{"title":"Are leukotrienes really the world’s best bronchoconstrictors and at least 100 to 1000 times more potent than histamine?","authors":"Thomas Boehm, Bernd Jilma","doi":"10.1016/j.drudis.2025.104349","DOIUrl":null,"url":null,"abstract":"<div><div>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.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 5","pages":"Article 104349"},"PeriodicalIF":6.5000,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Discovery Today","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1359644625000625","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
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.
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.