Yamada N, Takahashi S, Todd K G, Baker G B, Paetsch P R
Department of Psychiatry, University of Alberta, Edmonton, Canada.
J Pharm Sci. 1993 Sep;82(9):934-7. doi: 10.1002/jps.2600820912.
Time- and dose-response analyses were undertaken to investigate the effects of the substituted hydrazine monoamine oxidase (MAO) inhibitors iproniazid and nialamide on the following: MAO-A and -B activity; levels of gamma-aminobutyric acid (GABA), alanine (ALA), and the neurotransmitter amines dopamine, noradrenaline, and 5-hydroxytryptamine (serotonin) and their acid metabolites; and the activity of GABA-transaminase and ALA-transaminase. The results showed that these drugs are relatively potent MAO inhibitors but, unlike the unsubstituted hydrazine MAO inhibitor phenelzine, they do not produce increased GABA and ALA levels in brain. These experiments suggest that a free hydrazine group is necessary for MAO inhibitors to also have marked effects on GABA and ALA.
进行了时间和剂量反应分析，以研究取代肼单胺氧化酶（MAO）抑制剂异烟肼和尼亚酰胺对以下方面的影响：MAO - A和 - B活性；γ-氨基丁酸（GABA）、丙氨酸（ALA）以及神经递质胺类多巴胺、去甲肾上腺素和5-羟色胺（血清素）及其酸性代谢产物的水平；以及GABA转氨酶和ALA转氨酶的活性。结果表明，这些药物是相对强效的MAO抑制剂，但与未取代肼的MAO抑制剂苯乙肼不同，它们不会使脑中GABA和ALA水平升高。这些实验表明，游离肼基团对于MAO抑制剂对GABA和ALA产生显著影响是必要的。
