Kinemuchi H, Arai Y, Toyoshima Y, Tadano T, Kisara K
Department of Pharmacology, School of Medicine, Showa University, Tokyo, Japan.
Jpn J Pharmacol. 1988 Feb;46(2):197-9. doi: 10.1254/jjp.46.197.
To further clarify highly MAO-A- or -B-selective inhibitory properties of 5-fluoro-alpha-methyltryptamine (5-FMT) and p-chloro-beta-methylphenethylamine (p-CMPEA), we determined the types and K1 values of inhibition of rat brain MAO-A and -B activity in vitro. The kinetic data obtained showed that 5-FMT is a competitive MAO-A-selective inhibitor with about a 18,000-fold higher sensitivity than MAO-B. In contrast, p-CMPEA is a competitive MAO-B-selective inhibitor with about a 620-fold higher sensitivity. Based on the present findings of highly MAO-A- or -B-selective inhibition, these two compounds might prove to be of value in in vivo studies.
为了进一步阐明5-氟-α-甲基色胺（5-FMT）和对氯-β-甲基苯乙胺（p-CMPEA）对单胺氧化酶A（MAO-A）或单胺氧化酶B（MAO-B）的高度选择性抑制特性，我们在体外测定了大鼠脑MAO-A和MAO-B活性的抑制类型及K1值。所获得的动力学数据表明，5-FMT是一种竞争性MAO-A选择性抑制剂，其敏感性比MAO-B高约18000倍。相比之下，p-CMPEA是一种竞争性MAO-B选择性抑制剂，其敏感性高约620倍。基于目前对MAO-A或MAO-B的高度选择性抑制的研究结果，这两种化合物可能在体内研究中具有价值。
