Hallström G, Kammerer R C, Nguyen C H, Schmitz D A, Di Stefano E W, Cho A K
Drug Metab Dispos. 1983 Jan-Feb;11(1):47-53.
Four products of the in vitro oxidative metabolism of the piperidine ring of phencyclidine, 5-(1-phenylcyclohexylamino)valeraldehyde, V; N-(1-phenylcyclohexyl)-1,2,3,4-tetrahydropyridine, VIII; 5-(1-phenylcyclohexylamino)valeric acid, VII; and 1-phenylcyclohexylamine, IX, have been identified following derivatization, by GC/MS with stable isotope labeling and/or synthesis. The enamine, VIII, may be a work-up elimination product of a carbinolamine, alpha-hydroxy-N-(1-phenylcyclohexyl)piperidine, IV. The formation of all metabolites requires microsomal enzymes, but VII and the previously described N-(5-hydroxypentyl)-1-phenylcyclohexylamine, VI, also require soluble enzymes. Quantitative or semiquantitative data show that VI and VIII appear and disappear with time, whereas VII seems to be a terminal metabolite.
通过衍生化、气相色谱/质谱联用的稳定同位素标记和/或合成方法，已鉴定出苯环己哌啶哌啶环体外氧化代谢的四种产物，即5-(1-苯基环己基氨基)戊醛（V）、N-(1-苯基环己基)-1,2,3,4-四氢吡啶（VIII）、5-(1-苯基环己基氨基)戊酸（VII）和1-苯基环己胺（IX）。烯胺VIII可能是甲醇胺α-羟基-N-(1-苯基环己基)哌啶（IV）的后处理消除产物。所有代谢产物的形成都需要微粒体酶，但VII和先前描述的N-(5-羟戊基)-1-苯基环己胺（VI）也需要可溶性酶。定量或半定量数据表明，VI和VIII随时间出现和消失，而VII似乎是终末代谢产物。
