组胺H1受体功能及调节机制研究进展  

Advances on research of function and regulatory mechanism of Histamine H1 receptor

作　　者：高珍[1] 崔征[1] 寇俊萍[1] 

机构地区：[1]中国药科大学中药复方研究室,江苏南京211198

出　　处：《现代生物医学进展》2009年第19期3768-3771,共4页Progress in Modern Biomedicine

基　　金：国家自然科学基金(30873322)

摘　　要：组胺1型受体(H1R)受体作为组胺最主要的受体亚型,广泛分布于中枢和外周神经末梢,随着各类新型H1受体拮抗剂的发现和基因敲除动物的应用,H1R的功能研究及其活化调节机制研究也不断深入。组胺通过H1R参与调节机体多种重要的生理病理功能,如参与炎症反应、疼痛反应、血管调节、认知功能、睡眠清醒节律、饮食节律和肥胖等。H1R活化可激活磷脂酶C(PLC),PLC水解1,4,5-磷脂酰二磷酸盐产生甘油二酯(DAG)和肌醇三磷酸(IP3),后者激活细胞内Ca2+通道,活化氮氧化物合成酶,最终生成NO和鸟苷酸环化酶(cGMP),并引起钾通道开放,导致超极化;也可激活磷脂酶A2(PLA2)形成花生四烯酸(AA)。H1R可通过活化其基因转录水平进行上调。本文就近十年来国外相关进展情况做一综述。Histamine H1 receptor is one of the most important subtype of histamine receptors and it widely distributes in the central and peripheral nerve system.With discoveries of various kinds of antihistamines and application of Histamine H1 receptor knock out animals,its functions and the regulatory and activatory mechanisms have been understood more and more extensively and throughly.H1 receptor participates and regulates many crucial physiological and pathological functions in body,such as inflammatory reaction,pain, angioregulation, sleep-awake rhythm, diet rhythm and obesity and so forth. Such excitation is achieved by activation of Gq/11 and phospholipase C（PLC）, which leads to the formation of the two second messengers, diacylglycerol （DAG） and inositol 1,4,5-triphosphate （Ins （1,4,5）P3）. The latter activates Ca2＋-dependent processes including formation of nitric oxide and cyclic GMP and opening of K＋ channels, resulting in hyperpolarization. It also activates phospholipase A （PLA）, which leads to the formation of arachidonic acid （AA）. In this article, we reviewed the aboard research advances on Histamine H1 receptor in recent years.

关 键 词：H1受体 功能 调节机制 

分 类 号：Q75[生物学—分子生物学] Q78