Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands. [PDF]
PLoS ONE, 2019 In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
David Schaller +3 more
doaj +5 more sources
Effects of Methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to an open-space spatial maze [PDF]
Frontiers in Systems Neuroscience, 2012 The role of the histamine H3 receptor in anxiety is controversial, due to limitations in drug selectivity and limited validity of behavioral tests in previous studies. When exposed to an empty open field, Wistar rats spent more time in the outer area and
Abdel eEnnaceur +4 more
doaj +2 more sources
Multiple Targeting Approaches on Histamine H3 Receptor Antagonists [PDF]
Frontiers in Neuroscience, 2016 With the very recent market approval of pitolisant (Wakix®), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been
Mohammad eKhanfar +5 more
doaj +2 more sources
Novel chalcone-based fluorescent human histamine H3 receptor ligands as pharmacological tools [PDF]
Frontiers in Systems Neuroscience, 2012 Novel fluorescent chalcone-based ligands at human histamine H3 receptors (hH3R) have been designed, synthesized and characterized. Compounds described are non-imidazole analogues of ciproxifan with a tetralone motif. Tetralones as chemical precursors and
Holger eStark
doaj +3 more sources
Histamine H3 receptor inverse agonists/antagonists influence intra-regional cortical activity and inter-regional synchronization during resting state: an exploratory cortex-wide imaging study in mice [PDF]
Molecular BrainThe histaminergic system plays a key role in modulating learning and memory, wakefulness, and energy balance. Histamine H3 receptors constitutively inhibit the synthesis and release of histamine and other neurotransmitters. Therefore, H3 receptor inverse
Sentaro Kaita +3 more
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Histamine, histamine H3 receptor, and alcohol use disorder. [PDF]
Br J Pharmacol, 2020 Peer ...
Panula P.
europepmc +3 more sources
The Impact of H1–H4 Receptor Antagonists on the Levels of Selected Oxidative Stress Markers in Liver and Muscle Tissue in an Animal Model of Colitis [PDF]
PharmaceuticalsBackground/Objectives: The global prevalence and incidence of inflammatory bowel diseases have risen in the past two decades. Among them, Crohn’s disease and ulcerative colitis are still challenging to treat due to vascular and proliferative alterations.
Bartosz Bogielski +16 more
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Letter to the Editor in Response to “Efficacy and Safety of Histamine H3 Receptor Antagonist/Inverse Agonist Including Betahistine for Schizophrenia: A Systematic Review and Meta‐Analysis” by Nishii et al. [PDF]
Neuropsychopharmacology ReportsMuhammad Farhan
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Interaction of Central Glutamatergic and Histaminergic Systems on Food Intake Regulation in Layer Chickens [PDF]
Archives of Razi Institute, 2021 This study purposed to discover the connection between the central glutamatergic and histaminergic systems on feeding behavior in layer chickens. In the first experiment, chicks obtained intracerebroventricular (ICV) injections of saline (control ...
M Mobarhan Fard +3 more
doaj +1 more source
Loss of Melanopsin Photoreception and Antagonism of the Histamine H3 Receptor by Ciproxifan Inhibit Light-Induced Sleep in Mice [PDF]
, 2015 Light has direct effects on sleep and wakefulness causing arousal in diurnal animals and sleep in nocturnal animals. In the present study, we assessed the modulation of light-induced sleep by melanopsin and the histaminergic system by exposing mice to ...
Colas, Damien +4 more
core +18 more sources