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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Inhibition of airway hyperreactivity, edema, and lung cell infiltration by compound U-83836E in sensitized guinea pigs.
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Inhibition of airway hyperreactivity, edema, and lung cell infiltration by compound U-83836E in sensitized guinea pigs.

机译:化合物U-83836E在致敏的豚鼠中抑制气道高反应性,水肿和肺细胞浸润。

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摘要

Sensitized guinea pigs were used to assess the effect of treatment with the compound U-83836E ((-)-2-[[4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl]methyl]-3 ,4-dihydro-2,5,7,8-tetramethyl-2H--benzopyran-6-ol, dihydrochloride) on the antigen-induced late-phase (16 h) airway hyperreactivity, increase in inflammatory cell number, edema, and release of inflammatory mediators in the bronchoalveolar lavage (BAL) fluid. After antigen challenge, an increase of the in vitro reactivity of the trachea and upper bronchi to acetylcholine and histamine and an increase in the number of leukocytes in the BAL fluid, mainly eosinophils and mononuclear cells, were observed. The concentrations of proteins, histamine, and PGE2 in the BAL fluid were also significantly increased by 53, 57, and 216%, respectively, after antigen challenge. Treatment with U-83836E (10 mg/kg) given i.p. 17 and 3 h before and 6 h after antigen challenge inhibited by approximately 80% the total cell number in the airways and the BAL fluid protein content. Moreover, this treatment totally inhibited airway hyperreactivity. Histamine and PGE2 levels in the BAL fluid were not significantly affected by U-83836E treatment. These results indicate that U-83836E is effective against some of the characteristic features of asthma in ovalbumin-sensitized guinea pigs.
机译:致敏的豚鼠用于评估化合物U-83836E((-)-2-[[4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl] methyl]的治疗效果-3,4-dihydro-2,5,7,8-tetramethyl-2H--benzopyran-6-ol,dihydrochloride)对抗原诱导的晚期(16 h)气道高反应性,炎症细胞数量增加,水肿,并在支气管肺泡灌洗液(BAL)中释放炎性介质。抗原攻击后,观察到气管和上支气管对乙酰胆碱和组胺的体外反应性增加,以及BAL液中主要是嗜酸性粒细胞和单核细胞的白细胞数量增加。抗原攻击后,BAL液中蛋白质,组胺和PGE2的浓度也分别显着增加了53、57和216%。腹膜内给予U-83836E(10 mg / kg)处理。抗原攻击之前和之后的17和3小时以及之后的6小时抑制了气道中的总细胞数和BAL流体蛋白含量的大约80%。而且,这种治疗完全抑制了气道高反应性。 U-83836E处理不会明显影响BAL液中的组胺和PGE2水平。这些结果表明,U-83836E对卵白蛋白致敏的豚鼠哮喘的某些特征有效。

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