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Metabolism of a new synthetic opioid tetrahydrofuranylfentanyl in fresh isolated human hepatocytes: Detection and confirmation of ring-opened metabolites.
Drug Testing and Analysis ( IF 2.6 ) Pub Date : 2020-01-19 , DOI: 10.1002/dta.2743 Tatsuyuki Kanamori 1 , Hiroki Segawa 1 , Tadashi Yamamuro 1 , Kenji Kuwayama 1 , Kenji Tsujikawa 1 , Yuko T Iwata 1
Drug Testing and Analysis ( IF 2.6 ) Pub Date : 2020-01-19 , DOI: 10.1002/dta.2743 Tatsuyuki Kanamori 1 , Hiroki Segawa 1 , Tadashi Yamamuro 1 , Kenji Kuwayama 1 , Kenji Tsujikawa 1 , Yuko T Iwata 1
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The metabolism of a new synthetic opioid tetrahydrofuranylfentanyl (THF‐fentanyl) was investigated using fresh human hepatocytes. Fourteen metabolites of THF‐fentanyl, such as tetrahydrofuran ring‐opened metabolites, desphenethylated metabolites, hydroxylated metabolites, and hydroxylated and methoxylated metabolites and their glucuronides, were detected in the culture medium of hepatocytes incubated with THF‐fentanyl. Six metabolites, i.e. desphenethylated metabolite, 4′‐hydroxy‐THF‐fentanyl, β‐hydroxy‐THF‐fentanyl, 4′‐hydroxy‐3′‐methoxy‐THF‐fentanyl, ring‐opened alcohol metabolite, and ring‐opened carboxylic acid metabolite, were identified via chemically synthesized authentic standards. A ring‐opened alcohol metabolite and a ring‐opened carboxylic acid metabolite are thought to be formed by reduction or oxidation of the intermediate aldehyde, which was formed by ring‐opening of the metabolite hydroxylated at the carbon atom adjacent to the oxygen atom of the tetrahydrofuran ring. A ring‐opened carboxylic acid metabolite was the main metabolite of THF‐fentanyl based on the peak intensity.
中文翻译：
新的合成阿片样物质四氢呋喃基芬太尼在新鲜分离的人肝细胞中的代谢：开环代谢物的检测和确认。
使用新鲜的人类肝细胞研究了新的合成阿片样物质四氢呋喃基芬太尼（THF-芬太尼）的代谢。在用THF-芬太尼孵育的肝细胞培养基中检测到THF-芬太尼的14种代谢物，例如四氢呋喃开环代谢物，去乙基化的代谢物，羟基化的代谢物以及羟基化和甲氧基化的代谢物及其葡糖醛酸。六种代谢物，即去乙基化代谢物，4'-羟基-THF-芬太尼，β-羟基-THF-芬太尼，4'-羟基-3'-甲氧基-THF-芬太尼，开环醇代谢物和开环羧酸代谢产物是通过化学合成的真实标准品鉴定的。开环的醇代谢物和开环的羧酸代谢物被认为是通过中间体醛的还原或氧化而形成的，它是通过在与四氢呋喃环的氧原子相邻的碳原子处羟基化的代谢物开环而形成的。基于峰强度，开环的羧酸代谢物是THF-芬太尼的主要代谢物。
更新日期：2020-01-19
中文翻译：
新的合成阿片样物质四氢呋喃基芬太尼在新鲜分离的人肝细胞中的代谢：开环代谢物的检测和确认。
使用新鲜的人类肝细胞研究了新的合成阿片样物质四氢呋喃基芬太尼（THF-芬太尼）的代谢。在用THF-芬太尼孵育的肝细胞培养基中检测到THF-芬太尼的14种代谢物，例如四氢呋喃开环代谢物，去乙基化的代谢物，羟基化的代谢物以及羟基化和甲氧基化的代谢物及其葡糖醛酸。六种代谢物，即去乙基化代谢物，4'-羟基-THF-芬太尼，β-羟基-THF-芬太尼，4'-羟基-3'-甲氧基-THF-芬太尼，开环醇代谢物和开环羧酸代谢产物是通过化学合成的真实标准品鉴定的。开环的醇代谢物和开环的羧酸代谢物被认为是通过中间体醛的还原或氧化而形成的，它是通过在与四氢呋喃环的氧原子相邻的碳原子处羟基化的代谢物开环而形成的。基于峰强度，开环的羧酸代谢物是THF-芬太尼的主要代谢物。
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