Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases

Bassem Sadek, Ali Saad, Adel Sadeq, Fakhreya Jalal, Holger Stark

Research output: Contribution to journalReview articlepeer-review

121 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)415-430
Number of pages16
JournalBehavioural Brain Research
Publication statusPublished - Oct 1 2016


  • Brain histamine receptors
  • Cognitive symptoms
  • H3R Antagonists
  • Histamine
  • Neuropsychiatric diseases

ASJC Scopus subject areas

  • Behavioral Neuroscience


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