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[苯甲酰胺衍生物对大鼠脑单胺氧化酶体外活性的影响]

[Effect of benzamide derivatives on rat brain monoamine oxidase activity in vitro].

作者信息

Gol'dina O A, Zagorevskiĭ V A, Lopatina K I, Sokolova T V, Gankina E M

出版信息

Biull Eksp Biol Med. 1986 Aug;102(8):170-2.

PMID:3742029
Abstract

The ability of moclobamide and other benzamide derivatives to inhibit the activity of monoamine oxidase in the rat brain was studied. Distinct effects of these compounds on the deamination of serotonin and norepinephrine (MAO-A substrates); 2-phenylethylamine (selective MAO-B substrate); tyramine and dopamine (MAO-A and MAO-B substrates) are shown. It was demonstrated that among all the compounds studied moclobamide appeared to be the most active and selective inhibitor of MAO-A: at a concentration of 100 microM it caused a 100% inhibition of serotonin and norepinephrine deamination, which might be explained by the presence of C1 atom in the para-position of benzene ring in moclobamide molecule. Other benzamide derivatives were less active in inhibiting MAO-A and had but a negligible effect on dopamine- and 2-phenylethylamine deamination.

摘要

研究了吗氯贝胺及其他苯甲酰胺衍生物抑制大鼠脑内单胺氧化酶活性的能力。展示了这些化合物对5-羟色胺和去甲肾上腺素(单胺氧化酶A底物)、2-苯乙胺(选择性单胺氧化酶B底物)、酪胺和多巴胺(单胺氧化酶A和B底物)脱氨基作用的不同影响。结果表明,在所研究的所有化合物中,吗氯贝胺似乎是最具活性和选择性的单胺氧化酶A抑制剂:在浓度为100微摩尔时,它可导致5-羟色胺和去甲肾上腺素脱氨基作用被100%抑制,这可能是由于吗氯贝胺分子苯环对位存在C1原子所致。其他苯甲酰胺衍生物在抑制单胺氧化酶A方面活性较低,对多巴胺和2-苯乙胺脱氨基作用的影响可忽略不计。

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