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组胺H4受体及其拮抗剂的研究进展

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组胺H4 受体(histamine H4 receptor,H4R)是组胺受体的亚型之一,主要在免疫系统和胃肠道组织中表达.组胺是H4R的内源性配体,其与H4R结合可导致白介素等促炎因子的分泌显著增加,并招募免疫细胞至炎症部位,促进多种炎症和癌症的发生和发展.H4R可作为潜在的药物靶标,在炎症性肠病、过敏性鼻炎、特应性皮炎、过敏性哮喘、类风湿关节炎、神经病理性炎症和癌症等疾病的治疗中发挥重要作用.因此,新型选择性H4R拮抗剂的研究对其药物开发具有重要意义.综述H4R及其拮抗剂的研究情况,旨在为本领域的深入研究提供参考.
Research Progress of Histamine H4 Receptor and Its Antagonists
Histamine H4 receptor(H4R),one of the subtypes of histamine receptors,is mainly expressed in the immune system and gastrointestinal tissues.The binding of histamine,the endogenous ligand of H4R,to H4R can lead to a significant increase of pro-inflammatory factors such as interleukin,and recruit immune cells to the inflammatory site,promoting the occurrence and development of a variety of inflammations and cancers.H4R can be used as a potential drug target for the treatment of inflammatory bowel disease,allergic rhinitis,atopic rhinitis,allergic asthma,rheumatoid arthritis,neuropathic inflammation,cancer and other diseases.Therefore,the study of novel selective H4R antagonists is of great significance for its drug development.This paper reviews the research progress of H4R and its antagonists in the hope of providing some reference for the research in this field.

histamine H4 receptorantagonistselectivityinflammationcancer

唐鸿铭、侯滔、王纪霞、周维佳

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大连海洋大学,辽宁 大连 116023

中国科学院大连化学物理研究所,辽宁 大连 116023

赣江中药创新中心江西省中药药效物质基础重点实验室,江西 南昌 330000

组胺H4受体 拮抗剂 选择性 炎症 癌症

2024

药学进展
中国药科大学

药学进展

影响因子:0.624
ISSN:1001-5094
年,卷(期):2024.48(12)