Kumar S, Pandey B R, Parmar S S, Gallagher J R, Mayer G G
Res Commun Chem Pathol Pharmacol. 1984 Apr;44(1):163-6.
Nine 1-(3,4-dimethoxyphenethyl)-2-methyl-4-(substituted benzylidene)-5- imidazolones were evaluated for their ability to inhibit the activity of rat brain monoamine oxidase during oxidative deamination of tyramine, 5-hydroxytryptamine (serotonin), and kynuramine. All substituted imidazolones inhibited monoamine oxidase activity. A concentration-dependent inhibition of monoamine oxidase was observed using kynuramine as the substrate and the degree of enzyme inhibition was also evaluated on the basis of their I50 values. Preincubation of imidazolones with the enzyme preparations for varying lengths of time prior to the addition of substrate in no way altered their degree of inhibition and thus exhibited a reversible nature of inhibition. A kinetic study carried out with 1-(3,4-dimethoxy-phenethyl)-2-methyl-4-(4- nitrobenzylidene )-5- i midazolone revealed a competitive nature of inhibition of rat brain monoamine oxidase.
对9种1-(3,4-二甲氧基苯乙基)-2-甲基-4-(取代亚苄基)-5-咪唑酮进行了评估，考察它们在酪胺、5-羟色胺（血清素）和犬尿胺氧化脱氨过程中抑制大鼠脑单胺氧化酶活性的能力。所有取代的咪唑酮均能抑制单胺氧化酶活性。以犬尿胺为底物时，观察到单胺氧化酶的浓度依赖性抑制作用，并且还根据其半数抑制浓度（I50）值评估了酶抑制程度。在添加底物之前，将咪唑酮与酶制剂预孵育不同时长，这丝毫没有改变它们的抑制程度，因此显示出抑制作用的可逆性。对1-(3,4-二甲氧基苯乙基)-2-甲基-4-(4-硝基亚苄基)-5-咪唑酮进行的动力学研究揭示了其对大鼠脑单胺氧化酶抑制作用的竞争性本质。
