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设计型精神兴奋剂:药理学及差异

Designer psychostimulants: pharmacology and differences.

作者信息

Iversen Leslie, White Michael, Treble Ric

机构信息

Department of Pharmacology, University of Oxford, Mansfield Road, OX1 3QT, UK.

Forensic Adviser, Advisory Council on the Misuse of Drugs (ACMD) Secretariat, 2 Marsham Street, London SW1P 4DP, UK.

出版信息

Neuropharmacology. 2014 Dec;87:59-65. doi: 10.1016/j.neuropharm.2014.01.015. Epub 2014 Jan 20.

DOI:10.1016/j.neuropharm.2014.01.015
PMID:24456744
Abstract

More than 200 novel psychoactive drugs have been reported in Europe, with 73 added in 2012 and additional compounds encountered every week in 2013. Many of these are "designer psychostimulants" which aim to mimic the subjective effects of amphetamines, cocaine or 3,4-methylenedioxymethylamphetamine (MDMA; "Ecstasy"). Several drugs are based on the beta-ketoamphetamine cathinone chemical structure, others include aminoindanes, aminotetralins, piperazines, amphetamine analogues and pipradrol derivatives. Although a detailed analysis of the pharmacology of these novel drugs is largely lacking, a number of scientific studies have been reported in 2011-2013 and these are reviewed. All of the novel psychostimulants activate monoamine systems in the brain - with differing dopamine (DA) v serotonin (5-HT) preferences. Those activating principally DA systems are amphetamine-like stimulants, such as naphyrone, desoxypipradrol, 3,4-methylenedioxypyrovalerone (MDPV), and benzylpiperazine while those preferentially activating 5-HT mechanisms are MDMA-like or cocaine-like stimulants, such as mephedrone, methylone and other substituted cathinones, aminoindanes, aminotetralins and piperazines. The ability of mephedrone and other novel psychostimulants to substitute for methylamphetamine or cocaine in drug discrimination tests in rats, and the ability of mephedrone to induce conditioned place preference and to sustain self-administration behaviour suggests that this and other cocaine/methylamphetamine-like drugs have dependence liability. This article is part of the Special Issue entitled 'CNS Stimulants'.

摘要

欧洲已报告了200多种新型精神活性药物,2012年新增73种,2013年每周都会发现更多新化合物。其中许多是“设计型精神兴奋剂”,旨在模拟苯丙胺、可卡因或3,4-亚甲基二氧甲基苯丙胺(摇头丸)的主观效果。几种药物基于β-酮苯丙胺卡西酮化学结构,其他药物包括氨基茚满、氨基四氢萘、哌嗪、苯丙胺类似物和匹哌氮酯衍生物。尽管对这些新型药物的药理学缺乏详细分析,但2011 - 2013年已有一些科学研究报告,本文对此进行综述。所有新型精神兴奋剂都会激活大脑中的单胺系统——对多巴胺(DA)和5-羟色胺(5-HT)的偏好各不相同。主要激活DA系统的是苯丙胺类兴奋剂,如萘黄酮、去氧匹哌氮酯、3,4-亚甲基二氧吡咯戊酮(MDPV)和苄基哌嗪,而优先激活5-HT机制的是摇头丸类或可卡因类兴奋剂(如甲氧麻黄酮、甲烯二氧吡咯戊酮和其他取代卡西酮、氨基茚满、氨基四氢萘和哌嗪)。甲氧麻黄酮和其他新型精神兴奋剂在大鼠药物辨别试验中替代甲基苯丙胺或可卡因的能力,以及甲氧麻黄酮诱导条件性位置偏爱和维持自我给药行为的能力表明,这种药物和其他可卡因/甲基苯丙胺类药物具有成瘾倾向。本文是名为“中枢神经系统兴奋剂”特刊的一部分。

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