Zhou Shiyang, Huang Gangliang
Chongqing Key Laboratory of Green Synthesis and Application, Active Carbohydrate Research Institute, Chongqing Normal University Chongqing 401331 China.
Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, College of Chemistry and Chemical Engineering, Hainan Normal University Haikou 571158 China
RSC Adv. 2020 Feb 4;10(10):5874-5885. doi: 10.1039/c9ra10659f.
Histamine is formed by the decarboxylation of histidine catalyzed by enzymes. It is an endogenous biologically active substance involved in multiple complex physiological processes as an important chemical transmitter. Histamine receptors have four subtypes, H, H, H and H, all of which are G protein coupling receptors (GPCRs) with different physiological functions. Histamine plays an important role in the pathophysiological mechanism of allergic diseases, and the antagonistic effect of histamine has become an important way to study anti-allergic drugs, wherein the anti-allergic drugs used in clinical practice are mainly H receptor antagonists. Currently, there are many varieties of H receptor antagonists in clinical applications, which can be divided into ethylenediamine antagonists, amino ether antagonists, propylamine antagonists, tricyclic antagonists, piperazine antagonists and piperidine antagonists depending on their chemical structures. This article mainly reviews the research progress of allergic reactions with histamine H receptor antagonists and expounds the important aspects of the design and synthesis of various new compounds.
组胺是由酶催化组氨酸脱羧形成的。它是一种内源性生物活性物质,作为重要的化学递质参与多种复杂的生理过程。组胺受体有四种亚型,即H₁、H₂、H₃和H₄,它们均为具有不同生理功能的G蛋白偶联受体(GPCRs)。组胺在过敏性疾病的病理生理机制中起重要作用,组胺拮抗作用已成为研究抗过敏药物的重要途径,其中临床应用的抗过敏药物主要是H₁受体拮抗剂。目前临床应用的H₁受体拮抗剂有多种品种,根据其化学结构可分为乙二胺类拮抗剂、氨基醚类拮抗剂、丙胺类拮抗剂、三环类拮抗剂、哌嗪类拮抗剂和哌啶类拮抗剂。本文主要综述组胺H₁受体拮抗剂在过敏反应方面的研究进展,并阐述各种新化合物设计与合成的重要方面。