Suppr超能文献

一种新型硫化氢释放型阿司匹林的药理学特性

Pharmacological profile of a novel H(2)S-releasing aspirin.

作者信息

Sparatore Anna, Perrino Elena, Tazzari Valerio, Giustarini Daniela, Rossi Ranieri, Rossoni Giuseppe, Erdmann Kati, Schröder Henning, Del Soldato Piero

机构信息

Istituto di Chimica Farmaceutica e Tossicologica "Pietro Pratesi", University of Milano, Italy.

出版信息

Free Radic Biol Med. 2009 Mar 1;46(5):586-92. doi: 10.1016/j.freeradbiomed.2008.11.013. Epub 2008 Dec 6.

Abstract

The pharmacological profile of a new, safe, and effective hydrogen sulfide (H(2)S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H(2)S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H(2)S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.

摘要

本文描述了一种新型、安全且有效的阿司匹林硫化氢(H₂S)释放衍生物(ACS14)的药理学特征。我们报告了ACS14及其脱乙酰代谢产物(ACS21)的合成、初步药代动力学及其体内代谢情况,以及大鼠静脉给药后的血浆H₂S水平。ACS14保留了母体化合物抑制血栓素的活性,但似乎对胃黏膜有保护作用,这是通过增加H₂S/谷胱甘肽的形成、血红素加氧酶-1启动子活性以及抑制异前列腺素,从而影响氧化还原失衡来实现的。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验