中枢组织胺H3受体在睡眠-觉醒调节中的功用及作为治疗睡眠障碍药物干预靶点的依据  

The Brain Histamine H3 Receptors: Sleep-Wake Control and Novel Therapeutic Targets for Sleep Disorders

作　　者：赵妍[1,2,3] 林建生 

机构地区：[1]中山大学中山医学院生理教研室,广州510080 [2]法国国家健康与医学研究院/国家科学研究中心 [3]里昂大学医学院大脑觉醒机制研究室,里昂69373

出　　处：《生理科学进展》2014年第1期7-15,共9页Progress in Physiological Sciences

摘　　要：中枢组织胺(组胺)神经元位于下丘脑后部并广泛投射到全脑各部,在维持上行觉醒方面发挥重要作用。组胺H3受体调节组胺合成、释放及组胺神经元的活动,还参与调节脑内其它神经递质释放。凭借广泛区域表达和对多种神经递质的调节,H3受体近年备受重视并成为睡眠调节和对抗睡眠-觉醒障碍的有力药物干预靶点。随着对H3受体研究的深入及其在临床领域的应用,有必要对H3受体在睡眠觉醒调节中的作用作一综述,这对进一步探索H3受体的生理功能和临床药理学研究具有重要意义。Histaminergic neurons are located exclusively in the posterior hypothalamus from where they project to virtually all brain areas and fulfill a major role in the maintenance of waking. H3-receptors are firstly autoreceptors damping the release and synthesis of histamine and the firing of histamine neurons. This action also extends to heteroreceptors on most other neurotransmitter systems, allowing a powerful control over multiple homeostatic functions. The particular properties and locations of H3-receptors pro- vide quite favorable attributes to make this a most promising target for sleep-wake control and sleep disor- ders. This review summarizes the most recent data on the role of H3-receptor in physiological sleep-wake regulation and preclinical and clinical evidence supporting H3-receptor as brain target for therapy of sleep and vigilance disorders.

关 键 词：组织胺 H3受体 睡眠-觉醒 睡眠障碍 

分 类 号：R338[医药卫生—人体生理学]