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[布洛芬和萘普生与内过氧化物前列腺素合成酶的相互作用机制]

[Mechanism of ibuprofen and naproxen interaction with endoperoxide prostaglandin synthetase].

作者信息

Muratov V K, Varfolomeev S D, Igumnova N D, Mevkh A T, Churiukanov V V

出版信息

Farmakol Toksikol. 1984 Jan-Feb;47(1):71-4.

PMID:6423406
Abstract

The authors studied the pattern and mechanism of ibuprophen and naproxen interaction with endoperoxideprostaglandin synthetase (PGH synthetase) of sheep vesicular glands. The enzymatic activity of PGH synthetase was determined polarographically with the aid of a Clark electrode. Ibuprophen and naproxen were found to inhibit completely PGH synthetase at concentrations of the order of 1 X 10(-5) M. As regards the mechanism of action both the drugs are competitive inhibitors of this enzyme with reference to arachidonic acid and incompetitive inhibitors with reference to adrenaline, an electron donor.

摘要

作者研究了布洛芬和萘普生与绵羊精囊内过氧化物前列腺素合成酶(PGH合成酶)相互作用的模式和机制。借助克拉克电极通过极谱法测定PGH合成酶的酶活性。发现布洛芬和萘普生在1×10⁻⁵M左右的浓度下可完全抑制PGH合成酶。就作用机制而言,这两种药物相对于花生四烯酸是该酶的竞争性抑制剂,相对于电子供体肾上腺素是非竞争性抑制剂。

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