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Histamine receptors

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https://www.readbyqxmd.com/read/28635673/toxicity-of-naphthalene-and-benzene-on-tribollium-castaneum-herbst
#1
Nerlis Pajaro-Castro, Karina Caballero-Gallardo, Jesus Olivero-Verbel
Naphthalene and benzene are widely-used volatile organic compounds. The aim of this research was to examine the toxicological effects of naphthalene and benzene against Tribolium castaneum as an animal model. Adult insects were exposed to these aromatic compounds to assess mortality after 4-48 h of exposure. The lethal concentration 50 (LC50) for naphthalene, naphthalin, and benzene were 63.6 µL/L, 20.0 µL/L, and 115.9 µL/L in air, respectively. Real-time polymerase chain reaction (PCR) analysis revealed expression changes in genes related to oxidative stress and metabolism [Glutathione S-Transferase (Gst), and Cytochrome P450 6BQ8 (Cyp6bq8)]; reproduction and metamorphosis [Hormone receptor in 39-like protein (Hr39), Ecdysone receptor: (Ecr), and Chitin synthase 2 (Chs2)]; and neurotransmission [Histamine-gated chloride channel 2 (Hiscl2)] in insects exposed for 4 h to 70...
June 21, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28626527/systematic-data-mining-reveals-synergistic-h3r-mchr1-ligands
#2
David Schaller, Stefanie Hagenow, Gina Alpert, Alexandra Naß, Robert Schulz, Marcel Bermudez, Holger Stark, Gerhard Wolber
In this study, we report a ligand-centric data mining approach that guided the identification of suitable target profiles for treating obesity. The newly developed method is based on identifying target pairs for synergistic positive effects and also encompasses the exclusion of compounds showing a detrimental effect on obesity treatment (off-targets). Ligands with known activity against obesity-relevant targets were compared using fingerprint representations. Similar compounds with activities to different targets were evaluated for the mechanism of action since activation or deactivation of drug targets determines the pharmacological effect...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28622592/second-generation-h1-antihistamines-interaction-with-food-and-alcohol-a-systematic-review
#3
REVIEW
Paweł Paśko, Tomasz Rodacki, Renata Domagała-Rodacka, Krzysztof Palimonka, Monika Marcinkowska, Danuta Owczarek
Histamine is a mediator of many physiological processes. It plays an important role in modulating allergy reactions and immune system responses. H1 receptor is a therapeutic target for drugs applied in allergic diseases such as allergic rhinoconjunctivitis, urticarial, or atopic dermatitis. H1-antihistamines display different chemical structures, pharmacokinetics and a potential for drug-drug and drug-food interactions. Drug-food interactions are known to reduce therapeutic effects of the medicine, as well as to induce a potent adverse drug reactions...
June 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28618071/histamine-receptor-2-modifies-inkt-cell-activity-within-the-inflamed-lung
#4
R Ferstl, R Frei, W Barcik, E Schiavi, K Wanke, M Ziegler, N Rodriguez-Perez, D Groeger, P Konieczna, S Zeiter, D Nehrbass, Roger Lauener, C A Akdis, L O'Mahony
BACKGROUND: Histamine is a key immunoregulatory mediator and can dampen proinflammatory responses via activation of histamine receptor 2 (H2 R). The aim of this study was to determine the role of H2 R in modulating lung inflammatory responses. METHODS: H2 R was blocked using famotidine or activated using dimaprit in both the ovalbumin (OVA) and house dust mite extract (HDM) murine models of respiratory inflammation. H2 R-deficient animals and CD1d/ H2 R-deficient animals were utilized to examine the CD1d presentation of lipid antigens (αGal-Cer or OCH) to invariant Natural Killer T (iNKT) cells...
June 15, 2017: Allergy
https://www.readbyqxmd.com/read/28616446/treatment-with-anti-fc%C3%AE%C2%B5ri%C3%AE-antibody-exacerbates-eae-and-t-cell-immunity-against-myelin
#5
Silvia Musio, Massimo Costanza, Pietro Luigi Poliani, Elena Fontana, Manuela Cominelli, Gabriella Abolafio, Lawrence Steinman, Rosetta Pedotti
OBJECTIVE: To investigate the effects of targeting the high-affinity receptor for immunoglobulin E (FcεRI), that plays a central role in allergic responses and is constitutively expressed on mast cells and basophils, in clinical disease and autoimmune T-cell response in experimental MS. METHODS: Experimental autoimmune encephalomyelitis (EAE) was induced in C57BL/6 mice by immunization with myelin oligodendrocyte glycoprotein 35-55. Anti-FcεRI α-chain antibody was administered intraperitoneally...
May 2017: Neurology® Neuroimmunology & Neuroinflammation
https://www.readbyqxmd.com/read/28615015/the-gastroprotective-effect-of-ethyl-acetate-fraction-of-hot-water-extract-of-trichosanthes-cucumerina-linn-and-its-underlying-mechanisms
#6
Ramani Karunakaran, M Ira Thabrew, G Mayuri Thammitiyagodage, B Prasanna Galhena, L D A Menuka Arawwawala
BACKGROUND: Antacids, anticholinergic drugs, histamine H2- receptor antagonists and irreversible proton pump inhibitors have been used for the treatment of gastric ulcers. However, prolonged use of these drugs may lead to series of adverse effects such as diarrhea, headache, rash, hypertension, muscular and joint pain. Therefore, there is an urgent need of more effective and safer treatments with fewer side effects. The aim of the present study was to scientifically evaluate the gastroprotective activity of fractions of the hot water extract of Trichosanthes cucumerina Linn (Family: Cucurbitaceae) aerial parts with a view to identifying the fraction with the best gastroprotective activity and the possible mechanism/s by which this fraction exert gastroprotection...
June 14, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28614417/antipsychotic-medications-and-stroke-in-schizophrenia-a-case-crossover-study
#7
Wen-Yin Chen, Lian-Yu Chen, Hsing-Cheng Liu, Chi-Shin Wu, Shu-Yu Yang, Chun-Hung Pan, Shang-Ying Tsai, Chiao-Chicy Chen, Chian-Jue Kuo
BACKGROUND: The association between antipsychotic use and the risk of stroke in schizophrenic patients is controversial. We sought to study the association in a nationwide cohort with schizophrenia. METHODS: Using a retrospective cohort of patients with schizophrenia (N = 31,976) derived from the Taiwan National Health Insurance Research Database, 802 new-onset cases of stroke were identified within 10 years of follow-up (from 2000 through 2010). We designed a case-crossover study using 14-day windows to explore the risk factors of stroke and the association between antipsychotic drugs and the risk of stroke...
2017: PloS One
https://www.readbyqxmd.com/read/28613003/systematic-review-pharmacotherapy-for-high-output-enterostomies-or-enteral-fistulas
#8
REVIEW
F E E de Vries, L F Reeskamp, O van Ruler, I van Arum, W Kuin, G Dijksta, J W Haveman, M A Boermeester, M J Serlie
BACKGROUND: High-output enterocutaneous fistula or enterostomies can cause intestinal failure. There is a wide variety of options in medical management of patients with high output. AIM: To systematically review the literature on available pharmacotherapy to reduce output and to propose an algorithm for standard of care. METHODS: Relevant databases were systematically reviewed to identify studies on pharmacotherapy for reduction in (high-) output enterostomies or fistula...
June 14, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28607673/risk-factors-for-clostridium-difficile-infections-an-overview-of-the-evidence-base-and-challenges-in-data-synthesis
#9
Paul Eze, Evelyn Balsells, Moe H Kyaw, Harish Nair
BACKGROUND: Recognition of a broad spectrum of disease and development of Clostridium difficile infection (CDI) and recurrent CDI (rCDI) in populations previously considered to be at low risk has renewed attention on differences in the risk profile of patients. In the absence of primary prevention for CDI and limited treatment options, it is important to achieve a deep understanding of the multiple factors that influence the risk of developing CDI and rCDI. METHODS: We conducted a review of systematic reviews and meta-analyses on risk factors for CDI and rCDI published between 1990 and October 2016...
June 2017: Journal of Global Health
https://www.readbyqxmd.com/read/28606938/peptide-mediated-mast-cell-activation-ligand-similarities-for-receptor-recognition-and-protease-induced-regulation
#10
REVIEW
Lei Lu, Marianna Kulka, Larry D Unsworth
MCs are crucial regulators of the innate immune response. MC degranulation is a rapid response mechanism that allows for the release of a stored plethora of inflammatory mediators, including histamine, heparin, various serine proteases, chemokines, and cytokines. The activation of MCs can lead to the de novo expression of a variety of chemokines and cytokines that can influence a variety of outcomes: inflammation, angiogenesis, and others. A variety of IgE-independent mediators, including IgG, cytokines, chemokines, exogenous molecules, drugs, and cationic peptides, and others, can directly trigger MC activation...
June 12, 2017: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/28603044/relaxation-of-isolated-guinea-pig-trachea-by-apigenin-a-constituent-of-celery-via-inhibition-of-phosphodiesterase
#11
Junn-Lain Chen, Wun-Chang Ko
Apigenin, was reported to have vasodilatory effects by inhibiting Ca(2+) influx through both voltage- and receptor-operated calcium channels, but not by inhibiting cAMP- or cGMP-phosphodiesterases (PDEs) in rat thoracic aorta. However, apigenin was reported to inhibit PDE1, 2 and 3 in guinea-pig lung and heart. The aim of this study was to clarify that guinea-pig tracheal relaxation by apigenin whether via PDE inhibition. We isometrically recorded the tension of isolated guinea-pig tracheal segments on a polygraph...
June 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28592369/preliminary-study-of-histamine-h4-receptor-expressed-on-human-cd4-t-cells-and-its-immunomodulatory-potency-in-the-il-17-pathway-of-psoriasis
#12
Song Hee Han, Min Seok Hur, Min Jung Kim, Bo Mi Kim, Kyoung Woon Kim, Hae Rim Kim, Yong Beom Choe, Kyu Joong Ahn, Yang Won Lee
BACKGROUND: Previous studies have shown the expression of histamine H4 receptor (H4R) on CD4(+) T cells, especially human CD4(+) Th2-polarized T cells. OBJECTIVE: This study aimed to investigate the role of H4R on these effector T cells in psoriasis. METHODS: We enrolled three patients each with active psoriasis, inactive psoriasis, scalp seborrheic dermatitis, and three normal controls, and compared the basal expression of H4R mRNA in their peripheral blood CD4(+) T cells...
May 29, 2017: Journal of Dermatological Science
https://www.readbyqxmd.com/read/28591796/histamine-enhances-theta-coupled-spiking-and-gamma-oscillations-in-the-medial-entorhinal-cortex-consistent-with-successful-spatial-recognition
#13
Quanhui Chen, Fenlan Luo, Faguo Yue, Jianxia Xia, Qin Xiao, Xiang Liao, Jun Jiang, Jun Zhang, Bo Hu, Dong Gao, Chao He, Zhian Hu
Encoding of spatial information in the superficial layers of the medial entorhinal cortex (sMEC) involves theta-modulated spiking and gamma oscillations, as well as spatially tuned grid cells and border cells. Little is known about the role of the arousal-promoting histaminergic system in the modification of information encoded in the sMEC in vivo, and how such histamine-regulated information correlates with behavioral functions. Here, we show that histamine upregulates the neural excitability of a significant proportion of neurons (16...
June 7, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28590010/proton-pump-inhibitors-and-risk-of-mild-cognitive-impairment-and-dementia
#14
Felicia C Goldstein, Kyle Steenland, Liping Zhao, Whitney Wharton, Allan I Levey, Ihab Hajjar
OBJECTIVES: To examine the risk associated with the use of proton pump inhibitors (PPIs) of conversion to mild cognitive impairment (MCI), dementia, and specifically Alzheimer's disease (AD). DESIGN: Observational, longitudinal study. SETTING: Tertiary academic Alzheimer's Disease Centers funded by the National Institute on Aging. PARTICIPANTS: Research volunteers aged 50 and older with two to six annual visits; 884 were taking PPIs at every visit, 1,925 took PPIs intermittently, and 7,677 never reported taking PPIs...
June 7, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28587746/corrigendum-to-quantitative-prediction-of-histamine-h1-receptor-occupancy-by-the-sedative-and-non-sedative-antagonists-in-the-human-central-nervous-system-based-on-systemic-exposure-and-preclinical-data-drug-metab-pharmacokinet-32-2017-135-144
#15
Kayoko Kanamitsu, Yoshitane Nozaki, Yoko Nagaya, Yuichi Sugiyama, Hiroyuki Kusuhara
No abstract text is available yet for this article.
May 22, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28585360/functional-and-phenotypic-analysis-of-basophils-allows-determining-distinct-subtypes-in-patients-with-chronic-urticaria
#16
Michèle Myriam Rauber, Julia Pickert, Lily Holiangu, Christian Möbs, Wolfgang Pfützner
BACKGROUND: Chronic urticaria (CU) is a frequent skin disease characterized by relapsing appearance of pruritic hives. While clinical symptoms are due to the release of histamine by cutaneous mast cells, the underlying pathophysiology is still unknown. However, previous studies indicate that basophils might be of relevance. Besides, the occurrence of autoantibodies against IgE or its receptor, FcεRI, and the therapeutic efficacy of anti-IgE antibodies imply that IgE-mediated mechanisms also play an important role in CU...
June 5, 2017: Allergy
https://www.readbyqxmd.com/read/28584269/time-dependent-changes-and-potential-mechanisms-of-glucose-lipid-metabolic-disorders-associated-with-chronic-clozapine-or-olanzapine-treatment-in-rats
#17
Xuemei Liu, Zhixiang Wu, Jiamei Lian, Chang-Hua Hu, Xu-Feng Huang, Chao Deng
Chronic treatment with second-generation antipsychotic drugs (SGAs) has been associated with an increased risk of metabolic syndrome. To evaluate the longitudinal changes in glucose-lipid homeostasis after SGA use, we studied the time-dependent effects of olanzapine (OLZ) (3 mg/kg, b.i.d.) or clozapine (CLZ) (20 mg/kg, b.i.d.) treatment on metabolic profiles for 9 weeks in rats. Although only OLZ significantly increased body weight in rats, both OLZ and CLZ elevated blood lipid levels. Chronic OLZ treatment induced significant weight gain leading to a higher fasting insulin level and impaired glucose tolerance, whereas CLZ lowered fasting insulin levels and impaired glucose tolerance independent of weight gain...
June 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28579188/effects-of-histamine-2-receptor-antagonists-and-proton-pump-inhibitors-on-the-pharmacokinetics-of-gefitinib-in-patients-with-non-small-cell-lung-cancer
#18
Hayato Yokota, Kazuhiro Sato, Yuji Okuda, Hiroyuki Kobayashi, Masahide Takeda, Mariko Asano, Hiroshi Ito, Masatomo Miura
INTRODUCTION: In this study, we investigated the degree of drug interactions between gefitinib and gastric acid suppressants (ie, histamine 2-receptor antagonists [H2RAs] or proton pump inhibitors [PPIs]) with a clinical standard dose in Japanese patients with non-small-cell lung cancer. METHODS: Retrospectively, 47 patients were divided into 3 groups: gefitinib therapy with a PPI (15 patients) or an H2RA (8 patients) or gefitinib therapy alone (24 patients). On day 15 after beginning gefitinib therapy (administration at 08:00) with or without H2RA (administration twice daily at 08:00 and 18:30) or PPI (administration once daily at 08:00 or 18:30), whole blood samples were collected just prior to and at 1, 2, 4, 6, 8, 12, and 24 hours after administration...
May 10, 2017: Clinical Lung Cancer
https://www.readbyqxmd.com/read/28570220/effects-of-rupatadine-on-platelet-activating-factor-induced-human-mast-cell-degranulation-compared-with-desloratadine-and-levocetirizine-the-maspaf-study
#19
R Munoz-Cano, E Ainsua-Enrich, I Torres-Atencio, M Martin, J Sánchez-Lopez, J Bartra, C Picado, J Mullol, A Valero
BACKGROUND AND OBJECTIVE: Platelet-activating factor (PAF) is a lipid mediator involved in the pathophysiology of several allergic diseases, for example, in the amplification of mast cell (MC) activation in anaphylaxis. Rupatadine is an antihistamine with a demonstrated anti-PAF effect, although its capacity to inhibit PAF-induced MC degranulation has not been fully evaluated. Objectives: To compare the ability of rupatadine to inhibit PAF-induced MC degranulation with that of desloratadine and levocetirizine and to confirm the dual anti-H1 and anti-PAF activity of rupatadine...
2017: Journal of Investigational Allergology & Clinical Immunology
https://www.readbyqxmd.com/read/28565788/immunosuppressive-agents-are-associated-with-peptic-ulcer-bleeding
#20
Minoru Tomizawa, Fuminobu Shinozaki, Rumiko Hasegawa, Yoshinori Shirai, Yasufumi Motoyoshi, Takao Sugiyama, Shigenori Yamamoto, Naoki Ishige
Peptic ulcer bleeding can be fatal. Non-steroidal anti-inflammatory drugs (NSAIDs), corticosteroids and immunosuppressive agents are administered for long-term usage. The present study assessed the association between peptic ulcer bleeding and administration of NSAIDs, corticosteroids and immunosuppressive agents. Furthermore, the efficacy of lowering the risk of peptic ulcer bleeding with proton pump inhibitors (PPI) and histamine 2 receptor antagonists (H2RA) was evaluated. Medical records were retrospectively analyzed for patients subjected to an upper gastrointestinal (GI) endoscopy performed at the National Hospital Organization Shimoshizu Hospital (Yotsukaido, Japan) from October 2014 to September 2015...
May 2017: Experimental and Therapeutic Medicine
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