Green A L, McGachy H A
J Pharm Pharmacol. 1987 May;39(5):392-4. doi: 10.1111/j.2042-7158.1987.tb03405.x.
Five tricyclic antidepressants, amitriptyline, clomipramine, desipramine, imipramine and iprindole, have comparable potencies as inhibitors of monoamine oxidase in rodent brain and liver. With rodent brain, potency was always greater with phenethylamine as substrate than with benzylamine, and was generally least with 5-HT. With mouse liver, in which monoamine oxidase is mainly B type, potency with tyramine and dopamine as substrates was close to that found with phenethylamine. The kinetics of inhibition varied with both the substrate and the tissue, and were inconsistent with a simple ping-pong model for substrate oxidation. The relevance of these observations to clinical effectiveness is discussed.
五种三环类抗抑郁药，即阿米替林、氯米帕明、地昔帕明、丙咪嗪和茚满丙二胺，在啮齿动物脑和肝脏中作为单胺氧化酶抑制剂具有相当的效力。对于啮齿动物脑，以苯乙胺为底物时的效力总是高于以苄胺为底物时的效力，且通常以5-羟色胺为底物时效力最低。在小鼠肝脏中，单胺氧化酶主要为B型，以酪胺和多巴胺为底物时的效力与以苯乙胺为底物时相近。抑制动力学随底物和组织的不同而变化，且不符合底物氧化的简单乒乓模型。讨论了这些观察结果与临床疗效的相关性。
