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首页> 外文期刊>Toxicology Letters: An International Journal Providing a Forum for Original and Pertinent Contributions in Toxicology Research >Inhibition potential of 3,4-methylenedioxymethamphetamine (MDMA) and its metabolites on the in vitro monoamine oxidase (MAO)-catalyzed deamination of the neurotransmitters serotonin and dopamine
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Inhibition potential of 3,4-methylenedioxymethamphetamine (MDMA) and its metabolites on the in vitro monoamine oxidase (MAO)-catalyzed deamination of the neurotransmitters serotonin and dopamine

机译：3,4-亚甲二氧基甲基苯丙胺（MDMA）及其代谢物对单胺氧化酶（MAO）催化的神经递质5-羟色胺和多巴胺脱氨基的抑制作用

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Neurotoxicity of 3,4-methylenedioxymethamphetamine (MDMA) is still controversially discussed. Formation of reactive oxygen species e.g. based on elevated dopamine (DA) concentrations and DA quinone formation is discussed among others. Inhibition potential of MDMA metabolites regarding neurotransmitter degradation by catechol-O-methyltransferase and sulfotransferase was described previously. Their influence on monoamine oxidase (MAO) - the major DA degradation pathway-has not yet been studied in humans. Therefore the inhibition potential of MDMA and its metabolites on the deamination of the neurotransmitters DA and serotonin (5-HT) by MAO-A and B using recombinant human enzymes in vitro should be investigated. In initial studies, MDMA and MDA showed relevant inhibition (> 30%) toward MAO A for 5-HT and DA. No relevant effects toward MAO B were observed. Further investigation on MAO-A revealed MDMA as a competitive inhibitor of 5-HT and DA deamination with Ki 24.5 +/- 7.1 mu M and 18.6 +/- 4.3 mu M respectively and MDA as a mixed-type inhibitor with Ki 7.8 +/- 2.6 mM and 8.4 +/- 3.2 mu M respectively. Although prediction of in vivo relevance needs to be done with care, relevant inhibitory effects at expected plasma concentrations after recreational MDMA consumption seems unlikely based on the obtained data. (C) 2015 Elsevier Ireland Ltd. All rights reserved.
机译：3,4-亚甲二氧基甲基苯丙胺（MDMA）的神经毒性仍存在争议。活性氧的形成例如基于升高的多巴胺（DA）浓度和DA醌的形成等进行了讨论。以前已经描述了MDMA代谢物对儿茶酚-O-甲基转移酶和磺基转移酶对神经递质降解的抑制作用。它们对单胺氧化酶（MAO）-主要的DA降解途径的影响-尚未在人类中进行研究。因此，应研究MDMA及其代谢物在体外使用重组人酶对MAO-A和B脱除神经递质DA和5-羟色胺（5-HT）的潜力。在最初的研究中，MDMA和MDA对5-HT和DA对MAO A表现出相关的抑制作用（> 30％）。没有观察到对MAO B的相关影响。对MAO-A的进一步研究表明，MDMA作为5-HT和DA脱氨基的竞争性抑制剂，分别具有Ki 24.5 +/- 7.1μM和18.6 +/- 4.3μM，而MDA是具有Ki 7.8 + /的混合型抑制剂-分别为2.6 mM和8.4 +/- 3.2μM。尽管需要谨慎地进行体内相关性的预测，但根据获得的数据，在消遣性MDMA消费后，预期血浆浓度下的相关抑制作用似乎不太可能。 （C）2015 Elsevier Ireland Ltd.保留所有权利。

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