Ulgen M, Kajbaf M, Lamb J H, Jahanshahi M, Gorrod J W, Naylor S
Chelsea Department of Pharmacy, King's College London, University of London, UK.
Eur J Drug Metab Pharmacokinet. 1994 Oct-Dec;19(4):343-8. doi: 10.1007/BF03188861.
The metabolism of N-benzylcarbazole (NBC) was studied in vitro using hamster hepatic microsomes to establish whether the corresponding amide is formed. This work was carried out in order to see if the extremely low pka characteristic of such a benzylic amine would allow the formation of the carbonyl derivative. No amide formation was observed. However, a number of metabolic products were detected using HPLC, including the oxidative debenzylation products, namely carbazole and benzaldehyde, together with 2 phenolic isomers of NBC. These products were tentatively characterized by their UV spectra using a rapiscan UV detector connected to HPLC equipment. The structural characterization of these 4 metabolites, together with unchanged substrate, was carried out using desorption electron impact tandem mass spectrometry (DEI-MS/MS) on a hybrid instrument with EBQ1Q2 configuration.
使用仓鼠肝微粒体在体外研究了N-苄基咔唑（NBC）的代谢，以确定是否形成相应的酰胺。进行这项工作是为了查看这种苄胺极低的pKa特性是否会促使羰基衍生物的形成。未观察到酰胺形成。然而，使用高效液相色谱法检测到了许多代谢产物，包括氧化脱苄产物，即咔唑和苯甲醛，以及NBC的2种酚类异构体。这些产物通过连接到高效液相色谱设备的快速扫描紫外检测器，根据其紫外光谱进行了初步表征。使用具有EBQ1Q2配置的混合仪器，通过解吸电子碰撞串联质谱（DEI-MS/MS）对这4种代谢产物以及未变化的底物进行了结构表征。
