白三烯真的是世界上最好的支气管收缩剂，比组胺强至少100到1000倍吗？

IF 6.5 2区医学 Q1 PHARMACOLOGY & PHARMACY

Drug Discovery Today Pub Date : 2025-04-01 DOI:10.1016/j.drudis.2025.104349

Thomas Boehm, Bernd Jilma

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引用次数: 0

摘要

白三烯的效力是组胺的100到1000倍，这种说法是正确的吗？我们真的可以比较带电荷的单阳离子和脂类两亲分子在吸入后穿透上皮细胞层的能力吗？在这篇综述中，我们质疑临床和药物开发注意力从组胺转向白三烯受体拮抗剂治疗慢性哮喘和急性哮喘加重的转变。目前的数据表明，组胺很可能起着比以前认为的更重要的作用。是时候重新思考在支气管痉挛中介质的作用，并将注意力转移回组胺。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Are leukotrienes really the world’s best bronchoconstrictors and at least 100 to 1000 times more potent than histamine?

It has been stated numerous times that leukotrienes are 100 to 1000 times more potent compared with histamine, but is this statement correct? Can we really compare a charged mono-cation with lipoid amphiphiles in their ability to penetrate an epithelial cell layer after inhalation challenge? In this review we question the shift in clinical and drug development attention from histamine towards leukotriene receptor antagonists for the treatment of chronic asthma and acute asthma exacerbations. The presented data indicate that histamine very likely plays a much more important role than previously assumed. It is time to rethink mediator involvement during bronchospasm and shift attention back to histamine.

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来源期刊

Drug Discovery Today 医学-药学

CiteScore

14.80

自引率

2.70%

发文量

293

审稿时长

6 months

期刊介绍： Drug Discovery Today delivers informed and highly current reviews for the discovery community. The magazine addresses not only the rapid scientific developments in drug discovery associated technologies but also the management, commercial and regulatory issues that increasingly play a part in how R&D is planned, structured and executed. Features include comment by international experts, news and analysis of important developments, reviews of key scientific and strategic issues, overviews of recent progress in specific therapeutic areas and conference reports.