title: Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases.
abstract: The potential contributions of the brain histaminergic system in neurodegenerative diseases, and the possiblity of histamine-targeting treatments is attracting considerable interests. The histamine H3 receptor (H3R) is expressed mainly in the central nervous system, and is, consequently, an attractive pharmacological target. Although recently described clinical trials have been disappointing in attention deficit hyperactivity disorder (ADHD) and schizophrenia (SCH), numerous H3R antagonists, including pitolisant, demonstrate potential in the treatment of narcolepsy, excessive daytime sleepiness associated with cognitive impairment, epilepsy, and Alzheimer's disease (AD). This review focuses on the recent preclinical as well as clinical results that support the relevance of H3R antagonists for the treatment of cognitive symptoms in neuropsychiatric diseases, namely AD, epilepsy and SCH. The review summarizes the role of histaminergic neurotransmission with focus on these brain disorders, as well as the effects of numerous H3R antagonists on animal models and humans.
authors.affiliation: Department of Pharmacology & Therapeutics, College of Medicine & Health Sciences, United Arab Emirates University, P.O. Box 17666, Al Ain, United Arab Emirates. Electronic address: bassem.sadek@uaeu.ac.ae.
authors.forename: Bassem
authors.initials: B
authors.lastname: Sadek
authors.affiliation: Department of Pharmacology & Therapeutics, College of Medicine & Health Sciences, United Arab Emirates University, P.O. Box 17666, Al Ain, United Arab Emirates.
authors.forename: Ali
authors.initials: A
authors.lastname: Saad
authors.affiliation: College of Pharmacy, Al Ain University of Science and Technology, Al Ain, United Arab Emirates.
authors.forename: Adel
authors.initials: A
authors.lastname: Sadeq
authors.affiliation: Department of Pharmacology & Therapeutics, College of Medicine & Health Sciences, United Arab Emirates University, P.O. Box 17666, Al Ain, United Arab Emirates.
authors.forename: Fakhreya
authors.initials: F
authors.lastname: Jalal
authors.affiliation: Institute of Pharmaceutical and Medicinal Chemistry, Heinrich Heine University, Universitaetsstr. 1, 40225 Düsseldorf, Germany.
authors.forename: Holger
authors.initials: H
authors.lastname: Stark
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy*; D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000503:physiopathology; D002986:Clinical Trials as Topic; D004195:Disease Models, Animal; D004827:Epilepsy / Q000188:drug therapy*; D006633:Histamine Antagonists / Q000008:administration & dosage / Q000627:therapeutic use*; D006801:Humans; D008568:Memory / Q000187:drug effects; D011968:Receptors, Histamine / Q000502:physiology; D018100:Receptors, Histamine H3 / Q000502:physiology*; D012559:Schizophrenia / Q000188:drug therapy*
chemical_list: D006633:Histamine Antagonists; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3
keywords: Brain histamine receptors; Cognitive symptoms; H3R Antagonists; Histamine; Neuropsychiatric diseases