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
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Kv4.2 mediates histamine modulation of preoptic neuron activity and body temperature. [PDF]
PLoS ONE, 2011 Histamine regulates arousal, circadian rhythms, and thermoregulation. Activation of H3 histamine receptors expressed by preoptic GABAergic neurons results in a decrease of their firing rate and hyperthermia.
Jasmine Sethi +2 more
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Calyx and dimorphic neurons of mouse Scarpa's ganglion express histamine H3 receptors [PDF]
BMC Neuroscience, 2009 Background Histamine-related drugs are commonly used in the treatment of vertigo and related vestibular disorders. The site of action of these drugs however has not been elucidated yet.
Zucca Gianpiero +5 more
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The Histamine H3 Receptor: Structure, Pharmacology, and Function [PDF]
Molecular Pharmacology, 2016 Among the four G protein-coupled receptors (H1-H4) identified as mediators of the biologic effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclusive expression in the nervous system and the large variety of isoforms generated by alternative splicing of the corresponding mRNA.
Ana-Maricela García-Gálvez +4 more
openaire +4 more sources
The evidence for histamine H3 receptor-mediated endothelium-dependent relaxation in isolated rat aorta [PDF]
Mediators of Inflammation, 1995 The presence of histamine H3 receptors was evaluated on the rat aorta endothelium. In the presence of pyrilamine (1 nM, 7 nM, 10 nM) or thioperamide (1 nM, 10 nM, 30 nM) the concentration–response curve for histamine-induced (0.1 nM − 0.01 mM ...
D. M. Djuric, I. Z. Andjelkovic
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Changes in Histamine Receptors (H1, H2, and H3) Expression in Rat Medial Vestibular Nucleus and Flocculus after Unilateral Labyrinthectomy: Histamine Receptors in Vestibular Compensation. [PDF]
PLoS ONE, 2013 Vestibular compensation is the process of behavioral recovery following peripheral vestibular lesion. In clinics, the histaminergic medicine is the most widely prescribed for the treatment of vertigo and motion sickness, however, the molecular mechanisms
Liuqing Zhou +6 more
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Multiple Targeting Approaches on Histamine H3 Receptor Antagonists
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
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Molecules, 2018 H3 receptors present on histaminergic and non-histaminergic neurons, act as autoreceptors or heteroreceptors controlling neurotransmitter release and synthesis.
Roman Guryn +6 more
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Role of histamine H3 receptor in glucagon‐secreting αTC1.6 cells [PDF]
FEBS Open Bio, 2015 Pancreatic α‐cells secrete glucagon to maintain energy homeostasis. Although histamine has an important role in energy homeostasis, the expression and function of histamine receptors in pancreatic α‐cells remains unknown.
Tadaho Nakamura +7 more
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Integrative role of the histaminergic system in feeding and taste perception [PDF]
Frontiers in Systems Neuroscience, 2012 Feeding behavior is regulated by a complex interplay of many endogenous substances, such as peptides and neurotransmitters in the central nervous system.
Tomoko eIshizuka, Atsushi eYamatodani
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