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[非甾体抗炎制剂对血浆激肽释放酶作用及缓激肽生物学效应的比较评价]

[Comparative evaluation of the action of nonsteroidal anti-inflammatory preparations on blood plasma kallikrein and the biological effects of bradykinin].

作者信息

Shvarts G Ia, Paskhina T S, Iakubovskaia R I

出版信息

Farmakol Toksikol. 1984 Jul-Aug;47(4):74-81.

PMID:6566613
Abstract

A study was made of the effects of voltaren, naproxen, flurbiprophen and ibuprophen comparatively to those of acetylsalicylic acid, butadion and indomethacin on the reactions of kininogenesis and biological effects of bradykinin. It was found that in therapeutic concentrations (10(-6)-10(-2) M), the drugs do not inhibit BAEE-esterase activity but nonspecifically inhibit (with the exception of flurbiprophen and butadion) the kininogenase activity of the highly purified human blood plasma kallikrein. A good agreement was discovered in rats between the anti-inflammatory action and protective effect of the drugs on the toxicity of the kininogenesis stimulant, cellulose sulfate. When administered in effective concentrations and doses these drugs exerted an unmarked inhibitory effect on the degree of the spasmogenous and microcirculatory reactions to exogenous bradykinin.

摘要

研究比较了双氯芬酸、萘普生、氟比洛芬和布洛芬与阿司匹林、布他酮和吲哚美辛对激肽生成反应及缓激肽生物学效应的影响。结果发现,在治疗浓度(10⁻⁶ - 10⁻² M)下,这些药物不抑制BAEE酯酶活性,但除氟比洛芬和布他酮外,可非特异性抑制高度纯化的人血浆激肽释放酶的激肽原酶活性。在大鼠中发现,这些药物的抗炎作用与其对激肽生成刺激剂硫酸纤维素毒性的保护作用之间存在良好的一致性。当以有效浓度和剂量给药时,这些药物对外源性缓激肽引起的痉挛性和微循环反应程度产生不明显的抑制作用。

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