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Psychoactive 'bath salts': Not so soothing

机译:具有精神活性的“沐浴盐”:不太舒缓

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Recently there has been a dramatic rise in the abuse of so-called bath salts products that are purchased as legal alternatives to illicit drugs like cocaine and 3,4-methylenedioxymethamphetamine (MDMA). Baths salts contain one or more synthetic derivatives of the naturally-occurring stimulant cathinone. Low doses of bath salts produce euphoria and increase alertness, but high doses or chronic use can cause serious adverse effects such as hallucinations, delirium, hyperthermia and tachycardia. Owing to the risks posed by bath salts, the governments of many countries have made certain cathinones illegal, namely: 4-methylmethcathinone (mephedrone), 3,4-methylenedioxymethcathinone (methylone) and 3,4-methylenedioxypyrovalerone (MDPV). Similar to other psychomotor stimulants, synthetic cathinones target plasma membrane transporters for dopamine (i.e., DAT), norepinephrine (i.e., NET) and serotonin (i.e, SERT). Mephedrone and methylone act as non-selective transporter substrates, thereby stimulating non-exocytotic release of dopamine, norepinephrine and serotonin. By contrast, MDPV acts as a potent blocker at DAT and NET, with little effect at SERT. Administration of mephedrone or methylone to rats increases extracellular concentrations of dopamine and serotonin in the brain, analogous to the effects of MDMA. Not surprisingly, synthetic cathinones elicit locomotor activation in rodents. Stimulation of dopamine transmission by synthetic cathinones predicts a high potential for addiction and may underlie clinical adverse effects. As popular synthetic cathinones are rendered illegal, new replacement cathinones are appearing in the marketplace. More research on the pharmacology and toxicology of abused cathinones is needed to inform public health policy and develop strategies for treating medical consequence of bath salts abuse.
机译:最近,滥用所谓浴盐产品的现象急剧增加,这些产品是可卡因和3,4-亚甲基二氧基甲基苯丙胺(MDMA)等非法药物的合法替代品。浴盐包含一种或多种天然刺激性卡西酮的合成衍生物。低剂量的沐浴盐会产生欣快感,并提高机敏性,但是高剂量或长期使用会导致严重的不利影响,例如幻觉,del妄,体温过高和心动过速。由于沐浴盐带来的风险,许多国家的政府已将某些卡西酮定为非法,即:4-甲基甲卡西酮(甲氧麻黄酮),3,4-亚甲基二氧甲卡西酮(甲酮)和3,4-亚甲基二氧吡咯烷酮(MDPV)。与其他精神运动兴奋剂类似,合成的卡西酮将质膜转运蛋白靶向多巴胺(即DAT),去甲肾上腺素(即NET)和血清素(即SERT)。甲氧麻黄酮和甲酮可作为非选择性转运蛋白底物,从而刺激多巴胺,去甲肾上腺素和5-羟色胺的非胞外释放。相比之下,MDPV在DAT和NET中充当有效的阻止者,而对SERT的影响很小。给大鼠服用甲氧麻黄酮或甲酮会增加脑中多巴胺和5-羟色胺的细胞外浓度,类似于MDMA的作用。毫不奇怪,合成的Cathinones在啮齿动物中引起运动活化。合成卡西酮对多巴胺传播的刺激预示着成瘾的可能性很高,并且可能是临床不良反应的基础。随着流行的合成卡西酮被非法化,新的替代卡西酮正在市场上出现。需要对滥用的卡西酮进行更多的药理学和毒理学研究,以指导公共卫生政策并制定治疗滥用浴盐的医疗后果的策略。

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