组胺受体及抗组胺药的分类及其在变应性鼻炎中的应用

Classification of histamine receptors and the application of their antihistamines in allergic rhinitis

摘要:

组胺是体内一种重要的化学介质，可通过活化H1、H2、H3、H4等类型受体参与多种病理生理过程。在变应性鼻炎（AR）的速发相中，肥大细胞脱颗粒释放组胺等炎性介质，组胺与鼻黏膜中H1受体结合触发喷嚏、鼻痒和流涕等症状，应用H1受体拮抗剂（H1RAs）可显著缓解上述症状。新近研究发现鼻黏膜中除H1受体外还存在H2、H3和H4受体，应用其相应的受体拮抗剂同样可缓解鼻部症状，提示组胺除与H1受体结合外，同时也可与H2、H3和H4受体结合，参与AR的发生发展。本文就组胺、组胺4型受体及拮抗剂分类及其在AR治疗中的应用作一综述。

Abstract:

Histamine is an important chemical medium in the body, which can participate in a variety of pathophyseologic processes by activating H1, H2, H3, and H4 receptors. In the acute phase of allergic rhinitis (AR), the degranulation of mast cells releases histamine and other inflammatory mediators. Histamine binds to H1 receptors in the nasal mucosa to trigger sneezing, nasal itching, rhinorrhea and other symptoms. Application of H1 receptor antagonists (H1RAs) can significantly alleviate the above symptoms. Additionally, recent studies have found the presence of H2, H3 and H4 receptors in the nasal mucosa which can also relieve nasal symptoms by corresponding receptor antagonists. It is suggested that histamine could not only bind to H1 receptor, but also bind to H2, H3 and H4 receptors, which participated in the occurrence and the development of AR. This review focuses on the research progress of histamine， the four histamine receptors and antihistamines in the area of pathogenesis and treatment of AR.