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https://www.readbyqxmd.com/read/28820054/qsar-modeling-of-histamine-h3r-antagonists-inverse-agonists-as-future-drugs-for-neurodegenerative-diseases
#1
Michelle Fidelis Corrêa, João Paulo Dos Santos Fernandes
Histamine H3 receptor (H3R) is associated with several neuropsychological diseases. It is predominantly expressed in the central nervous system as presynaptic receptor, especially in regions associated with cognition and behavior, and is responsible for modulate the synthesis and release of histamine and other neurotransmitters such as acetylcholine, dopamine and serotonin. Therefore, H3R is an important target involved in several CNS disorders, such as narcolepsy, attention deficit hyperactivity disorder and schizophrenia...
August 17, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28820006/an-immunohistochemical-investigation-of-renal-phospholipidosis-and-toxicity-in-rats
#2
Jing Ying Ma, Sandra Snook, Sheryl Garrovillo, Charles Johnson, David La
Immunohistochemical staining for the lysosome-associated membrane protein 2 (LAMP-2) has been proposed previously as an alternative to electron microscopy to identify hepatic phospholipidosis. This study used LAMP-2 immunohistochemistry (IHC) to diagnose phospholipidosis in rats exhibiting renal tubular injury. Rats were administered toreforant, a histamine H4 receptor antagonist by oral gavage at a dose of 3, 10, or 100 mg/kg/d for 6 months. Hematoxylin and eosin staining revealed renal tubular epithelial cell vacuolation, hypertrophy, degeneration, and luminal dilation in the 100 mg/kg/d group animals...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28818391/role-of-capillary-pericytes-and-precapillary-arterioles-in-the-vascular-mechanism-of-betahistine-in-a-guinea-pig-inner-ear-model
#3
Mattis Bertlich, Friedrich Ihler, Bernhard G Weiss, Saskia Freytag, Michael Strupp, Mark Jakob, Martin Canis
AIMS: Betahistine is a histamine analogue that is used for the treatment of Menière's disease. Animal studies showed that it increases local blood flow in the stria vascularis. In terms of its mode of action, recent studies have prompted discussion of whether betahistine actively affects cochlear microcirculation by dilations of pericytes or of precapillary arterioles or by mere downstream effects. Hence, we investigated the effects of betahistine on cochlear capillary pericytes and precapillary arterioles...
August 14, 2017: Life Sciences
https://www.readbyqxmd.com/read/28818177/angioedema
#4
Janina Hahn, Thomas K Hoffmann, Bastian Bock, Melanie Nordmann-Kleiner, Susanne Trainotti, Jens Greve
BACKGROUND: Acute angioedema of the upper airways can be life-threatening. An important distinction is drawn between mast-cell-mediated angioedema and bradykinin-mediated angioedema; the treatment of these two entities is fundamentally different. METHODS: This review is based on pertinent articles retrieved by a selective search in PubMed and on guidelines concerning the treatment of angioedema. The authors draw on their own clinical experience in their assessment of the literature...
July 24, 2017: Deutsches Ärzteblatt International
https://www.readbyqxmd.com/read/28817204/new-insight-into-the-control-of-peptic-ulcer-by-targeting-the-histamine-h2-receptor
#5
Vijai Singh, Nisarg Gohil, Robert Ramírez-García
Peptic ulcer disease is one of the major challenges in public health globally and new evidence shows that it can be controlled by targeting the histamine H2 receptor (H2 R). Recently, a number of H2 R antagonists have been synthesized and used to block the action of histamine on the parietal cells in the stomach and decrease the acid production. In this study, we modeled the H2 R by homology modeling using the 3-D crystal structure and this model was validated based on free energy and amino acid residues present in the allowed regions of a Ramachandran plot...
August 17, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28815720/pharmacological-evidence-of-involvement-of-nitric-oxide-pathway-in-anti-pruritic-effects-of-sumatriptan-in-chloroquine-induced-scratching-in-mice
#6
Nazgol-Sadat Haddadi, Sattar Ostadhadi, Saeed Shakiba, Khashayar Afshari, Nastaran Rahimi, Arash Foroutan, Ahmad-Reza Dehpour
Chloroquine (CQ) induces histamine-independent itch in human and mice. We recently reported the role of intradermal nitric oxide (NO)/ cyclic guanosine monophosphate (cGMP) pathway in CQ-evoked scratching in mice. Chloroquine stimulates neuronal nitric oxide synthase (nNOS) activity to over-producing NO in the skin. Sumatriptan, a 5-hydroxytryptamine 1b/1d receptors (5-HTR1b/1d) agonist, is involved in pain and used to treat migraine and cluster headaches. According to previous studies, sumatriptan inhibits NOS activity...
August 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28814067/neuro-immune-interactions-in-allergic-diseases-novel-targets-for-therapeutics
#7
Tiphaine Voisin, Amélie Bouvier, Isaac M Chiu
Recent studies have highlighted an emerging role for neuro-immune interactions in mediating allergic diseases. Allergies are caused by an overactive immune response to a foreign antigen. The peripheral sensory and autonomic nervous system densely innervates mucosal barrier tissues including the skin, respiratory tract and gastrointestinal (GI) tract that are exposed to allergens. It is increasingly clear that neurons actively communicate with and regulate the function of mast cells, dendritic cells, eosinophils, Th2 cells and type 2 innate lymphoid cells in allergic inflammation...
June 1, 2017: International Immunology
https://www.readbyqxmd.com/read/28812277/milonine-an-alkaloid-of-cissampelos-sympodialis-eichl-menispermaceae-inhibits-histamine-release-of-activated-mast-cells
#8
Adriano Francisco Alves, Giciane Carvalho Vieira, Francisco Allysson A F Gadelha, Luiz Henrique Agra Cavalcante-Silva, Marco Aurélio Martins, José Maria Barbosa-Filho, Marcia Regina Piuvezam
Milonine is an alkaloid of Cissampelos sympodialis Eichl. (Menispermaceae), a plant used in the northeast of Brazil to treat allergies such as asthma, rhinitis, and other conditions. Previously, several alkaloids were isolated from its roots and leaves with pharmacological properties in asthma and acute inflammation models. Therefore, the aim of this study was to evaluate the milonine effect on mast cells degranulation in vivo and in vitro. Swiss mice (n = 8) were used in models of paw edema induced by carrageenan, compound 48/80, or histamine...
August 15, 2017: Inflammation
https://www.readbyqxmd.com/read/28808406/peimine-inhibits-the-production-of-proinflammatory-cytokines-through-regulation-of-the-phosphorylation-of-nf-%C3%AE%C2%BAb-and-mapks-in-hmc-1-cells
#9
Ji Hye Park, Bina Lee, Hyun Kab Kim, Eun-Young Kim, Jae-Hyun Kim, Ju-Hee Min, Sunkook Kim, Youngjoo Sohn, Hyuk-Sang Jung
BACKGROUND: Peimine is a major biologically active component of Fritillaria ussuriensis. Peimine was investigated in chronic inflammation response, but it has not been studied in mast cell-related immediate allergic reaction. The present study aimed to evaluate anti-allergic effect of peimine in human mast cell (HMC-1). MATERIALS AND METHODS: The effect of peimine on cell viability was measured by MTS assay in HMC-1. Histamine release was investigated in rat peritoneal mast cells (RPMCs)...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808054/mst4-phosphorylates-acap4-to-orchestrate-apical-membrane-remodeling-during-gastric-acid-secretion
#10
Xiao Yuan, Phil Y Yao, Jiying Jiang, Yin Zhang, Zeqi Su, Wendy Yao, Xueying Wang, Ping Gui, McKay Mullen, Calmour Henry, Tarsha Ward, Wenwen Wang, Larry Brako, Ruijun Tian, Xuannv Zhao, Fengsong Wang, Xinwang Cao, Dongmei Wang, Xing Liu, Xia Ding, Xuebiao Yao
The digestion in the stomach depends on acidification of the lumen. Histamine-elicited acid secretion is triggered by activation of PKA cascade, which ultimately results in the insertion of gastric H,K-ATPases into the apical plasma membranes of parietal cells. Our recent study revealed the functional role of PKA-MST4-ezrin signaling axis in histamine-elicited acid secretion (Jiang et al., 2015. J. Biol. Chem. 290, 28272-28285). However, it remains uncharacterized how PKA-MST4-ezrin signaling axis operates the insertion of H,K-ATPases into the apical plasma membranes of gastric parietal cells...
August 14, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28806173/the-%C3%AE-alanine-transporter-balat-is-required-for-visual-neurotransmission-in-drosophila
#11
Yongchao Han, Liangyao Xiong, Ying Xu, Tian Tian, Tao Wang
The recycling of neurotransmitters is essential for sustained synaptic transmission. In Drosophila, histamine recycling is required for visual synaptic transmission. Synaptic histamine is rapidly taken up by laminar glia, and is converted to carcinine. After delivered back to photoreceptors, carcinine is hydrolyzed to release histamine and β-alanine. This histamine is repackaged into synaptic vesicles, but it is unclear how the β-alanine is returned to the laminar glial cells. Here, we identified a new β-alanine transporter, which we named BalaT (Beta-alanine Transporter)...
August 14, 2017: ELife
https://www.readbyqxmd.com/read/28804811/serum-diamine-oxidase-in-pseudoallergy-in-the-pediatric-population
#12
Joanna Kacik, Barbara Wróblewska, Sławomir Lewicki, Robert Zdanowski, Bolesław Kalicki
Histamine intolerance (pseudoallergy) is a poorly investigated type of food hypersensitivity. The main enzyme responsible for histamine degradation in the extracellular matrix is diamine oxidase (DAO). Disturbances in the concentration or activity of DAO may lead to the development of clinical signs of allergy. The aim of the present work was to assess the DAO concentration, peripheral blood morphology, lymphocytes phenotyping (CD3+, CD4+, CD8+, CD19+, NK cells, NKT cells, and activated T-cells), and natural regulatory Treg (nTregs) cell population (CD4+, CD25+, CD127low, and FoxP3) in 34 pediatric patients with histamine-dependent syndromes...
August 15, 2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28802126/derp1-modified-dendritic-cells-attenuate-allergic-inflammation-by-regulating-the-development-of-t-helper-type1-th1-th2-cells-and-regulatory-t-cells-in-a-murine-model-of-allergic-rhinitis
#13
Shaoqing Yu, Bing Han, Shuangxi Liu, Hong Wang, Wenjie Zhuang, Yu Huang, Ruxin Zhang
The CD4(+)CD25(+)Foxp3(+) regulatory T cells (Tregs) are known to regulate Th2-induced allergic rhinitis (AR). In this study, we evaluated the efficacy of Derp1-modified dendritic cells (DCs) in AR immunotherapy. Derp1 was synthesized and transfected into DCs to generate Derp1-modified DCs. Phenotypes of Derp1-modified DCs were analyzed with flow cytometry using antibodies against DC markers CD11c, CD11b, CD59, CD103 and Toll-like receptor 1(TLR1). Four groups of subject mice were formed; the controls were treated with immature DCs, while the AR mice models were sensitized with Derp1(AR) and treated with DCs(DC-AR) or Derp1-modified DCs (Derp1DC-AR)...
August 9, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28801980/effects-of-proton-pump-inhibitors-and-famotidine-on-elimination-of-plasma-methotrexate-evaluation-of-drug-drug-interactions-mediated-by-organic-anion-transporter-3
#14
Katsuya Narumi, Yu Sato, Masaki Kobayashi, Ayako Furugen, Kumiko Kasashi, Takehiro Yamada, Takanori Teshima, Ken Iseki
Methotrexate (MTX) is an antifolate agent used in the treatment of numerous types of cancer, and eliminated by active tubular secretion via organic anion transporter 3 (OAT3). Gastric antisecretory drugs, such as proton pump inhibitors (PPIs) and histamine H2 receptor antagonists, are widely used among patients with cancer in clinical practice. The aim of the present study was to analyze the potential drug-drug interactions between MTX and gastric antisecretory drugs in high-dose MTX (HD-MTX) therapy. We retrospectively analyzed the impact of PPIs on the plasma MTX concentration on 73 cycles of HD-MTX therapy performed in 43 patients...
August 12, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28800937/vortioxetine-a-new-alternative-for-the-treatment-of-major-depressive-disorder
#15
Estela Salagre, Iria Grande, Brisa Solé, Jose Sanchez-Moreno, Eduard Vieta
Major Depressive Disorder (MDD) is a serious psychiatric condition. Its treatment remains a challenge nowadays. Vortioxetine is a novel antidepressant with a unique profile, as it acts as a multimodal serotoninergic agent. Its efficacy in MDD has been established in many short- and long-term studies, with 7 positive, 4 negative and 1 failed randomized controlled trials. Moreover, its ability to modulate a wide range of neurotransmitters (serotonin, dopamine, norepinephrine, histamine, glutamate or GABA) confers vortioxetine pro-cognitive effects...
August 8, 2017: Revista de Psiquiatrí́a y Salud Mental
https://www.readbyqxmd.com/read/28800865/contemporary-reviews-in-critical-care-medicine-anaphylaxis
#16
REVIEW
Daniel LoVerde, Onyinye I Iweala, Ariana Eginli, Guha Krishnaswamy
Anaphylaxis is a systemic, life threatening disorder triggered by mediators released by mast cells and basophils activated via allergic (IgE-mediated) or non-allergic (non-IgE-mediated) mechanisms. It is a rapidly evolving, multisystem process involving the integumentary, pulmonary, gastrointestinal and cardiovascular systems. Anaphylaxis and angioedema are serious disorders that can lead to fatal airway obstruction and culminate in cardiorespiratory arrest resulting in hypoxemia and/or shock. Often, these disorders can be appropriately managed in an outpatient setting...
August 8, 2017: Chest
https://www.readbyqxmd.com/read/28797771/biphenyloxy-alkyl-piperidine-and-azepane-derivatives-as-histamine-h3-receptor-ligands
#17
Dorota Łażewska, Maria Kaleta, J Stephan Schwed, Tadeusz Karcz, Szczepan Mogilski, Gniewomir Latacz, Agnieszka Olejarz, Agata Siwek, Monika Kubacka, Annamaria Lubelska, Ewelina Honkisz, Jadwiga Handzlik, Barbara Filipek, Holger Stark, Katarzyna Kieć-Kononowicz
Novel biphenyloxy-alkyl derivatives of piperidine and azepane were synthesized and evaluated for their binding properties at the human histamine H3 receptor. Two series of compounds were obtained with a meta- and a para-biphenyl moiety. The alkyl chain spacer contained five and six carbon atoms. The highest affinity among all compounds was shown by 1-(6-(3-phenylphenoxy)hexyl)azepane (13) with a Ki value of 18nM. Two para-biphenyl derivatives, 1-(5-(4-phenylphenoxy)pentyl)piperidine (14; Ki=25nM) and 1-(5-(4-phenylphenoxy)pentyl)azepane (16; Ki=34nM), classified as antagonists in a cAMP accumulation assay (IC50=4 and 9nM, respectively), were studied in detail...
July 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28796107/the-effect-of-functional-mandibular-shift-on-the-muscle-spindle-systems-in-head-neck-muscles-and-the-related-neurotransmitter-histamine
#18
Bing-Li Du, Jiang-Ning Li, Hong-Ming Guo, Song Li, Biao Liu
The aim of this study is to explore the effects of abnormal occlusion and functional recovery caused by functional mandible deviation on the head and neck muscles and muscle spindle sensory-motor system by electrophysiological response and endogenous monoamine neurotransmitters' distribution in the nucleus of the spinal tract. Seven-week-old male Wistar rats were randomly divided into 7 groups: normal control group, 2W experimental control group, 2W functional mandible deviation group, 2W functional mandible deviation recovery group, 4W experimental control group, 4W functional mandible deviation group, 4W functional mandible deviation recovery group...
August 8, 2017: Journal of Craniofacial Surgery
https://www.readbyqxmd.com/read/28793837/further-investigation-of-equine-fescue-oedema-induced-by-mediterranean-tall-fescue-lolium-arundinaceum-infected-with-selected-fungal-endophytes-epichlo%C3%A3-coenophiala
#19
S C Finch, J S Munday, B L Sutherland, J B Vlaming, L R Fletcher
AIMS: To determine if equine fescue oedema (EFO) induced by grazing Mediterranean-type tall fescue (Lolium arundinaceum) infected with selected endophytes (Epichloë coenophiala) could be prevented by treatment with the corticosteroid, methylprednisolone, and anti-histamine cetirizine, and to determine concentrations of lolines, specifically N-acetyl norloline (NANL), in grasses grazed by horses that did and did not develop EFO. METHODS: Four horses were grazed on AR542-infected Mediterranean tall fescue pasture (from Day 0) for 7 days prior to being subjected to euthanasia...
August 9, 2017: New Zealand Veterinary Journal
https://www.readbyqxmd.com/read/28791419/mapping-of-the-binding-sites-of-human-histamine-n-methyltransferase-hnmt-monoclonal-antibodies
#20
Hubert G Schwelberger, Johannes Feurle, Gunnar Houen
OBJECTIVE: Recently, we characterized mouse monoclonal antibodies that allow the specific and sensitive detection of human histamine N-methyltransferase (HNMT). To understand differences in binding characteristics and recognition of enzyme variants we mapped the antibody binding sites. METHODS: Fragments of human HNMT were expressed as glutathione S-transferase fusion proteins that were used for testing antibody binding on immunoblots. Combined information from species cross-reactivity, sequence comparison, protein structure, and binding site prediction software were used to localize the epitope recognized by each antibody...
August 8, 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
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