology, National Center for Toxicological Research/FDA, 3900 NCTR Rd, HFT-132, Jefferson, AR, 72079, United States.

Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, NIDA/NIAAA 9800 Medical Center Drive Rm 228A, MSC-3373, Bethesda, MD, 20892, United States.

出版信息

Neurosci Lett. 2017 Aug 10;655:76-81. doi: 10.1016/j.neulet.2017.06.059. Epub 2017 Jul 3.

DOI:10.1016/j.neulet.2017.06.059
PMID:28684237
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6176714/
Abstract

Bath salts, or synthetic cathinones, have cocaine-like or amphetamine-like properties and induce psychoactive effects via their capacity to modulate serotonin (5-HT) and dopamine (DA). Structurally distinct synthetic cathinones are continuously being generated to skirt existing drug laws. One example of these modified compounds is cathinone phthalimide (CP), which has already appeared on the global market. The lack of toxicological studies on the effects of CP on monoaminergic systems led to the development of the present study in order to generate an acute toxicity profile for CP, and to clarify whether it primarily affects both dopamine and serotonin, like the synthetic cathinones mephedrone and methylone, or primarily affects dopamine, like 3, 4-methylenedioxypyrovalerone (MDPV). For the first time, the toxicity profile of CP (10μM-1000μM) is reported. In pheochromocytoma cells, exposure to CP induced cell death, and altered mitochondrial function, as well as intracellular DA and 5-HT levels; at the same time, reduced glutathione (GSH) levels remained unaffected. This seems to indicate that CP functions like mephedrone or methylone. The role of CP metabolites, the effect of CP induced hyperthermia on neurotoxicity, and its ability to traverse the blood-brain barrier warrant further consideration.

摘要

浴盐,即合成卡西酮,具有类似可卡因或安非他命的特性,并通过调节血清素(5-羟色胺,5-HT)和多巴胺(DA)的能力产生精神活性作用。结构各异的合成卡西酮不断涌现,以规避现行的药品法律。这些经过改良的化合物之一是卡西酮邻苯二甲酰亚胺(CP),它已出现在全球市场上。由于缺乏关于CP对单胺能系统影响的毒理学研究,因此开展了本研究,旨在生成CP的急性毒性概况,并阐明它是否像合成卡西酮甲氧麻黄酮和甲酮那样主要影响多巴胺和血清素,或者像3,4-亚甲基二氧吡咯戊酮(MDPV)那样主要影响多巴胺。首次报告了CP(10μM - 1000μM)的毒性概况。在嗜铬细胞瘤细胞中,暴露于CP会导致细胞死亡,并改变线粒体功能以及细胞内多巴胺和血清素水平;同时,还原型谷胱甘肽(GSH)水平不受影响。这似乎表明CP的作用方式与甲氧麻黄酮或甲酮类似。CP代谢物的作用、CP诱导的体温过高对神经毒性的影响及其穿越血脑屏障的能力值得进一步研究。