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大鼠脑中两种单胺氧化酶对多巴胺的代谢及其受西莫沙酮的抑制作用。

The metabolism of dopamine by both forms of monoamine oxidase in the rat brain and its inhibition by cimoxatone.

作者信息

Fowler C J, Benedetti M S

出版信息

J Neurochem. 1983 Jun;40(6):1534-41. doi: 10.1111/j.1471-4159.1983.tb08123.x.

Abstract

In the rat brain, dopamine is metabolised by both A and B forms of monoamine oxidase (MAO), although the A form of the enzyme is the major component. The Km of MAO-A toward dopamine (120 microM) is lower than the Km of MAO-B toward this substrate (340 microM). The activity of MAO-A was lower in old rats than in young rats, and the same degree of decrease was found for 5-hydroxytryptamine as for dopamine as substrates for this enzyme form. The activity of MAO-B was higher in the old rats, the degree of increase being the same for dopamine as for beta-phenethylamine as substrates for this enzyme form. The Ki values of the inhibition of MAO-A by cimoxatone and MD770222 (the principal plasma metabolite of cimoxatone) were independent of the substrate used to assay for activity, but were lower than the Ki values for the inhibition of MAO-B by these compounds.

摘要

在大鼠脑中,多巴胺可被单胺氧化酶(MAO)的A、B两种形式代谢,不过该酶的A形式是主要成分。MAO-A对多巴胺的米氏常数(Km)(120微摩尔)低于MAO-B对该底物的米氏常数(340微摩尔)。老年大鼠中MAO-A的活性低于年轻大鼠,对于作为该酶形式底物的5-羟色胺和多巴胺而言,其降低程度相同。老年大鼠中MAO-B的活性较高,对于作为该酶形式底物的多巴胺和β-苯乙胺而言,其升高程度相同。西莫沙酮和MD770222(西莫沙酮的主要血浆代谢物)对MAO-A抑制作用的抑制常数(Ki)值与用于测定活性的底物无关,但低于这些化合物对MAO-B抑制作用的Ki值。

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