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7-(1,3-二硫杂环戊烷-2-基甲基)-1,3-二甲基黄嘌呤的体内抗炎活性。

In vivo anti-inflammatory activity of 7-(1,3-dithiolan-2-ylmethyl)-1,3-dimethylxanthine.

作者信息

Reboani M C, Franzone J S

机构信息

Research Laboratories of Istituto Biologico Chemioterapico ABC S.p.A., Turin, Italy.

出版信息

Drugs Exp Clin Res. 1990;16(6):277-84.

PMID:2086162
Abstract

A new methylxanthine derivative [7-(1,3-dithiolan-2-ylmethyl)-1,3-dimethylxanthine, ABC 99] with mucoregulatory and antibronchospastic properties has been studied. ABC 99 was observed to have marked anti-inflammatory activity in a series of experimental trials involving the principal mediators of inflammation (PAF, histamine, serotonin, LTC4-like substances, etc). It inhibits the formation of oedemas induced both by carrageenin and PAF in the rat paw, and reduces the increase in vascular permeability induced by histamine and serotonin. ABC 99 was also found to inhibit PAF-induced pleurisy, reducing the volume of pleural exudate and the presence of LTC4-like substances in the pleural cavity. When administered subacutely, ABC 99 checks the formation of granulation tissue caused by the subcutaneous implantation of cotton pellets in the rat. These experimental results indicate ABC 99 may be of particular interest in the treatment of respiratory disorders involving obstructive inflammation and bronchial hypersensitivity.

摘要

一种具有黏液调节和抗支气管痉挛特性的新型甲基黄嘌呤衍生物[7-(1,3-二硫杂环戊烷-2-基甲基)-1,3-二甲基黄嘌呤,ABC 99]已得到研究。在一系列涉及炎症主要介质(PAF、组胺、5-羟色胺、LTC4样物质等)的实验中,观察到ABC 99具有显著的抗炎活性。它能抑制角叉菜胶和PAF诱导的大鼠爪部水肿形成,并减轻组胺和5-羟色胺诱导的血管通透性增加。还发现ABC 99能抑制PAF诱导的胸膜炎,减少胸腔积液量以及胸腔中LTC4样物质的存在。当亚急性给药时,ABC 99可抑制大鼠皮下植入棉球引起的肉芽组织形成。这些实验结果表明,ABC 99在治疗涉及阻塞性炎症和支气管高敏反应的呼吸系统疾病方面可能具有特殊意义。

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