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麦角酸二乙胺和 3,4-亚甲基二氧吡咯戊酮(MDPV),“浴盐”的主要成分,对人体多巴胺转运体产生相反的作用。

Mephedrone and methylenedioxypyrovalerone (MDPV), major constituents of "bath salts," produce opposite effects at the human dopamine transporter.

机构信息

Department of Physiology and Biophysics, School of Medicine, Virginia Commonwealth University, Richmond, VA 23298, USA.

出版信息

Psychopharmacology (Berl). 2013 Jun;227(3):493-9. doi: 10.1007/s00213-013-2967-2. Epub 2013 Jan 31.

Abstract

RATIONALE

Psychoactive "bath salts" represent a relatively new drug of abuse combination that was placed in Schedule I in October 2011. Two common ingredients of bath salts include the cathinone analogs: mephedrone and methylenedioxypyrovalerone (MDPV). The mechanism of action of these synthetic cathinone analogs has not been well investigated.

MATERIALS AND METHODS

Because cathinone and methcathinone are known to act as releasing agents at the human dopamine transporter (hDAT), mephedrone and MDPV were investigated at hDAT expressed in Xenopus oocytes.

RESULTS

Whereas mephedrone was found to have the signature of a dopamine-releasing agent similar to methamphetamine or methcathinone, MDPV behaved as a cocaine-like reuptake inhibitor of dopamine.

CONCLUSIONS

Mephedrone and MDPV produce opposite electrophysiological signatures through hDAT expressed in oocytes. Implications are that the combination (as found in bath salts) might produce effects similar to a combination of methamphetamine and cocaine.

摘要

原理

精神活性“浴盐”代表了一种相对较新的滥用药物组合,已于 2011 年 10 月被列入附表 I。浴盐的两种常见成分包括:苯丙胺类似物:甲卡西酮和 3,4-亚甲基二氧吡咯戊酮(MDPV)。这些合成苯丙胺类似物的作用机制尚未得到充分研究。

材料与方法

由于苯丙胺和甲卡西酮已知在人多巴胺转运体(hDAT)上作为释放剂起作用,因此在表达于人卵母细胞中的 hDAT 上研究了甲卡西酮和 MDPV。

结果

尽管发现甲卡西酮具有类似于甲基苯丙胺或甲卡西酮的多巴胺释放剂的特征,但 MDPV 表现为可卡因样多巴胺再摄取抑制剂。

结论

甲卡西酮和 MDPV 通过在卵母细胞中表达的 hDAT 产生相反的电生理特征。这意味着这种组合(如在浴盐中发现的)可能会产生类似于甲基苯丙胺和可卡因的组合的效果。

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