ＡＭＴとＭＡＯ阻害剤作用について
TITL: Studies of monoamine oxidase and semicarbazide-sensitive amine oxidase.II. Inhibition by alpha-methylated substrate-analogue monoamines, alpha-methyltryptamine, alpha-methylbenzylamine and two enantiomers of alpha-methylbenzylamine.
AUTH: Arai Y; Toyoshima Y; Kinemuchi H
CITE: Jpn J Pharmacol 1986 Jun; 41 (2): 191-7
ABST:The alpha-methylated substrate-analogue monoamines, dl-alpha-methyltryptamine, dl-alpha-methylbenzylamine and two optical isomers of alpha-methylbenzylamine, were shown to be inhibitors of rat lung semicarbazide-sensitive amine oxidase (SSAO), with dl-alpha-methyltryptamine being the most potent and d-alpha-methylbenzylamine, the least. The three compounds, dl-alpha-methyltryptamine and the two isomers of alpha-methylbenzylamine also inhibited rat brain monoamine oxidase (MAO)-A and -B with a greater selectivity towards MAO-A.
ｄｌ−アルファメチルトリプタミン、ｄｌ−アルファメチルベンジルアミン、そしてｄｌ−アルファメチルベンジルアミンの二つのオプティカルインソマー（光学用異性体？）が、ネズミの肺における実験でアミンの抑制（ＳＳＡＯ）作用があることがわかった。ｄｌ−アルファメチルトリプタミンがもっとも影響があり、ｄｌ−メチルベンジルアミンが最も少ない。これら三つの化合物、ｄｌ−アルファメチルトリプタミンとｄｌ−メチルベンジルアミンの二つの異性体はネズミの脳において、モノアミンオキシダーゼ（ＭＡＯ）−ＡとＢの阻害作用をあらわした。特にＭＡＯ−Ａにおいて影響が強い。
Preincubation of rat lung and brain homogenates with either of these compounds revealed that the inhibition of MAO and SSAO is reversible. The modes of inhibition of MAO-A and -B were competitive with the substrates tested. However, inhibition of SSAO by dl-alpha-methyltryptamine was found to be a mixed type (with a Ki value of 47 microM) and those by the racemic form and two isomers of alpha-methylbenzylamine were non-competitive (with Ki values of 90 microM for the racemic compound, 1070 microM for the d-isomer and 72 microM for the l-isomer). The present results indicate that SSAO can recognize optical isomers and that some alpha-methylated monoamines tested in the present study inhibit SSAO with properties different from those as MAO inhibitors.
ｄｌ−アルファメチルトリプタミンのＳＳＡＯ阻害は混合型だとかなんとかかんとか・・・
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