Results 1 to 10 of about 467,605 (318)

Activation of carbonic anhydrase isoforms involved in modulation of emotional memory and cognitive disorders with histamine agonists, antagonists and derivatives [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Carbonic anhydrases (CAs, EC 4.2.1.1) activators were shown to be involved in memory enhancement and learning in animal models of cognition. Here we investigated the CA activating effects of a large series of histamine based compounds, including ...
Gustavo Provensi, Alessio Nocentini, Maria Beatrice Passani, Patrizio Blandina, Claudiu T. Supuran   +4 more
doaj   +3 more sources

Revisiting Preclinical Observations of Several Histamine H3 Receptor Antagonists/Inverse Agonists in Cognitive Impairment, Anxiety, Depression, and Sleep–Wake Cycle Disorder

Frontiers in Pharmacology, 2022
A relationship appears to exist between dysfunction of brain histamine (HA) and various neuropsychiatric brain disorders. The possible involvement of brain HA in neuropathology has gained attention recently, and its role in many (patho)physiological ...
Mera Alhusaini, Mera Alhusaini, Nermin Eissa, Nermin Eissa, Nermin Eissa, Ali K. Saad, Ali K. Saad, Rami Beiram, Rami Beiram, Bassem Sadek, Bassem Sadek   +10 more
doaj   +2 more sources

Structural insights into the agonists binding and receptor selectivity of human histamine H4 receptor

Nature Communications, 2023
Histamine is a biogenic amine that participates in allergic and inflammatory processes by stimulating histamine receptors. The histamine H4 receptor (H4R) is a potential therapeutic target for chronic inflammatory diseases such as asthma and atopic ...
Dohyun Im, Jun-ichi Kishikawa, Yuki Shiimura, Hiromi Hisano, Akane Ito, Yoko Fujita-Fujiharu, Yukihiko Sugita, Takeshi Noda, Takayuki Kato, Hidetsugu Asada, So Iwata   +10 more
doaj   +2 more sources

Histamine 2/3 receptor agonists alleviate perioperative neurocognitive disorders by inhibiting microglia activation through the PI3K/AKT/FoxO1 pathway in aged rats

Journal of Neuroinflammation, 2020
Background Microglia, the principal sentinel immune cells of the central nervous system (CNS), play an extensively vital role in neuroinflammation and perioperative neurocognitive disorders (PND).
Yi-Nan Chen, Huan-Huan Sha, Yi-Wei Wang, Qin Zhou, Piplu Bhuiyan, Na-Na Li, Yan-Ning Qian, Hong-Quan Dong   +7 more
doaj   +2 more sources

The Roles of Cardiovascular H2-Histamine Receptors Under Normal and Pathophysiological Conditions

Frontiers in Pharmacology, 2021
This review addresses pharmacological, structural and functional relationships among H2-histamine receptors and H1-histamine receptors in the mammalian heart.
Joachim Neumann, Uwe Kirchhefer, Stefan Dhein, Britt Hofmann, Ulrich Gergs   +4 more
doaj   +2 more sources

Isoform-Specific Biased Agonism of Histamine H3 Receptor Agonists [PDF]

Molecular Pharmacology, 2017
The human histamine H3 receptor (hH3R) is subject to extensive gene splicing that gives rise to a large number of functional and nonfunctional isoforms. Despite the general acceptance that G protein-coupled receptors can adopt different ligand-induced conformations that give rise to biased signaling, this has not been studied for the H3R; further, it ...
Darren M, Riddy, Anna E, Cook, Natalie A, Diepenhorst, Sanja, Bosnyak, Ryan, Brady, Clotilde, Mannoury la Cour, Elisabeth, Mocaer, Roger J, Summers, William N, Charman, Patrick M, Sexton, Arthur, Christopoulos, Christopher J, Langmead   +11 more
openaire   +3 more sources

Pathophysiological Roles of Histamine Receptors in Cancer Progression: Implications and Perspectives as Potential Molecular Targets

Biomolecules, 2021
High levels of histamine and histamine receptors (HRs), including H1R~H4R, are found in many different types of tumor cells and cells in the tumor microenvironment, suggesting their involvement in tumor progression.
Phuong Linh Nguyen, Jungsook Cho
doaj   +2 more sources

PKC-dependent Phosphorylation of the H1 Histamine Receptor Modulates TRPC6 Activity [PDF]

Cells, 2014
Transient receptor potential canonical 6 (TRPC6) is a cation selective, DAG-regulated, Ca2+-permeable channel activated by the agonists of Gq-protein-coupled heptahelical receptors.
Xingjuan Chen, Christian Egly, Ashley M. Riley, Wennan Li, Paul Tewson, Thomas E. Hughes, Anne Marie Quinn, Alexander G. Obukhov   +7 more
doaj   +4 more sources

Histamine therapeutic efficacy in metastatic melanoma: Role of histamine H4 receptor agonists and opportunity for combination with radiation

OncoTarget, 2017
The aims of the work were to improve our knowledge of the role of H4R in melanoma proliferation and assess in vivo the therapeutic efficacy of histamine, clozapine and JNJ28610244, an H4R agonist, in a preclinical metastatic model of melanoma ...
N Massari, Melisa B. Nicoud, Lorena Sambuco, G. Cricco, Diego J. Martinel Lamas, María V. Herrero Ducloux, Horacio Blanco, Elena Rivera, Vanina A. Medina   +8 more
openalex   +3 more sources

β2-Adrenergic Receptor-Mediated Histamine H1 Receptor Down-Regulation: Another Possible Advantage of β2 Agonists in Asthmatic Therapy

Journal of Pharmacological Sciences, 2004
To clarify heterologous regulation of a receptor is important in considering medication. Histamine constricts the airway smooth muscle through the action to the H1 receptor (H1R), which contributes to asthma.
Nozomi Kawakami, Katsuhiro Miyoshi, Shuhei Horio, Hiroyuki Fukui   +3 more
doaj   +3 more sources