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组胺H1和H4受体在变应性炎症中的作用:新型抗组胺药的探索

The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines.

作者信息

Thurmond Robin L, Gelfand Erwin W, Dunford Paul J

机构信息

Johnson & Johnson Pharmaceutical Research & Development, L.L.C. San Diego, California 92121, USA.

出版信息

Nat Rev Drug Discov. 2008 Jan;7(1):41-53. doi: 10.1038/nrd2465.

DOI:10.1038/nrd2465
PMID:18172439
Abstract

Histamine has a key role in allergic inflammatory conditions. The inflammatory responses resulting from the liberation of histamine have long been thought to be mediated by the histamine H1 receptor, and H1-receptor antagonists--commonly known as antihistamines--have been used to treat allergies for many years. However, the importance of histamine in the pathology of conditions such as asthma and chronic pruritus may have been underestimated. Here, we review accumulating evidence suggesting that histamine indeed has roles in inflammation and immune function modulation in such diseases. In particular, the discovery of a fourth histamine receptor (H4) and its expression on numerous immune and inflammatory cells has prompted a re-evaluation of the actions of histamine, suggesting a new potential for H4-receptor antagonists and a possible synergy between H1 and H4-receptor antagonists in targeting various inflammatory conditions.

摘要

组胺在过敏性炎症状态中起关键作用。长期以来,人们一直认为组胺释放所引发的炎症反应是由组胺H1受体介导的,而H1受体拮抗剂——通常被称为抗组胺药——多年来一直用于治疗过敏症。然而,组胺在哮喘和慢性瘙痒等病症病理过程中的重要性可能被低估了。在此,我们综述了越来越多的证据,这些证据表明组胺确实在这类疾病的炎症和免疫功能调节中发挥作用。特别是,第四种组胺受体(H4)的发现及其在众多免疫和炎症细胞上的表达,促使人们重新评估组胺的作用,这表明H4受体拮抗剂具有新的潜力,并且H1和H4受体拮抗剂在针对各种炎症状态时可能存在协同作用。

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The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines.组胺H1和H4受体在变应性炎症中的作用:新型抗组胺药的探索
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