近日,公安部禁讀情報(bào)技術(shù)中心胡文老師,使用IPHASE品牌產(chǎn)品:pHLMs在《Biomedical chromatography》期刊上發(fā)表文章《Metabolism of four novel structural analogs of ketamine, 2-FXE [2-(ethylamino)-2-(2-fluorophenyl) cyclohexan-1-one], 2-MDCK [2-(methylamino)-2-(o-tolyl) cyclohexan-1-one], 3-DMXE [2-(ethylamino)-2-(m-tolyl) cyclohexan-1-one], and 2-DMXE [2-(ethylamino)-2-(o-tolyl) cyclohexan-1-one], in human liver microsomes based on ultra-performance liquid chromatography–high-resolution tandem mass spectrometry》,影響因子1.8!
本論文中提到:新的精神活性物質(zhì)不斷涌現(xiàn),其中具有2-氨基-2-苯基環(huán)己酮核心結(jié)構(gòu)的氯安酮類似物因其持續(xù)參與急性中毒而引起全球關(guān)注,這些物質(zhì)的監(jiān)測(cè)很大程度上依賴于代謝數(shù)據(jù)的獲取,然而,缺乏這些新興結(jié)構(gòu)類似物的體外人類代謝信息給藥物控制工作帶來(lái)了重大挑戰(zhàn),為了應(yīng)對(duì)這一挑戰(zhàn),研究了四種新型氯安酮結(jié)構(gòu)類似物的第一階段代謝模式,手次利用人肝微粒體,使用超高效液相色譜法和高分辨率串聯(lián)質(zhì)譜法鑒定代謝物,研究結(jié)果表明,N-脫烷基化和羥基化是主要的代謝反應(yīng),還有其他顯著的反應(yīng),包括氧化、還原和脫水。
摘要
New psychoactive substances are constantly emerging, among which ketamine analogs with the core structure of 2-amino-2-phenylcyclohexanone have attracted global attention due to their continued involvement in acute intoxications. The monitoring of these substances largely relies on the acquisition of metabolic data. However, the lack of in vitro human metabolism information for these emerging structural analogs presents significant challenges to drug control efforts. To address this challenge, we investigated the first-phase metabolism patterns of four novel ketamine structural analogs of 2-FXE [2-(ethylamino)-2-(2-fluorophenyl) cyclohexan-1-one], 2-MDCK [2-(methylamino)-2-(o-tolyl) cyclohexan-1-one], 3-DMXE [2-(ethylamino)-2-(m-tolyl) cyclohexan-1-one], and 2-DMXE [2-(ethylamino)-2-(o-tolyl) cyclohexan-1-one] utilizing human liver microsomes for the first time. Metabolites were identified using ultra-performance liquid chromatography coupled with high-resolution tandem mass spectrometry. Our findings reveal that N-dealkylation and hydroxylation are the primary metabolic reactions, alongside other notable reactions, including oxidation, reduction, and dehydration. Based on our extensive research, we propose Ndealkylation and hydroxylation metabolites as appropriate analytical markers for monitoring the consumption of these substances.
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