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[丙咪嗪对突触体部分钾离子 - 对硝基苯磷酸酶活性的抑制性质]

[Nature of the melipramine inhibition of the K+-n-nitrophenyl phosphatase activity of a synaptosomal fraction].

作者信息

Locherga V I, Matyshevskaia O P, Glebova L N

出版信息

Farmakol Toksikol. 1978 Jan-Feb;41(1):19-23.

PMID:23957
Abstract

The influence of antidepressant melipramine (imipramine) on the K+-paranitrophenyl-phosphatase (K+-n-NFP-ase) activity of the synaptosomal fraction in the bull's brain cortex, treated with sodium iodide, was studied in in vitro experiments. Melipramine (5.10(-5)--10(-3)M) is shown to inhibit the K+-n-NFP-ase activity, competing with potassium ions. With pH changing from acid and neutral to alkaline values the inhibitory action of melipramine gains in intensity, whereas the protective effect of potassium ions declines. It is suggested that one of the mechanisms responsible for the inhibition of the K+-p-NFP-ase activity by melipramine is interaction of the inhibitor in the anionic sections of the enzyme complex.

摘要

在体外实验中,研究了抗抑郁药米帕明(丙咪嗪)对经碘化钠处理的公牛大脑皮层突触体部分的钾-对硝基苯磷酸酶(K+-n-NFP-酶)活性的影响。结果表明,米帕明(5×10⁻⁵ - 10⁻³M)与钾离子竞争,抑制K+-n-NFP-酶活性。随着pH值从酸性、中性变为碱性,米帕明的抑制作用增强,而钾离子的保护作用减弱。提示米帕明抑制K+-p-NFP-酶活性的机制之一是抑制剂与酶复合物阴离子部分的相互作用。

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