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Histamine receptors

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https://www.readbyqxmd.com/read/28102361/effectiveness-and-tolerability-of-different-recommended-doses-of-ppis-and-h2ras-in-gerd-network-meta-analysis-and-grade-system
#1
Chao Zhang, Joey S W Kwong, Rui-Xia Yuan, Hao Chen, Chang Xu, Yi-Pin Wang, Gong-Li Yang, Jin-Zhu Yan, Le Peng, Xian-Tao Zeng, Hong Weng, Jie Luo, Yu-Ming Niu
Proton pump inhibitors (PPIs) and histamine-2-receptor antagonists (H2RAs) are used for gastro-esophageal reflux disease (GERD); however, the clinical evidence for treatment is poor. We evaluated the effectiveness and tolerability of different doses of PPIs, H2RAs and placebo in adults with GERD. Six online databases were searched through September 1, 2016. All related articles were included and combined with a Bayesian network meta-analysis from randomized controlled trials (RCTs). The GRADE systems were employed to assess the main outcome...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28101683/allergy-histamine-and-antihistamines
#2
Martin K Church
This chapter concentrates on the role in allergic disease of histamine acting on H1-receptors. It is clear that allergy has its roots in the primary parasite rejection response in which mast cell-derived histamine creates an immediate hostile environment and eosinophils are recruited for killing. This pattern is seen in allergic rhinitis where the early events of mucus production and nasal itching are primarily histamine mediated whereas nasal blockage is secondary to eosinophil infiltration and activation...
January 19, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28094875/neuroendocrinology-of-mast-cells-challenges-and-controversies
#3
REVIEW
Theoharis C Theoharides
Mast cells (MC) are hemopoietically-derived tissue immune cells that are ubiquitous in the body, including neuroendocrine organs such as the hypothalamus, pineal, pituitary, ovaries, pancreas and uterus where their action is not well understood. Mast cells have historically been associated with allergies because of their rich content of histamine and tryptase, but more recently with regulation of immunity and inflammation due their synthesis and release of numerous cytokines and chemokines. Mast cells are located perivascularly and express numerous receptors for diverse ligands such as allergens, pathogens, neurotransmitters, neuropeptides and hormones including acetylcholine, calcitonin gene-related peptide (CGRP), corticosteroids, corticotropin-releasing hormone (CRH), β-endorphin, epinephrine, 17β-estradiol, gonadotrophins, hemokinin-A (HKA), leptin, melatonin, neurotensin (NT), parathyroid hormone (PTH), substance P (SP) and vasoactive instestinal peptide (VIP)...
January 17, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28092808/antinociceptive-effect-of-co-administered-nmda-and-histamine-h4-receptor-antagonists-in-a-rat-model-of-acute-pain
#4
Renata Wolińska, Anna Leśniak, Małgorzata Żochowska, Mariusz Sacharczuk, Katarzyna Kieć-Kononowicz, Magdalena Bujalska-Zadrożny
BACKGROUND: The histamine H4 receptor (H4R) has attracted a lot of attention in terms of its role in antinociception. The N-Methyl-d-aspartic acid (NMDA) receptor is a well-characterized participant in pain pathways. However, it's influence on H4R signaling is poorly understood. Thus, in the present study we investigated the effect of a selective H4R antagonist JNJ7777120 (25mg/kg) and a NMDA receptor antagonist MK-801 (0.1-10μg) on nociceptive thresholds in a rat acute pain model. METHODS: The influence of intrathecally (it), intracerebroventricularly (icv) and intraplantarly (ipl) administered MK-801 co-injected with JNJ7777120 administered intraperitoneally (ip) was determined in the modified Randall-Selitto paw pressure, the tail flick and plantar tests...
October 29, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28078254/achyranthes-japonica-nakai-water-extract-suppresses-binding-of-ige-antibody-to-cell-surface-fc%C3%A9-ri
#5
Sun Yup Shim, Mina Lee, Kyung Dong Lee
Achyranthes japonica Nakai (AJN) water extract has a variety of physiological properties, including anti-diabetic, anti-cancer, anti-inflammatory, anti-microbial, and anti-oxidative activities. In the present study, the inhibitory effects of AJN extract were investigated in high affinity immunoglobulin E receptor (FcɛRI)-mediated KU812F cells activation. AJN extract showed suppressive effects on histamine release and intracellular calcium [Ca(2+)]i elevation from anti-FcɛRI antibody (CRA-1)-stimulated cells in a dose-dependent manner...
December 2016: Preventive Nutrition and Food Science
https://www.readbyqxmd.com/read/28064014/gpr55-agonist-lysophosphatidylinositol-and-lysophosphatidylcholine-inhibit-endothelial-cell-hyperpolarization-via-gpr-independent-suppression-of-na-ca-2-exchanger-and-endoplasmic-reticulum-ca-2-refilling
#6
Alexander I Bondarenko, Fabrizio Montecucco, Olga Panasiuk, Vadim Sagach, Nataliya Sidoryak, Karim J Brandt, François Mach
Lysophosphatidylinositol (LPI) and lysophosphatidylcholine (LPC) are lipid signaling molecules that induce endothelium-dependent vasodilation. In addition, LPC suppresses acetylcholine (Ach)-induced responses. We aimed to determine the influence of LPC and LPI on hyperpolarizing responses in vitro and in situ endothelial cells (EC) and identify the underlying mechanisms. Using patch-clamp method, we show that LPI and LPC inhibit EC hyperpolarization to histamine and suppress Na(+)/Ca(2+) exchanged (NCX) currents in a concentration-dependent manner...
January 4, 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28059035/the-sdldl-reduces-mrc1-expression-level-and-secretion-of-histamine-in-differentiated-m2-macrophages-from-patients-with-coronary-artery-stenosis
#7
Ameneh Yarnazari, Mohammad Najafi, Parisa Hassanpour, Syed Reza Hosseini-Fard, Abdollah Amirfarhangi
The macrophage polarization is proposed to be involved in initial events and remodeling of atherosclerosis plaques. Mannose receptor, C type 1 (MRC1) is a trans-membrane glycoprotein participating in phagocytosis and, is highly expressed in the M2 macrophages. The aim of this study was to investigate the effects of sdLDL (small dense LDL) on the MRC1 gene expression level and secretion of histamine in the differentiated M2 macrophages from monocytes of patients with coronary artery stenosis and healthy subjects...
January 5, 2017: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/28057587/dual-role-of-histamine-on-microglia-induced-neurodegeneration
#8
REVIEW
S Barata-Antunes, A C Cristóvão, J Pires, S M Rocha, L Bernardino
Several hypotheses have been raised about the dual role of histamine in neurological disorders, and evidences have shown its crucial involvement in the modulation of microglia-mediated neuroinflammation. Previously, we reported that the administration of histamine induces a deleterious effect by promoting a pro-inflammatory phenotype on microglia that in turn compromises dopaminergic neuronal survival. Contrary, under lipopolysaccharide challenge, histamine inhibits the injurious effect of microglia-mediated inflammation, protecting dopaminergic neurons, suggesting that the modulation of microglial activity is dependent on the environmental context...
January 2, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28049400/elucidating-treatment-of-alzheimer-s-disease-via-different-receptors
#9
Badar Ul Islam, Mohd Shahnawaz Khan, Nasimudeen R Jabir, Mohammad Amjad Kamal, Shams Tabrez
Alzheimer's disease (AD) is an irreversible multifaceted neurodegenerative disorder that gradually degrades neuronal cells. Presently, it is the most common reason for the memory loss and dementia in older individuals. It is patho-physiologically described by extracellular amyloid beta (Aβ) deposition, intracellular neurofibrillary tangles (NFTs) retention, neuronal decline, and neurotransmitter system derangement. Various receptors such as nicotinic acetylcholine, N-methyl-D-aspartate, insulin, serotonin, adenosine, and histamine are actively involved in the physiological progression of AD...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28042359/non-prescription-proton-pump-inhibitors-for-self-treating-frequent-heartburn-the-role-of-the-canadian-pharmacist
#10
David Armstrong, Nardine Nakhla
Heartburn and acid regurgitation are the cardinal symptoms of gastroesophageal reflux and occur commonly in the Canadian population. Multiple non-prescription treatment options are available for managing these symptoms, including antacids, alginates, histamine-H2 receptor antagonists (H2RAs), and proton-pump inhibitors (PPIs). As a result, pharmacists are ideally positioned to recommend appropriate treatment options based upon an individual's needs and presenting symptoms, prior treatment response, comorbid medical conditions, and other relevant factors...
October 2016: Pharmacy Practice
https://www.readbyqxmd.com/read/28040476/asp73-dependent-and-independent-regulation-of-the-affinity-of-ligands-for-human-histamine-h1-receptors-by-na
#11
Shigeru Hishinuma, Kiyoe Kosaka, Chizuru Akatsu, Yoshihiro Uesawa, Hiroyuki Fukui, Masaru Shoji
The affinity of ligands for G-protein-coupled receptors (GPCR) is allosterically regulated by Na(+) via a highly conserved aspartate residue (Asp(2.50)) in the second transmembrane domain of GPCRs. In the present study, we examined the Na(+)-mediated regulation of the affinity of ligands for Gq/11-protein-coupled human histamine H1 receptors in Chinese hamster ovary cells. The affinities of 3 agonists and 20 antihistamines were evaluated by their displacement curves against the binding of [(3)H]-mepyramine to membrane preparations in the presence or absence of 100 mM NaCl...
December 28, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28026039/positive-correlation-of-vanilloid-receptor-subtype1-and-prostaglandin-e2-expression-with-pain-in-leiomyomas
#12
Yoshiko Kagimoto, Kenshi Yamasaki, Ryoko Shimada-Ohmori, Liu Nan, Yukikazu Numata, Setsuya Aiba
Cutaneous leiomyomas are benign smooth muscle tumors that are occasionally painful. The mechanism of pain related to leiomyoma is not fully understood. To investigate the possible involvement of algoneic factors in pain from cutaneous leiomyomas. We present a case of cutaneous leiomyoma with severe, diffused pain in a large area and collected 10 more specimens of cutaneous leiomyoma with or without pain in patient histories. We immunohistochemiacally examined the expression of algoneic factors: serotonin, histamin, Substance P, PGE2, BDKRB2, VR1 and CGRP...
December 27, 2016: Journal of Dermatology
https://www.readbyqxmd.com/read/28025094/serotonergic-mechanisms-of-trigeminal-meningeal-nociception-implications-for-migraine-pain
#13
Erkan Kilinc, Cindy Guerrero-Toro, Andrey Zakharov, Carmela Vitale, Max Gubert-Olive, Ksenia Koroleva, Arina Timonina, Liliana L Luz, Irina Shelukhina, Raisa Giniatullina, Fatma Tore, Boris V Safronov, Rashid Giniatullin
Serotonergic mechanisms play a central role in migraine pathology. However, the region-specific effects of serotonin (5-HT) mediated via multiple types of receptors in the nociceptive system are poorly understood. Using extracellular and patch-clamp recordings, we studied the action of 5-HT on the excitability of peripheral and central terminals of trigeminal afferents. 5-HT evoked long-lasting TTX-sensitive firing in the peripheral terminals of meningeal afferents, the origin site of migraine pain. Cluster analysis revealed that in majority of nociceptive fibers 5-HT induced either transient or persistent spiking activity with prevailing delta and theta rhythms...
December 23, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/28013257/use-of-proton-pump-inhibitors-and-the-risk-of-listeriosis-a-nationwide-registry-based-case-control-study
#14
Anne Kvistholm Jensen, Jacob Simonsen, Steen Ethelberg
BACKGROUND: Recent studies suggest that proton pump inhibitors (PPIs) may increase the risk for listeriosis. We aimed to investigate a potential association in cases of non-pregnancy associated listeriosis, using registry data. METHODS: We conducted a population-based case-control study using Danish health registries. Case-patients (n=721) were defined as patients ≥45 years notified with listeriosis, July 1994 to December 2012. We selected 34,800 control-subjects by risk-set sampling...
December 24, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28000952/human-basophils-are-differentially-activated-by-and-are-a-source-of-il-31
#15
Ulrike Raap, Manuela Gehring, Svea Kleiner, Urda Rüdrich, Britta Eiz-Vesper, Helmut Haas, Alexander Kapp, Bernhard F Gibbs
BACKGROUND: Basophils are important effector cells involved in the pathogenesis of inflammatory skin diseases including chronic urticaria which is associated by increased IL-31 serum levels. So far the effects of IL-31 on human basophils are unknown. OBJECTIVE: To analyse the functional role of IL-31 in basophil biology. METHODS: IL-31 expression was evaluated in skin samples derived from chronic spontaneous urticaria patients. Oncostatin M receptor (OSMR), IL-31 receptor A (RA) and IL-31 protein expressions were analysed on human basophils from healthy donors...
December 21, 2016: Clinical and Experimental Allergy: Journal of the British Society for Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/27997171/pyrimidine-based-inhibitors-of-dynamin-i-gtpase-activity-competitive-inhibition-at-the-pleckstrin-homology-domain
#16
Luke R Odell, Mohammed K Abdel-Hamid, Timothy A Hill, Ngoc Chau, Kelly A Young, Fiona M Deane, Jennette A Sakoff, Sofia Andersson, James A Daniel, Phillip J Robinson, Adam McCluskey
The large GTPase dynamin mediates membrane fission during clathrin-mediated endocytosis (CME). The aminopyrimidine compounds were reported to disrupt dynamin localization to the plasma membrane via the PH domain and implicate this mechanism in the inhibition of CME. We have used a computational approach of binding site identification, docking, and interaction energy calculations to design and synthesize a new library of aminopyrimidine analogues targeting site-2 of the pleckstrin homology (PH) domain. The optimized analogues showed low micromolar inhibition against both dynamin I (IC50 = 10...
December 20, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27988399/spasmogenic-and-spasmolytic-activities-of-agastache-mexicana-ssp-mexicana-and-a-mexicana-ssp-xolocotziana-methanolic-extracts-on-the-guinea-pig-ileum
#17
Rosa Ventura-Martínez, Rodolfo Rodríguez, María Eva González-Trujano, Guadalupe E Ángeles-López, Myrna Déciga-Campos, Claudia Gómez
ETHNOPHARMACOLOGICAL RELEVANCE: Agastache mexicana has been used in traditional medicine for relief of abdominal pain and treatment of other diseases. Two subspecies have been identified: A. mexicana ssp. mexicana (AMM) and A. mexicana ssp. xolocotziana (AMX) and both are used traditionally without distinction or in combination. AIM OF THE STUDY: To determine the effect of methanol extracts of A. mexicana ssp. mexicana and A. mexicana ssp. xolocotziana on gut motility and their possible mechanism of action...
January 20, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27986566/a-flavanone-derivative-from-the-asian-medicinal-herb-perilla-frutescens-potently-suppresses-ige-mediated-immediate-hypersensitivity-reactions
#18
Rikiya Kamei, Takashi Fujimura, Miki Matsuda, Kotaro Kakihara, Noriko Hirakawa, Kenji Baba, Kazuhisa Ono, Kenji Arakawa, Seiji Kawamoto
Perilla frutescens is a dietary leafy herb consumed as a traditional Japanese condiment as well as used for Chinese medicine with anti-inflammatory activity. Here we report a hitherto-unrecognized P. frutescens phytochemical that potently suppresses IgE-mediated type I hypersensitivity reactions. Structural analysis reveals that the purified anti-allergic compound (Perilla-derived methoxyflavanone, PDMF) is identified as 8-hydroxy-5,7-dimethoxyflavanone. PDMF significantly inhibits IgE-mediated histamine release from RBL-2H3 rat basophilic leukemia cells as compared with those seen in known P...
January 29, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27986539/antihistamines-as-promising-drugs-in-cancer-therapy
#19
REVIEW
Ana I Faustino-Rocha, Rita Ferreira, Adelina Gama, Paula A Oliveira, Mário Ginja
Histamine is a biogenic amine, synthetized and released by mast cells, which acts as a vasodilator in several pathologic processes, namely in allergies and conjunctivitis. Its role on cancer is not fully understood. High levels of histamine have been associated with a bivalent behavior in regulation of several tumors (i.e. cervical, ovarian, vaginal, uterine, vulvar, colorectal cancer, and melanoma), promoting or inhibiting their growth. Histamine receptors (H1, H2, H3 and H4) are present in a vast group of cells, including tumor cells, making them sensitive to histamine variations...
December 13, 2016: Life Sciences
https://www.readbyqxmd.com/read/27979988/the-effect-of-acute-aerobic-exercise-and-histamine-receptor-blockade-on-arterial-stiffness-in-african-americans-and-caucasians
#20
Huimin Yan, Sushant M Ranadive, Abbi D Lane-Cordova, Rebecca M Kappus, Michael A Behun, Marc D Cook, Jeffrey A Woods, Kenneth R Wilund, Tracy Baynard, John R Halliwill, Bo Fernhall
African-Americans (AA) exhibit exaggerated central blood pressure (BP) and arterial stiffness measured by pulse wave velocity (PWV) in response to an acute bout of maximal exercise compared to Caucasians (CA). However, whether potential racial differences exist in central BP, elastic, or muscular arterial distensibility following submaximal aerobic exercise remains unknown. Histamine receptor activation mediates sustained post-exercise hyperemia in CA but the effect on arterial stiffness is unknown. This study sought to determine the effects of an acute bout of aerobic exercise on central BP and arterial stiffness, and the role of histamine receptors, in AA and CA...
December 15, 2016: Journal of Applied Physiology
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