Histamine H3-receptors and sleep-wake regulation.
Summary of "Histamine H3-receptors and sleep-wake regulation."
The histaminergic system fulfills a major role in the maintenance of waking. Histaminergic neurons are exclusively located in the posterior hypothalamus from where they project to most areas of the central nervous system. The histamine H3-receptors are autoreceptors damping histamine synthesis, the firing frequency of histamine neurons and the release of histamine from axonal varicosities. Importantly, this action extends also 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 H3-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.
1 Universite Claude Bernard, Lyon, France;
This article was published in the following journal.
Name: The Journal of pharmacology and experimental therapeutics
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/20864502
- DOI: http://dx.doi.org/10.1124/jpet.110.170134
Medical and Biotech [MESH] Definitions
Movements or behaviors associated with sleep, sleep stages, or partial arousals from sleep that may impair sleep maintenance. Parasomnias are generally divided into four groups: arousal disorders, sleep-wake transition disorders, parasomnias of REM sleep, and nonspecific parasomnias. (From Thorpy, Sleep Disorders Medicine, 1994, p191)
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
Sleep-wake Transition Disorders
Parasomnias characterized by behavioral abnormalities that occur during the transition between wakefulness and sleep (or between sleep and wakefulness).
Histamine H3 Antagonists
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP DISORDERS and MEMORY DISORDERS.
Receptors, Histamine H3
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
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