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Volume 24, Issue 28
  • ISSN: 1568-0266
  • E-ISSN: 1873-4294

Abstract

Neuroinflammation is a process involved in a variety of central nervous system (CNS) diseases and is being increasingly recognized as a key mediator of cognitive impairments. Neuroinflammatory responses including glial activation, increased production of proinflammatory cytokines, and aberrant neuronal signaling, contribute to cognitive dysfunctions. Histamine is a key peripheral inflammatory mediator, but plays an important role in neuroinflammatory processes as well. The unique localization of histamine H receptor (HR) in the CNS along with the modulation of the release of other neurotransmitters its action on heteroreceptors on non-histaminergic neurons have led to the development of several HR ligands for various brain diseases. HR antagonists/inverse agonists have revealed potential to treat diverse neuroinflammatory CNS disorders, including neurodegenerative diseases, attention-deficit hyperactivity syndrome and schizophrenia. In this mini review, we provide a brief overview on the crucial involvement of the histaminergic transmission in the neuroinflammatory processes underlying these cognitive disorders, with a special focus on HR involvement. The anti-neuroinflammatory potential of single-targeted and multi-targeted HR antagonists/inverse agonists for the treatment of these conditions is discussed here.

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2024-11-21

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Tackling Neuroinflammation in Cognitive Disorders with Single-targeted and Multi-targeted Histamine H3 Receptor Modulators
Curr. Top. Med. Chem. 24, 2421 (2024); https://doi.org/10.2174/0115680266322294240816051818
/content/journals/ctmc/10.2174/0115680266322294240816051818
/content/journals/ctmc/10.2174/0115680266322294240816051818
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  • Article Type:     Review Article
Keyword(s): Cognitive disorders; Histamine H3 receptor; Multi-target compounds, Central nervous system; Neurodegenerative disease; Neuroinflammation

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