Zychlinski L, Montgomery M R
Toxicol Lett. 1984 Aug;22(2):133-8. doi: 10.1016/0378-4274(84)90056-0.
Monoamine oxidase (MAO) activity was determined in rat tissues following in vivo treatments with chlorphentermine (CP). Oxidation of seven amine substrates by liver, lung or brain mitochondrial MAO was investigated at 2 h after a single i.p. injection (60 mg/kg) or after repeated injection (once daily for 3 days, 20 mg/kg, i.p.). Deamination of the type A substrates, norepinephrine, serotonin and octopamine, was decreased significantly in liver, lung and brain after both single and repeated injections. Oxidative deamination of tyramine and dopamine (type A + B substrates) was also lowered in all organs after single and repeated exposure to CP, but to a lesser degree than the type A substrates. However, oxidation of the type B substrates, benzylamine and tryptamine, was unaffected by CP administration in comparison to control. These data indicate that CP is a specific inhibitor of mitochondrial MAO, form A.
在大鼠体内用氯苯丁胺(CP)处理后,测定了大鼠组织中的单胺氧化酶(MAO)活性。在单次腹腔注射(60mg/kg)2小时后或重复注射(每天一次,共3天,20mg/kg,腹腔注射)后,研究了肝脏、肺或脑线粒体MAO对七种胺底物的氧化作用。单次和重复注射后,肝脏、肺和脑中A型底物去甲肾上腺素、5-羟色胺和章鱼胺的脱氨基作用均显著降低。单次和重复暴露于CP后,所有器官中酪胺和多巴胺(A型+B型底物)的氧化脱氨作用也降低,但程度低于A型底物。然而,与对照相比,B型底物苄胺和色胺的氧化不受CP给药的影响。这些数据表明,CP是线粒体MAO A型的特异性抑制剂。