首页|苯乙胺类新精神活性物质2C-B-FLY和25B-NBOH的体外代谢研究

苯乙胺类新精神活性物质2C-B-FLY和25B-NBOH的体外代谢研究

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目的 探究苯乙胺类新精神活性物质 2C-B-FLY和 25B-NBOH在人肝微粒体中的体外代谢产物及代谢途径.方法 建立人肝微粒体孵育模型,样品在 37℃水浴共孵育 3 h后离心、吹干、复溶,用超高效液相色谱-Q Exactive质谱ESI+模式对样品进行检测,运用Full scan-ddMS2 数据依赖型采集模式对母药及其代谢产物进行检测.结果 经人肝微粒体体外孵育实验,2C-B-FLY经代谢共产生 4 种I相代谢物和 1 种乙酰化的II相代谢物,发生了羟基化、去溴化、N-乙酰化等代谢反应.25B-NBOH经代谢共产生8种I相代谢物和2种葡萄糖醛酸化的II相代谢物,包括的主要生物转化反应为O-去甲基化、羟基化、胺基脱氢、N-脱烷基化和葡萄糖醛酸化.结论 本研究阐述了2C-B-FLY和 25B-NBOH在人肝微粒体孵育体系中的代谢产物及代谢途径,为苯乙胺类新精神活性物质的体内检测提供科学依据.
Study on metabolism of phenethylamines new psychoactive substances 2C-B-FLY and 25B-NBOH in vitro
Objective To investigate the in vitro metabolites and metabolic pathways of phenethylamine new psychoactive substances 2C-B-FLY and 25B-NBOH in human liver microsomes.Methods The human liver microsome incubation model was established,and the samples were centrifuged,blow-dried and re-dissolved after 3 h of co-incubation in a water bath at 37℃.The samples were detected by ultra-high performance liquid chromatography Q Exactive mass spectrometry in ESI+mode,and the parent drug and its metabolites were examined by applying Full scan-ddMS2 data-dependent acquisition mode.Results After in vitro incubation with human liver microsomes,2C-B-FLY was metabolised to produce a total of four phase I metabolites and one acetylated phase II metabolite,which underwent metabolic reactions such as hydroxylation,debromination,and N-acetylation.25B-NBOH was metabolised to produce a total of eight phase I metabolites and two glucuronidated phase II metabolites,which comprised the major biotransformation reactions of O-demethylation,hydroxylation,amine dehydrogenation,N-dealkylation and glucuronidation.Conclusion This study describes the metabolites and metabolic pathways of 2C-B-FLY and 25B-NBOH in a human liver microsomal incubation system,providing a scientific basis for the in vivo detection of new psychoactive substance of the phenethylamine group.

New psychoactive substance2C-B-FLY25B-NBOHMetabolites in vitroMetabolic pathway

施妍、翟文娅、王鑫、阳硕、吴何坚

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司法鉴定科学研究院 上海市法医学重点实验室 上海市司法鉴定专业技术服务平台司法部司法鉴定重点实验室,上海 200063

新精神活性物质 2C-B-FLY 25B-NBOH 体外代谢产物 代谢途径

"十四五"国家重点研发计划资助项目国家自然科学基金司法部司法鉴定重点实验室资助项目上海市法医学重点实验室项目上海市司法鉴定专业技术服务平台资助项目

2022YFC33020038227193221DZ2270800

2024

中国法医学杂志
中国法医学会

中国法医学杂志

CSTPCD
影响因子:0.352
ISSN:1001-5728
年,卷(期):2024.39(4)