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左旋咪唑给药后赛马体内氨基苯丙胺的形成。合成氨基苯丙胺或左旋咪唑给药与现场氨基苯丙胺阳性样本后的定量和手性分析:初步报告。

The formation of aminorex in racehorses following levamisole administration. A quantitative and chiral analysis following synthetic aminorex or levamisole administration vs. aminorex-positive samples from the field: a preliminary report.

作者信息

Barker S A

机构信息

Department of Comparative Biomedical Sciences, School of Veterinary Medicine, Louisiana State University, Baton Rouge, LA 70803, USA.

出版信息

J Vet Pharmacol Ther. 2009 Apr;32(2):160-6. doi: 10.1111/j.1365-2885.2008.01015.x.

DOI:10.1111/j.1365-2885.2008.01015.x
PMID:19290946
Abstract

Beginning in 2004, the horseracing industry experienced an epidemic of drug positives for the amphetamine-like drug aminorex. Investigation of the therapeutic treatment of the horses called positive for this drug suggested that its source was from the administration of the anthelmintic levamisole. This study examines the urine concentrations of aminorex as a function of time following administration of synthetic, racemic aminorex. Confirmation of the presence of aminorex in urine samples from the horses known to be treated with levamisole is also presented as are data concerning the concentrations of aminorex in positives called from the field and the corresponding concentrations of levamisole found in the same samples. Furthermore, this study illustrates that the chiral isomer distribution of aminorex found in samples from the field is significantly different from that arising from the administration of synthetic, racemic aminorex and is similar to that observed from aminorex arising from levamisole administration. An examination of the chiral isomer distribution of aminorex and a determination of the presence of levamisole in a sample may be used to assess the source of an aminorex positive, distinguishing it from an intentional synthetic, racemic aminorex administration. The role of levamisole in aminorex formation is also discussed.

摘要

从2004年开始,赛马行业出现了类似苯丙胺的药物氨基雷司药物检测呈阳性的流行病。对被检测出该药物呈阳性的马匹的治疗情况进行调查后发现,其来源是驱虫药左旋咪唑的使用。本研究考察了合成消旋氨基雷司给药后,氨基雷司在尿液中的浓度随时间的变化情况。还展示了已知用左旋咪唑治疗的马匹尿液样本中氨基雷司的存在确认情况,以及来自现场检测出阳性的样本中氨基雷司的浓度数据和同一样本中相应的左旋咪唑浓度数据。此外,本研究表明,现场样本中发现的氨基雷司的手性异构体分布与合成消旋氨基雷司给药产生的手性异构体分布显著不同,与左旋咪唑给药产生的氨基雷司的手性异构体分布相似。对氨基雷司的手性异构体分布进行检测以及测定样本中左旋咪唑的存在情况,可用于评估氨基雷司阳性的来源,将其与故意使用合成消旋氨基雷司区分开来。还讨论了左旋咪唑在氨基雷司形成中的作用。

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