Adams J D, Baillie T A, Trevor A J, Castagnoli N
Biomed Mass Spectrom. 1981 Nov;8(11):527-38. doi: 10.1002/bms.1200081103.
The in vitro metabolic fate of the anesthetic agent ketamine [(+)2-o-chlorophenyl-2-methylaminocyclohexanone] has been evaluated using microsomal preparations from rat liver. With the aid of a rapid, nonselective metabolite extraction procedure and sample analysis by combined glass capillary gas chromatography low (and high) resolution mass spectrometry, eight metabolites of the drug were identified, six of which have not been reported previously. The novel metabolites were products of alicyclic ring hydroxylation of ketamine and of N-desmethylketamine (norketamine). Semi-quantitative analysis of metabolites produced during microsomal incubation was achieved using glass capillary gas chromatography. The results from this study indicate that 5,6-dehydronorketamine, previously considered to be a major biotransformation product of ketamine in mammalian systems, is almost certainly a methodological artefact.
已利用大鼠肝脏微粒体制剂评估了麻醉剂氯胺酮[（+）2-邻氯苯基-2-甲基氨基环己酮]的体外代谢命运。借助快速、非选择性的代谢物提取程序以及玻璃毛细管气相色谱-低（高）分辨率质谱联用进行样品分析，鉴定出该药物的8种代谢物，其中6种此前未见报道。这些新代谢物是氯胺酮和N-去甲基氯胺酮（去甲氯胺酮）脂环族环羟基化的产物。利用玻璃毛细管气相色谱对微粒体孵育过程中产生的代谢物进行了半定量分析。本研究结果表明，5,6-脱氢去甲氯胺酮（以前被认为是氯胺酮在哺乳动物系统中的主要生物转化产物）几乎肯定是一种方法学假象。
