Baker G B, Nazarali A J, Coutts R T, Micetich R G, Hall T W
Prog Neuropsychopharmacol Biol Psychiatry. 1984;8(4-6):657-60. doi: 10.1016/0278-5846(84)90031-9.
Brain levels of 5-hydroxytryptamine (5-HT), tryptamine (T), 2-phenylethylamine (PEA) and monoamine oxidase activity at 5, 15, 30, 60, 120 and 240 min were determined in male Sprague-Dawley rats after intraperitoneal injection of the "pro-drug" N-2-cyanoethyltranylcypromine (CE-TCP, dose 0.1 mMole/kg). Analyses of 5-HT, T and PEA were performed on an electron-capture gas chromatograph with a capillary column. Activity of MAO-A and MAO-B was measured using a radiochemical method. Results indicate substantial inhibition of MAO in rat brain after intraperitoneal administration of CE-TCP, leading to elevated levels of 5-HT, T and PEA as early as 5 min after drug administration. Increases in brain levels of the trace amines T and PEA were much greater (approximately 40 and 100 times control levels, respectively) than with 5-HT (approximately 1.8 times control level) 240 min after administration of CE-TCP.
在雄性斯普拉格-道利大鼠腹腔注射“前体药物”N-2-氰基乙基反苯环丙胺(CE-TCP,剂量0.1毫摩尔/千克)后,于5、15、30、60、120和240分钟测定其大脑中5-羟色胺(5-HT)、色胺(T)、2-苯乙胺(PEA)的水平以及单胺氧化酶活性。5-HT、T和PEA的分析在配备毛细管柱的电子捕获气相色谱仪上进行。MAO-A和MAO-B的活性采用放射化学方法测定。结果表明,腹腔注射CE-TCP后,大鼠大脑中的MAO受到显著抑制,给药后5分钟时5-HT、T和PEA水平就开始升高。给药240分钟后,痕量胺T和PEA的大脑水平升高幅度(分别约为对照水平的40倍和100倍)远大于5-HT(约为对照水平的1.8倍)。