Histamine H3 receptors and sleep-wake regulation.
The histaminergic system fulfills a major role in the maintenance of waking. Histaminergic neurons are located exclusively in the posterior hypothalamus from where they project to most areas of the central nervous system. The histamine H(3) receptors are autoreceptors damping histamine synthesis, the firing frequency of histamine neurons, and the release of histamine from axonal varicosities. It is noteworthy that this action also extends to heteroreceptors on the axons of most other neurotransmitter systems, allowing a powerful control over multiple homeostatic functions. The particular properties and locations of histamine H(3) receptors provide quite favorable attributes to make this a most promising target for pharmacological interventions of sleep and waking disorders associated with narcolepsy, Parkinson's disease, and other neuropsychiatric indications.
Lin
Jian-Sheng
JS
Institut National de la Santé et de la Recherche Médicale, Integrative Physiology of Brain Arousal Systems, Claude Bernard University, Lyon, France.
Sergeeva
Olga A
OA
Haas
Helmut L
HL
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D006632:Histamine / Q000502:physiology*; D006633:Histamine Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D018100:Receptors, Histamine H3 / Q000502:physiology*; D012894:Sleep Stages / Q000187:drug effects / Q000502:physiology*; D012893:Sleep Wake Disorders / Q000188:drug therapy / Q000378:metabolism; D014851:Wakefulness / Q000187:drug effects / Q000502:physiology*
D006633:Histamine Antagonists; D018100:Receptors, Histamine H3; D006632:Histamine