Coutts R T, Nazarali A J, Baker G B, Pasutto F M
Can J Physiol Pharmacol. 1986 Jun;64(6):724-8. doi: 10.1139/y86-122.
N-(2-Cyanoethyl)amphetamine (fenproporex, CE-AM) is a clinically used anorexiant claimed to be devoid of the stimulant properties associated with amphetamine (AM). This claim was inconsistent with preliminary studies conducted in our laboratories which indicated that CE-AM is metabolically dealkylated to AM to a considerable extent in the rat. Concentration-time profiles of CE-AM and its metabolites AM and 4-hydroxyamphetamine (4-OH-AM) in the rat brain were constructed after administration of CE-AM. Analyses of CE-AM, AM, and 4-OH-AM were performed by gas chromatography with electron-capture detection using pentafluorobenzoyl chloride (under aqueous conditions) as the derivatizing reagent. The half-life (t1/2) and the maximum concentration (Cmax) of AM after administration of CE-AM were calculated to be 2.04 and 0.56 times the respective t1/2 and Cmax obtained after an equimolar dose of AM. Significant differences in the profiles of 4-OH-AM were also observed. The Cmax of 4-OH-AM in rat brain after administration of CE-AM was nearly 4 times higher and the tmax (time at which concentration is maximum) 4 times lower than the respective Cmax and tmax values of 4-OH-AM observed after an equimolar dose of AM.
N-（2-氰基乙基）苯丙胺（芬普雷司，CE-AM）是一种临床使用的食欲抑制剂，据称不具有与苯丙胺（AM）相关的兴奋特性。这一说法与我们实验室进行的初步研究不一致，该研究表明，CE-AM在大鼠体内会在很大程度上代谢脱烷基生成AM。在给予CE-AM后，构建了大鼠脑中CE-AM及其代谢产物AM和4-羟基苯丙胺（4-OH-AM）的浓度-时间曲线。采用五氟苯甲酰氯（在水相条件下）作为衍生试剂，通过气相色谱-电子捕获检测法对CE-AM、AM和4-OH-AM进行分析。给予CE-AM后，AM的半衰期（t1/2）和最大浓度（Cmax）经计算分别为等摩尔剂量AM给药后相应t1/2和Cmax的2.04倍和0.56倍。在4-OH-AM的曲线中也观察到了显著差异。给予CE-AM后，大鼠脑中4-OH-AM的Cmax比等摩尔剂量AM给药后观察到的4-OH-AM相应Cmax值高近4倍，而达峰时间（浓度最高时的时间）则低4倍。
