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Histamine receptors

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https://www.readbyqxmd.com/read/28728999/histamine-h2-receptor-stimulation-up-regulates-th2-chemokine-ccl17-production-in-human-m2a-macrophages
#1
Susanne Mommert, Karl Gregor, Kristine Rossbach, Katrin Schaper, Torsten Witte, Ralf Gutzmer, Thomas Werfel
Stimulation of the histamine H2 receptor significantly increased CCL17 production in human monocyte derived M2a macrophages. These results may be helpful to identify novel therapeutical target structures in diseases driven at least in part by histamine.
July 17, 2017: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28728517/using-molecular-dynamics-for-the-refinement-of-atomistic-models-of-gpcrs-by-homology-modeling
#2
Cecylia S Lupala, Bahareh Rasaeifar, Patricia Gomez-Gutierrez, Juan J Perez
Despite GPCRs share a common seven helix bundle, analysis of the diverse crystallographic structures available reveal specific features that might be relevant for ligand design. Despite the number of crystallographic structures of GPCRs is steadily increasing, there are still challenges that hamper the availability of new structures. In the absence of a crystallographic structure, homology modelling remains one of the important techniques for constructing 3D models of proteins. In the present study we investigated the use of molecular dynamics simulations for the refinement of GPCRs models constructed by homology modeling...
July 20, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28728310/the-effect-of-h2-receptor-antagonist-in-acid-inhibition-and-its-clinical-efficacy
#3
REVIEW
Young Kwang Shim, Nayoung Kim
The first histamine H2 receptor antagonists (H2RAs) were developed in the early 1970s. They played a dominant role in treating peptic ulcer disease and gastroesophageal reflux disease (GERD). H2RAs block the production of acid by H(+), K(+)-ATPase at the parietal cells and produce gastric luminal anacidity for varying periods. H2RAs are highly selective, and they do not affect H1 receptors. Moreover, they are not anticholinergic agents. Sequential development of H2RAs, proton pump inhibitors (PPIs), and discovery of Helicobacter pylori infection changed the paradigm of peptic ulcer disease with marked decrease of morbidity and mortality...
July 25, 2017: Korean Journal of Gastroenterology, Taehan Sohwagi Hakhoe Chi
https://www.readbyqxmd.com/read/28722302/a-novel-neurological-function-of-rice-bran-a-standardized-rice-bran-supplement-promotes-non-rapid-eye-movement-sleep-in-mice-through-histamine-h1-receptors
#4
Min Young Um, Sojin Kim, Young-Ho Jin, Minseok Yoon, Hyejin Yang, Jaekwang Lee, Jonghoon Jung, Yoshihiro Urade, Zhi-Li Huang, Sangoh Kwon, Suengmok Cho
SCOPE: Although rice bran has been shown to be associated with a wide spectrum of health benefits, to date, there are no reports on its effects on sleep. We investigated the effect of rice bran on sleep and the mechanism underlying this effect. METHODS AND RESULTS: Electroencephalography was used to evaluate the effects of standardized rice bran supplement (RBS) and doxepin hydrochloride (DH), a histamine H1 receptor (H1 R) antagonist used as a positive control, on sleep in mice...
July 19, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28711557/postprandial-hypoglycemia-complication-of-peptic-ulcer-surgery
#5
Adnan Haider, James K Burks, H I Cheema, Angel Tejada
OBJECTIVE: Billroth II procedures (gastrojejunostomy with vagotomy) are seldom performed now, but were popular before the advent of histamine 2 (H2) receptor blockers and proton pump inhibitors (PPIs). Such procedures can be a cause of late postprandial hypoglycemia. METHOD: Formal evaluation, discussion of postprandial hypoglycemia. RESULTS: We present a case of an 85-year-old man who presented to the Endocrinology clinic with a complaint of "fainting spells following large meals...
July 12, 2017: American Journal of Medicine
https://www.readbyqxmd.com/read/28708434/epithelial-cells-induce-a-cyclooxygenase-1-dependent-endogenous-reduction-in-airway-smooth-muscle-contractile-phenotype
#6
Michael J O'Sullivan, Elizabeth Gabriel, Alice Panariti, Chan Y Park, Gijs Ijpma, Jeffrey J Fredberg, Anne-Marie Lauzon, James G Martin
Airway smooth muscle (ASM) cells are phenotypically regulated to exist in either a proliferative or a contractile state. However the influence of other airway structural cell types on ASM cell phenotype is largely unknown. Although epithelial cells are known to drive ASM proliferation, their effects on the contractile phenotype are uncertain. In the current study we tested the hypothesis that epithelial cells reduce the contractile phenotype of ASM cells. To do so, we measured force production by traction microscopy, gene and protein expression as well as calcium release by Fura-2 ratiometric imaging...
July 14, 2017: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/28701542/group-iv-nociceptors-develop-axonal-chemical-sensitivity-during-neuritis-and-following-treatment-of-the-sciatic-nerve-with-vinblastine
#7
Rosann M Govea, Mary F Barbe, Geoffrey M Bove
We have previously shown that nerve inflammation (neuritis) and transient vinblastine application lead to axonal mechanical sensitivity in nociceptors innervating deep structures. We have also shown that these treatments reduce axonal transport, and proposed that this leads to functional accumulation of mechanically sensitive channels in the affected part of the axons. While informing the etiology of mechanically induced pain, axonal mechanical sensitivity does not address the common report of ongoing radiating pain during neuritis, which could be secondary to the provocation of axonal chemical sensitivity...
July 12, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28699796/utilization-and-safety-of-proton-pump-inhibitors-and-histamine-2-receptor-antagonists-in-children-and-adolescents-an-observational-cohort-study
#8
A Ruigómez, S Johansson, P Nagy, L A García Rodríguez
BACKGROUND: Little is known about the use of acid-suppressing treatments and related safety events in children. OBJECTIVE: This study compared patient characteristics and safety outcomes among children prescribed acid-suppressing drugs for the first time. METHODS: The Health Improvement Network was used to determine the characteristics of children prescribed a proton pump inhibitor (PPI; esomeprazole or another PPI) or a histamine-2 receptor antagonist (H2RA) by UK primary care physicians between October 2009 and September 2012...
July 21, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28695272/cardiovascular-effects-of-histamine-in-three-widely-diverse-species-of-reptiles
#9
Nini Skovgaard, Augusto S Abe, Edwin W Taylor, Tobias Wang
The cardiovascular system of vertebrates is regulated by a vast number of regulatory factors, including histamine. In pythons, histamine induces a strong tachycardia and dilates the systemic vasculature, which resembles the cardiovascular response to the elevated metabolic rate during digestion. In fact, there is an important role of increased histaminergic tone on the heart during the initial 24 h of digestion in pythons. Whilst the cardiovascular effects of histamine are well studied in pythons, little is known about the effects in other groups of reptiles...
July 10, 2017: Journal of Comparative Physiology. B, Biochemical, Systemic, and Environmental Physiology
https://www.readbyqxmd.com/read/28690192/suppression-of-osteogenic-differentiation-in-mesenchymal-stem-cells-from-patients-with-ossification-of-the-posterior-longitudinal-ligament-by-a-histamine-2-receptor-antagonist
#10
Xizhe Liu, Gentaro Kumagai, Kanichiro Wada, Toshihiro Tanaka, Taku Fujita, Ayako Sasaki, Ken-Ichi Furukawa, Yasuyuki Ishibashi
Mesenchymal stem cells (MSCs) in ossification of the posterior longitudinal ligament (OPLL) patients have a high propensity toward osteogenesis. Histamine receptor H2 (H2R) antagonists (H2 blockers) like famotidine decrease ossification in patients, by an unclear mechanism. To confirm that MSCs express H2R and to clarify how H2 blockers suppress osteogenic differentiation, we used spinal-ligament MSCs from patients with OPLL or with cervical spondylotic myelopathy (CSM) (control). The MSCs were treated with 10, 30, or 100nM famotidine for 7 or 21 days...
July 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28688766/ligands-of-histamine-receptors-modulate-acid-sensing-ion-channels
#11
V Y Shteinikov, A S Korosteleva, T B Tikhonova, N N Potapieva, D B Tikhonov
Recently we found that synthetic compounds containing amino group linked to hydrophobic or aromatic moiety are potent modulators of the proton-gated channels (ASICs). These structures have clear similarity with ligands of histamine receptors. We have also demonstrated that histamine potentiates homomeric ASIC1a by shifting its activation dependence to less acidic conditions. In the present work the action of a series of histamine receptors ligands on recombinant ASIC1a and ASIC2a was characterized. Two types of action were found for ASIC1a...
July 5, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28687195/%C3%AE-2-microglobulin-elicits-itch-related-responses-in-mice-through-the-direct-activation-of-primary-afferent-neurons-expressing-transient-receptor-potential-vanilloid-1
#12
Tsugunobu Andoh, Takahito Maki, Sikai Li, Daisuke Uta
Uremic pruritus is an unpleasant symptom in patients undergoing hemodialysis, and the underlying mechanisms remain unclear. β2-Microglobulin (β2-MG) is well-known as an MHC class I molecule and its level is increased in the plasma of patients undergoing hemodialysis. In this study, we investigated whether β2-MG was a pruritogen in mice. Intradermal injections of β2-MG into the rostral back induced scratching in a dose-dependent manner. Intradermal injection of β2-MG into the cheek also elicited scratching, but not wiping...
July 4, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28686675/management-of-flu-like-syndrome-with-cetirizine-in-patients-with-relapsing-remitting-multiple-sclerosis-during-therapy-with-interferon-beta-results-of-a-randomized-cross-over-placebo-controlled-pilot-study
#13
Doriana Landi, Maria Albanese, Fabio Buttari, Fabrizia Monteleone, Laura Boffa, Silvia Rossi, Caterina Motta, Elisa Puma, Diego Centonze
BACKGROUND: Flu-like syndrome (FLS) is a common adverse event experienced by patients with relapsing-remitting multiple sclerosis (RRMS) treated with interferon beta (IFNβ). FLS can lead to poor treatment adherence and early IFNβ discontinuation. The involvement of interleukin-6 (IL-6) in the occurrence of FLS has been suggested. We hypothesized that cetirizine, a second-generation histamine H1 receptor antagonist able to reduce the levels of IL-6, might improve IFNβ-induced FLS. METHODS: We conducted a pilot, cross-over, randomized, placebo-controlled, double-blind study to evaluate the efficacy of cetirizine 10 mg added after each IFNβ injection to the standard of care for FLS (acetaminophen or nonsteroidal anti-inflammatory drugs) on FLS in patients with RRMS treated with IFNβ...
2017: PloS One
https://www.readbyqxmd.com/read/28684785/identification-of-histamine-h3-receptor-ligands-using-a-new-crystal-structure-fragment-based-method
#14
Ida Osborn Frandsen, Michael W Boesgaard, Kimberley Fidom, Alexander S Hauser, Vignir Isberg, Hans Bräuner-Osborne, Petrine Wellendorph, David E Gloriam
Virtual screening offers an efficient alternative to high-throughput screening in the identification of pharmacological tools and lead compounds. Virtual screening is typically based on the matching of target structures or ligand pharmacophores to commercial or in-house compound catalogues. This study provides the first proof-of-concept for our recently reported method where pharmacophores are instead constructed based on the inference of residue-ligand fragments from crystal structures. We demonstrate its unique utility for G protein-coupled receptors, which represent the largest families of human membrane proteins and drug targets...
July 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28684600/frontline-science-corticotropin-releasing-factor-receptor-subtype-1-is-a-critical-modulator-of-mast-cell-degranulation-and-stress-induced-pathophysiology
#15
Saravanan Ayyadurai, Amelia J Gibson, Susan D'Costa, Elizabeth L Overman, Laura J Sommerville, Ashwini C Poopal, Emily Mackey, Yihang Li, Adam J Moeser
Life stress is a major risk factor in the onset and exacerbation of mast cell-associated diseases, including allergy/anaphylaxis, asthma, and irritable bowel syndrome. Although it is known that mast cells are highly activated upon stressful events, the mechanisms by which stress modulates mast cell function and disease pathophysiology remains poorly understood. Here, we investigated the role of corticotropin-releasing factor receptor subtype 1 (CRF1) in mast cell degranulation and associated disease pathophysiology...
July 6, 2017: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/28680175/outcome-after-discontinuation-of-proton-pump-inhibitors-at-a-residential-care-site-quality-improvement-project
#16
Candy Lee, Anita Lo, Kiran Ubhi, Michael Milewski
BACKGROUND: Increased prescribing of proton pump inhibitors (PPIs) in the past few decades can be attributed mainly to long-term use of this type of therapy. Recent evidence indicates signals of harm associated with long-term use of PPIs, such as increased risk of Clostridium difficile infection, recurrence of C. difficile infection, and fracture. A few studies have assessed the effectiveness of step-down management of patients receiving long-term PPI therapy in ambulatory care settings...
May 2017: Canadian Journal of Hospital Pharmacy
https://www.readbyqxmd.com/read/28676480/risk-of-death-among-users-of-proton-pump-inhibitors-a-longitudinal-observational-cohort-study-of-united-states-veterans
#17
Yan Xie, Benjamin Bowe, Tingting Li, Hong Xian, Yan Yan, Ziyad Al-Aly
OBJECTIVE: Proton pump inhibitors (PPIs) are widely used, and their use is associated with increased risk of adverse events. However, whether PPI use is associated with excess risk of death is unknown. We aimed to examine the association between PPI use and risk of all-cause mortality. DESIGN: Longitudinal observational cohort study. SETTING: US Department of Veterans Affairs. PARTICIPANTS: Primary cohort of new users of PPI or histamine H2 receptor antagonists (H2 blockers) (n=349 312); additional cohorts included PPI versus no PPI (n=3 288 092) and PPI versus no PPI and no H2 blockers (n=2 887 030)...
July 4, 2017: BMJ Open
https://www.readbyqxmd.com/read/28674249/effects-of-gintonin-enriched-fraction-in-an-atopic-dermatitis-animal-model-involvement-of-autotaxin-regulation
#18
Byung-Hwan Lee, Ho-Kyoung Kim, Minhee Jang, Hyeon-Joong Kim, Sun-Hye Choi, Sung-Hee Hwang, Hyoung-Chun Kim, Hyewhon Rhim, Ik-Hyun Cho, Seung-Yeol Nah
Ginseng extract has been used for prevention of atopic dermatitis (AD) in experimental animal models. However, little is known about its active ingredients and the molecular mechanisms underlying its anti-AD effects. Recently, we isolated a unique lysophosphatidic acid (LPA) receptor ligand, gintonin, from ginseng. Gintonin, the glycolipoprotein fraction of ginseng, contains LPAs, mainly LPA C18 : 2 with other minor lysophospholipid components. A line of evidence showed that serum autotaxin (ATX) activity and level are significantly elevated in human AD patients compared to those in normal controls, which indicates that ATX may be involved in human AD...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28673013/coumarins-from-the-roots-of-angelica-dahurica-cause-anti-allergic-inflammation
#19
Dong Li, Li Wu
Allergic inflammation is induced by allergens and leads to various allergic diseases, including rhinitis, asthma and conjunctivitis. Histamine is important in the pathogenesis of an immunoglobulin E-dependent allergic reaction and results in the secretion of cytokines associated with inflammation. Angelica dahurica (A. dahurica) is a medicinal plant widely used in China for the treatment of symptoms related to allergic inflammation. The present study investigated the chemical constituents from A. dahurica and evaluated their reductive effect on allergic inflammation...
July 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28671980/fceri-density-and-spontaneous-secretion-from-human-basophils
#20
Donald MacGlashan
Mast cells and basophils depend on aggregation of the high-affinity IgE receptor, FceRI, to initiate secretion. A variety of studies have shown that FceRI densities vary 100 fold among subjects' basophils and it has been speculated that high densities might be responsible for unusual behaviors of the cells, notably sensitivity to certain monomeric IgE antibodies or spontaneous release. These studies experimentally examined the density dependence of spontaneous release and signaling element expression in subjects' basophils with FceRI densities ranging from approximately 6000 to 600,000 per cell...
2017: PloS One
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