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

  title={Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases},
  author={Bassem Sadek and Ali Saad and Adel Shaban Sadeq and Fakhreya Yousuf Jalal and Holger Stark},
  journal={Behavioural Brain Research},
  • B. Sadek, A. Saad, H. Stark
  • Published 1 October 2016
  • Psychology, Biology, Medicine
  • Behavioural Brain Research
Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, Anxiety, Depression, and Sleep–Wake Cycle Disorder
Preclinical applications of selected H3R antagonists/inverse agonists and their pharmacological effects on cognitive impairment, anxiety, depression, and sleep–wake cycle disorders are presented.
Role of Neuroinflammation in Autism Spectrum Disorder and the Emergence of Brain Histaminergic System. Lessons Also for BPSD?
The hypothesis that central histamine (HA) plays a significant role in the regulation of neuroinflammatory processes of microglia functions in numerous neuropsychiatric diseases, i.e., ASD, AD, SCH, Schizophrenia, epilepsy, and BPSD is examined.
H3 antagonists and postoperative cognitive dysfunction
  • C. Krishnamurti
  • Biology
    Journal of anaesthesiology, clinical pharmacology
  • 2019
Since histamine (HA) was first synthesized in 1907 and isolated as a bacterial contaminant of an extract of ergot in 1910, its role in health and disease and its molecular mechanism of action have
Central histaminergic signalling, neural excitability and epilepsy
The findings from animal and clinical epilepsy research on the role of brain histamine and its receptors are summarized and current gaps in the research are identified.
Inhibition of Histamine H3 receptor Attenuates Neuroinflammation and Cognitive Impairments in Alzheimer’s Disease via activating CREB Pathway
A novel mechanism involving inflammatory regulating behind the therapeutic effect of thioperamide in AD is uncovered, suggesting the H3R antagonist thi operamide improved cognitive impairment in APP/PS1 Tg mice via modulation of the CREB-mediated gliosis and inflammation inhibiting, which contributed to Aβ clearance.
Histamine H3 receptor antagonist E177 attenuates amnesia induced by dizocilpine without modulation of anxiety-like behaviors in rats
The observed results suggested a possible contribution of H3Rs in the alteration of brain neurotransmitters that accompany neurodegenerative diseases, such as AD.
A Neurochemical Approach to the Search for Drugs for the Treatment of Symptoms of Alzheimer’s Disease
An analysis of the reciprocal influences of neurons involved in the rapid-eye-movement phase of sleep (REM sleep) under the conditions of changes in the concentrations of various neuromodulators that are characteristic of Alzheimer’s disease shows that the treatment with the antagonists of orexin receptors is not appropriate.
Simultaneous Blockade of Histamine H3 Receptors and Inhibition of Acetylcholine Esterase Alleviate Autistic-Like Behaviors in BTBR T+ tf/J Mouse Model of Autism
The initial overall results observed in an idiopathic ASD mice model show that E100 alleviated the assessed behavioral deficits and demonstrate that simultaneous targeting of brain histaminergic and cholinergic neurotransmissions is crucial for palliation of ASD-like features, albeit further in vivo assessments on its effects on brain levels of ACh as well as HA are still needed.
QSAR Modeling of Histamine H3R Antagonists/inverse Agonists as Future Drugs for Neurodegenerative Diseases
It is shown that the steric and hydrophobic properties of the H3R ligands are most important to reach good affinity, and pharmacokinetics should also be considered in future models to ensure good CNS penetration.


Histaminergic system in brain disorders: lessons from the translational approach and future perspectives
The role of histaminergic system in brain disorders, as well as the effects of different histamine antagonists on animal models and humans, are summarized.
The histamine H3 receptor: an attractive target for the treatment of cognitive disorders
The purpose of this review is to acquaint the reader with the current understanding of H3 receptor localization and function as a modulator of neurotransmitter release and its effects on cognitive processes, as well as to provide an update on selected H3 antagonists in various states of preclinical and clinical advancement.
Histamine H3 receptor antagonists in relation to epilepsy and neurodegeneration: a systemic consideration of recent progress and perspectives
Evidence for diverse mechanisms of antiepileptic and neuroprotective effects that were observed in various experimental models both in vitro and in vivo are reviewed with the aim of establishing a more reliable basis for the future use of H3 receptor antagonists, thus improving their utility in epilepsy and associated neurotoxicity.
Preclinical evaluation of non-imidazole histamine H3 receptor antagonists in comparison to atypical antipsychotics for the treatment of cognitive deficits associated with schizophrenia.
Results suggest H(3)R antagonists may have the potential to ameliorate CDS and chronic, but not acute, treatment with ABT-239 significantly improved spontaneous alternation impairments in MAM rats tested in cross-maze.
Reversal of oxidative stress by histamine H₃ receptor-ligands in experimental models of schizophrenia.
The results of the present study revealed that H3R-antagonists possess antioxidant activity and could serve with dual mechanism by supplementing antioxidant needs of SCZ and at the same time controlling symptoms ofSCZ.
The role of histamine H4 receptor in immune and inflammatory disorders
The available data strongly point to the H4 receptor as a novel target for the pharmacological modulation of histamine‐transferred immune signals and offer an optimistic perspective for the therapeutic exploitation of this promising new drug target in inflammatory disorders.