首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Evaluation of antiasthmatic activity of 7,8,9, 10-tetrahydroazepino[2,l-b]quinazolin-12(6H)-one in combination with ambroxol in Guinea pigs
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Evaluation of antiasthmatic activity of 7,8,9, 10-tetrahydroazepino[2,l-b]quinazolin-12(6H)-one in combination with ambroxol in Guinea pigs

机译:评价7,8,9,10-四氢阿斯匹诺[2,1-b]喹唑啉-12(6H)-one与氨溴索联用对豚鼠的抗哮喘活性

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摘要

In the present study, the antiasthmatic activity of a 7,8,9,10-tetrahydro azepino[2,l-b]-quinazolin-12(6H)-one (TAZQ) and established mucolytic agent ambroxol, alone and in combination, in ovalbumin induced asthma in guinea pigs. TAZQ turned to be a potent bronchodilator when studied in in vitro tracheal strip preparation of sensitized guinea pigs against antigen induced contraction accompanied with notable antioxidant and anti-inflammatory activity at both 10 and 20 mg/kg doses. Ambroxol at the dose of 50 and 100 mg/kg found to possess potent antioxidant activity but devoid of any effect when studied for in vitro bronchodilatory or antigen induced bronchial hyper-responsiveness. The title compound in low dose combination with ambroxol significantly inhibited oval-bumin-induced airway hyper-responsiveness. The combination of two notably reduced eosinophilic infiltrations into lung and bronchoalveolar lavage fluid of sensitized animals signified the synergistic anti-inflammatory activity without any increase in bronchodilator activity of TAZQ. For relief in asthma attacks, presently studied bronchodilator mucolytic combination may be an effective treatment of choice that will take care of bronchoconstriction, bronchial inflammation, and restricted bronchial airflow due to mucus plugging into the bronchioles in acute and chronic asthma.
机译:在本研究中,在卵清蛋白中单独和组合使用7,8,9,10-四氢a庚啶[2,lb]-喹唑啉-12(6H)-one(TAZQ)和已确立的粘液溶解剂氨溴索的抗哮喘活性豚鼠诱发哮喘。当在致敏豚鼠的体外气管剥离制剂中针对抗原诱导的收缩同时具有明显的抗氧化剂和抗炎活性(分别为10和20 mg / kg剂量)时,TAZQ成为有效的支气管扩张剂。发现50和100 mg / kg的氨溴索具有强大的抗氧化活性,但在体外支气管扩张或抗原诱导的支气管高反应性研究中没有任何作用。低剂量与氨溴索合用的标题化合物可显着抑制卵白蛋白诱导的气道高反应性。致敏动物的肺和支气管肺泡灌洗液中嗜酸性粒细胞浸润的两种显着减少的组合表明协同的抗炎活性,而TAZQ的支气管扩张剂活性没有任何增加。为了缓解哮喘发作,目前研究的支气管扩张剂粘液溶解联合治疗可能是一种有效的治疗选择,它将治疗由于急,慢性哮喘中的粘液堵塞支气管而引起的支气管收缩,支气管发炎和支气管气流受限。

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