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GC-MS 和 LC-HR-MS/MS 研究设计药物β-萘基哌啶在大鼠尿液中的代谢和检测。

Studies on the metabolism and detectability of the designer drug β-naphyrone in rat urine using GC-MS and LC-HR-MS/MS.

机构信息

Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical, Pharmacology and Toxicology, Saarland University, D-66421, Homburg, Saar, Germany.

出版信息

Drug Test Anal. 2013 Apr;5(4):259-65. doi: 10.1002/dta.1443. Epub 2013 Jan 10.

DOI:10.1002/dta.1443
PMID:23303532
Abstract

Naphyrone (1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one; naphthylpyrovalerone, β-naphyrone) is a cathinone designer drug and was marketed as replacement for the synthetic cathinone derivative mephedrone. Meanwhile, naphyrone is also classified as a controlled drug in several countries. Therefore, the aim of this study was to identify the metabolites of naphyrone in rat urine using gas chromatography-mass spectrometry techniques and to show its detectability in urine samples. The following metabolic steps could be detected in rat urine: oxidation of the pyrrolidine ring to the corresponding lactam, hydroxylation of the propyl side chain and the naphthyl ring, degradation to the primary amines after opening of the pyrrolidine ring, and combinations of these steps. Assuming similar kinetics, an intake of naphyrone should be detectable in human urine mainly via its metabolites.

摘要

萘基吡咯烷酮(1-萘-2-基-2-吡咯烷-1-基-戊烷-1-酮;萘基丙基戊酮,β-萘基吡咯烷酮)是一种苯丙胺类兴奋剂,曾被作为合成苯丙胺衍生物甲卡西酮的替代品进行销售。同时,萘基吡咯烷酮在多个国家也被列为管制药物。因此,本研究旨在使用气相色谱-质谱联用技术鉴定大鼠尿液中的萘基吡咯烷酮代谢物,并展示其在尿液样本中的可检测性。在大鼠尿液中可以检测到以下代谢步骤:吡咯烷环氧化生成相应的内酰胺、丙基侧链和萘基环的羟化、吡咯烷环打开后生成伯胺,以及这些步骤的组合。假设动力学相似,萘基吡咯烷酮的摄入应该可以通过其代谢物在人体尿液中检测到。

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