Nazarali A J, Baker G B, Coutts R T, Pasutto F M
Prog Neuropsychopharmacol Biol Psychiatry. 1983;7(4-6):813-6. doi: 10.1016/0278-5846(83)90073-8.
Three N-alkylated analogues of amphetamine were administered intraperitoneally to male Sprague-Dawley rats and whole brain levels of amphetamine (AM) and the N-alkyl analogue were determined one hour after injection of the N-alkylated compounds. The drugs administered were the N-2-cyanoethyl-(I) (fenproporex), the N-3-chloropropyl-(II) (mefenorex) and the N-n-propyl-(III) derivatives of AM: the first two of these are used clinically as anorexiants, and the latter has been used extensively to study aspects of metabolism of AM-like compounds. Analysis of AM, I, II and III was performed using electron-capture gas chromatography with a capillary column after reaction of compounds with pentafluorobenzoyl chloride under aqueous conditions. In a second comparative study, equimolar doses (0.05 mMole/kg) of I or AM were administered intraperitoneally to the rats and brain levels determined after one hour. Results indicate extensive N-dealkylation occurs for compounds I, II and III in the rat.
将三种苯丙胺的N-烷基化类似物腹腔注射给雄性Sprague-Dawley大鼠，并在注射N-烷基化化合物一小时后测定全脑水平的苯丙胺（AM）和N-烷基类似物。所给药的药物为N-2-氰基乙基-（I）（苯丙雷司）、N-3-氯丙基-（II）（氯苯雷司）以及AM的N-正丙基-（III）衍生物：其中前两种在临床上用作食欲抑制剂，而后者已被广泛用于研究AM类化合物的代谢方面。在化合物于水相条件下与五氟苯甲酰氯反应后，使用带有毛细管柱的电子捕获气相色谱法对AM、I、II和III进行分析。在第二项比较研究中，将等摩尔剂量（0.05毫摩尔/千克）的I或AM腹腔注射给大鼠，并在一小时后测定脑内水平。结果表明，化合物I、II和III在大鼠体内发生了广泛的N-脱烷基化。
