Results 1 to 10 of about 13,967 (254)

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, Stefanie Hagenow, Holger Stark, Gerhard Wolber   +3 more
doaj   +8 more sources

Assessment of [125I]WYE-230949 as a novel histamine H3 receptor radiopharmaceutical. [PDF]

PLoS ONE, 2014
Histamine H3 receptor therapeutics have been proposed for several diseases such as schizophrenia, attention deficit hyperactivity disorder, Alzheimer's disease and obesity.
David Y Lewis, Sue Champion, David Wyper, Deborah Dewar, Sally Pimlott   +4 more
doaj   +3 more sources

H3 Histamine Receptor–Mediated Activation of Protein Kinase Cα Inhibits the Growth of Cholangiocarcinoma In vitro and In vivo [PDF]

, 2009
Histamine regulates functions via four receptors (HRH1, HRH2, HRH3, and HRH4). The D-myo-inositol 1,4,5-trisphosphate (IP(3))/Ca(2+)/protein kinase C (PKC)/mitogen-activated protein kinase pathway regulates cholangiocarcinoma growth.
Heather Francis, Paolo Onori, Eugenio Gaudio, Antonio Franchitto, Sharon DeMorrow, Julie Venter, Shelley Kopriva, Guido Carpino, Romina Mancinelli, Mellanie White, Fanyin Meng, Antonella Vetuschi, Roberta Sferra, Gianfranco Alpini   +13 more
openalex   +4 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, Rushdie M.A. ABUHAMDAH, Natasha L Lethbridge, Paul L Chazot, Ruan evan Rensburg   +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, Anna eAffini, Kiril eLutsenko, Katarina eNikolic, Stefania eButini, Holger eStark   +5 more
doaj   +2 more sources

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, Zampini Valeria, Botta Laura, Tritto Simona, Valli Paolo, Masetto Sergio   +5 more
doaj   +2 more sources

Multitargeting Histamine H₃ Receptor Ligands among Acetyl- and Propionyl-Phenoxyalkyl Derivatives. [PDF]

Molecules, 2023
Łażewska D, Kaleta M, Zaręba P, Godyń J, Dubiel M, Honkisz-Orzechowska E, Doroz-Płonka A, Więckowska A, Stark H, Kieć-Kononowicz K.   +9 more
europepmc   +3 more sources

Heteroreceptor Complexes Formed by Dopamine D1, Histamine H3, and N-Methyl-D-Aspartate Glutamate Receptors as Targets to Prevent Neuronal Death in Alzheimer’s Disease [PDF]

, 2016
Alzheimer’s disease (AD) is a neurodegenerative disorder causing progressive memory loss and cognitive dysfunction. Anti-AD strategies targeting cell receptors consider them as isolated units. However, many cell surface receptors cooperate and physically
Mar Rodríguez-Ruiz, Estefanía Moreno, David Moreno‐Delgado, Gemma Navarro, Josefa Mallol, Antonio Cortés, Carme Lluı́s, Enric I. Canela, Vicent Casadó, Peter J. McCormick, Rafael Franco   +10 more
openalex   +4 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 Brain
The 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, Yoshikazu Morishita, Kenta Kobayashi, Hiroshi Nomura   +3 more
doaj   +2 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]

Pharmaceuticals
Background/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, Katarzyna Michalczyk, Wojciech Gębski, Katarzyna Rozpędek, Elżbieta Szulińska, Bartosz Tempka, Aleksandra Zorychta, Elżbieta Chełmecka, Ewa Kaczmar, Piotr Głodek, Jakub John, Kamil Nikiel, Bronisława Skrzep-Poloczek, Jerzy Jochem, Katarzyna Kieć-Kononowicz, Dorota Łażewska, Dominika Stygar   +16 more
doaj   +2 more sources