Journal of Pharmacological Sciences, 2005 The second-generation histamine-H1-receptor antagonists, such as epinastine and cetirizine, are used as non-sedating antihistamines for treating allergic symptoms due to their poor ability to penetrate blood-brain barrier.
Junzo Kamei +4 more
doaj +1 more source
Novel chalcone-based fluorescent human histamine H 3 receptor ligands as pharmacological tools [PDF]
, 2012 Novel fluorescent chalcone-based ligands at human histamine H(3) receptors (hH(3)R) have been designed, synthesized, and characterized. Compounds described are non-imidazole analogs of ciproxifan with a tetralone motif.
Tomasch, Miriam +3 more
core +1 more source
Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]
, 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.
Hagenow, Stefanie +3 more
core +2 more sources
Histamine antagonists promote cancer immunosurveillance
OncoImmunology, 2023 Recently, a cellular mini-immune system comprising infinitely expandable dendritic cells and T cells led to the discovery that histamine receptor H1 antagonists act on T cells to stimulate their proliferation and polarization toward a Th1/Tc1 phenotype ...
Peng Liu, Guido Kroemer, Oliver Kepp
doaj +1 more source
Histamine receptors in GtoPdb v.2021.3 [PDF]
, 2021 Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [80, 173]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [80]. The human and rat
Chazot, Paul +19 more
core +2 more sources
Histamine H1 receptor antagonist attenuates catecholamine surge and organ injury after severe burns
Frontiers in Endocrinology, 2023 Severe burns induce a catecholamine surge, causing severe damage to the organism and raising the possibility of multisystem organ failure. Few strategies are generally acceptable to reduce catecholamine surge and organ injury post-burn.
Jizhuang Wang +8 more
doaj +1 more source
Cetirizine a histamine H1 receptor antagonist improves viral myocarditis [PDF]
Journal of Inflammation, 2010 We showed that mast cells played a critical role in the progression of heart failure induced by pressure overload and viral myocarditis in mice. In this study, we investigated the effect of cetirizine, a selective H1 receptor antagonist, on experimental viral myocarditis induced by encephalomyocarditis (EMC) virus.Four-week-old inbred male DBA/2 mice ...
Yamamoto Kanjo +2 more
openaire +3 more sources
Influence of mirtazapine on salivary cortisol in depressed patients [PDF]
, 2003 Unlike other antidepressants, mirtazapine does not inhibit the reuptake of norepinephrine or serotonin but acts as an antagonist at presynaptic alpha(2)-receptors, at postsynaptic 5-HT2 and 5-HT3 receptors, and at histaminergic H1 receptors. Furthermore,
Baghai, Thomas C. +3 more
core +1 more source
Histamine stimulates the proliferation of small and large cholangiocytes by activation of both IP3/Ca2+ and cAMP-dependent signaling mechanisms [PDF]
, 2012 Although large cholangiocytes exert their functions by activation of cyclic adenosine 3',5'-monophosphate (cAMP), Ca(2+)-dependent signaling regulates the function of small cholangiocytes. Histamine interacts with four receptors, H1-H4HRs.
Fanyin Meng +15 more
core +1 more source
Histamine and Histamine H4 Receptor Promotes Osteoclastogenesis in Rheumatoid Arthritis. [PDF]
, 2017 Histamine H4 receptor (H4R) has immune-modulatory and chemotaxic effects in various immune cells. This study aimed to determine the osteoclastogenic role of H4R in rheumatoid arthritis (RA).
Firestein, Gary S +5 more
core +1 more source