白三烯B_(4)受体拮抗剂的研究进展  

Research progress of leukotriene B_(4) receptor antagonists

作　　者：赵甜甜 沈珑瑛[1] 潘显道[1] ZHAO Tian-tian;SHEN Long-ying;PAN Xian-dao(Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)

机构地区：[1]中国医学科学院、北京协和医学院药物研究所,北京100050

出　　处：《药学学报》2022年第10期3133-3145,共13页Acta Pharmaceutica Sinica

基　　金：中国医学科学院医学与健康科技创新工程项目(2021-1-I2M-028)。

摘　　要：白三烯B(leukotriene B_(4),LTB_(4))是一种促炎调节因子,多数炎症细胞均可产生。LTB_(4)与其受体BLT1(leukotriene B_(4)receptor 1)结合后可通过趋化作用和黏附分子上调将嗜中性粒细胞和巨噬细胞迁移至炎症部位。大量研究表明LTB_(4)-BLT1轴与自身免疫性疾病及炎症的发生有关。因此,LTB_(4)受体拮抗剂对治疗这类疾病具有重要作用。本文简略描述了LTB_(4)的作用,综述了目前处于临床或临床前研究的LTB_(4)受体拮抗剂的研究进展。Leukotriene B_(4)(LTB_(4))is a proinflammatory lipid mediator that is synthesized by a number of inflammatory cells.Binding of LTBto its receptor leukotriene B_(4)receptor 1(BLT1)can migrate neutrophils and macrophages to inflammatory sites through chemotaxis and up-regulation of adhesion molecules.Many researches have shown that LTB_(4)-BLT1 axis is related to the occurrence of autoimmune disorders and other inflammatory diseases.Receptor antagonists of LTB_(4)are thus expected to be useful therapeutics for these diseases.In this review,we briefly describe the biological function of LTB_(4)and summarize the preclinical and clinical developments of LTB_(4)receptor antagonists.

关 键 词：白三烯B_(4) 拮抗剂 构效关系 

分 类 号：R914[医药卫生—药物化学]