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

ZHAO Yan;LIN Jian-Sheng;Department of Physiology,Zhongshan School of Medicine,Sun Yat-Sen University;Integrative Physiology of Brain Arousal Systems,Lyon Neuroscience Research Center,INSERM U1028-CNRS UMR 5292,Faculty of Medicine,Claude Bernard University;  
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 provide quite favorable attributes to make this a most promising target for sleep-wake control and sleep disorders. 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.
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