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Article Abstract
H(3)R inverse agonists based on an aminopropoxy-phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse model of recognition memory.
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| http://dx.doi.org/10.1002/cmdc.200900055 | DOI Listing |
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Efficacy and Safety of Histamine H3 Receptor Antagonist/Inverse Agonist Including Betahistine for Schizophrenia: A Systematic Review and Meta-Analysis.
Neuropsychopharmacol Rep
September 2025
Department of Psychiatry, Fujita Health University School of Medicine, Toyoake, Aichi, Japan.
Aim: Whether histamine H3 receptor antagonists (H3R-ANTs)/inverse agonists (H3R-IAs) provides benefit for the treatment of schizophrenia remains unclear. This meta-analysis was conducted to address the above clinical question.
Methods: Cognitive Function Scale's composite score (primary), seven domains of cognitive function (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning/problem solving, and social cognition) score, University of California San Diego Performance-Based Skills Assessment score, psychopathology scales score, discontinuation rate, and incidence of individual adverse events were among the study outcomes.
Pitolisant alleviates brain network dysfunction and cognitive deficits in a mouse model of Alzheimer's disease.
Transl Psychiatry
April 2025
Brain Research Center and State Key Laboratory of Trauma and Chemical Poisoning, Third Military Medical University, Chongqing, 400038, China.
Histamine H receptor (HR) antagonists regulate histamine release that modulates neuronal activity and cognitive function. Although HR is elevated in Alzheimer's disease (AD) patients, whether HR antagonists can rescue AD-associated neural impairments and cognitive deficits remains unknown. Pitolisant is a clinically approved HR antagonist/inverse agonist that treats narcolepsy.
View Article and Find Full Text PDFHistamine H receptor blockade alleviates neuropathic pain through the regulation of glial cells activation.
Biomed Pharmacother
February 2025
Maj Institute of Pharmacology, Polish Academy of Sciences, Department of Neurochemistry, 12 Smetna Str., Krakow 31-343, Poland. Electronic address:
Neuropathic pain is a disorder affecting the somatosensory nervous system. However, this condition is also characterized by significant neuroinflammation, primarily involving CNS-resident non-neuronal cells. A promising target for developing new analgesics is histamine H receptor (HR); thus, we aimed to determine the influence of a novel HR antagonist/inverse agonist, E-98 (1-(7-(4-chlorophenoxy)heptyl)-3-methylpiperidine), on pain symptoms and glia activation in model of neuropathic pain in male mice (chronic constriction injury to the sciatic nerve).
View Article and Find Full Text PDFHistamine H receptor antagonists/inverse agonists: a patent review (October 2017 - December 2023) documenting progress.
Expert Opin Ther Pat
January 2025
Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Kraków, Poland.
Introduction: Histamine H receptor antagonists/inverse agonists, since the discovery of histamine H receptor (HR), are important ligands in the search for new potential drugs. The most interesting are CNS diseases as these receptors are mainly there present.
Areas Covered: The current review covers patent applications/patents that were published during the last 6 years (October 2017 - December 2023).
Tackling Neuroinflammation in Cognitive Disorders with Single-targeted and Multi-targeted Histamine H3 Receptor Modulators.
Curr Top Med Chem
November 2024
Department of Pharmacy and Biotechnology, University of Bologna, via Belmeloro 6, 40126, Bologna, Italy.
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.
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