title: [The histaminergic system: a target for innovative treatments of cognitive deficits].
abstract: The central effects of histamine are mediated by H(1), H(2) and H(3) receptors. The H(3) receptor inhibits histamine release in brain. Therefore, H(3) receptor inverse agonists, by suppressing this brake, enhance histamine neuron activity. The histaminergic system plays a major role in cognition and H(3) receptor inverse agonists are expected to be a potential therapeutics for cognitive deficits of Alzheimer's disease (AD). They are eagerly awaited inasmuch as other treatments of the disease, such as tacrine or memantine, also enhance, through different mechanisms, histaminergic neurotransmission. An important loss of histaminergic neurons has been observed in AD. In contrast, levels of the histamine metabolite in the CSF of AD patients show that their global activity is decreased by only 25%. This indicates that activating histamine neurons in AD can be envisaged.
authors.affiliation: Laboratoire de Neurobiologie et Pharmacologie Moléculaire, Inserm U894, Centre de Psychiatrie et Neurosciences, Paris, France.
authors.forename: Mouhammad
authors.initials: M
authors.lastname: Motawaj
authors.forename: Aude
authors.initials: A
authors.lastname: Burban
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Davenas
authors.forename: Florence
authors.initials: F
authors.lastname: Gbahou
authors.forename: Raphaël
authors.initials: R
authors.lastname: Faucard
authors.forename: Séverine
authors.initials: S
authors.lastname: Morisset
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Arrang
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy* / Q000503:physiopathology; D000818:Animals; D003072:Cognition Disorders / Q000188:drug therapy / Q000209:etiology / Q000503:physiopathology; D016503:Drug Delivery Systems; D054314:Drug Inverse Agonism; D006632:Histamine / Q000378:metabolism*; D017442:Histamine Agonists / Q000494:pharmacology; D006801:Humans; D009474:Neurons / Q000378:metabolism; D018100:Receptors, Histamine H3 / Q000187:drug effects* / Q000378:metabolism
chemical_list: D017442:Histamine Agonists; D018100:Receptors, Histamine H3; D006632:Histamine