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Histamine receptors

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https://www.readbyqxmd.com/read/28921918/proteomic-response-of-human-umbilical-vein-endothelial-cells-to-histamine-stimulation
#1
Pelin Esma Emirbayer, Ankit Sinha, Vladimir Ignatchenko, Stefanie Hoyer, Jan Dörrie, Niels Schaft, Monika Pischetsrieder, Thomas Kislinger
The histamine receptors (HRs) represent a subclass of G protein-coupled receptors (GPCRs) and comprise four subtypes. Due to their numerous physiological and pathological effects, HRs are popular drug targets for the treatment of allergic reactions or the regulation of gastric acid secretion. Hence, an understanding of the functional selectivity of HR ligands has gained importance. These ligands can bind to specific GPCRs and selectively activate defined pathways. Supporting the activation of a therapeutically necessary pathway without the activation of other signaling cascades can result in drugs with more specific activity and fewer side effects...
September 18, 2017: Proteomics
https://www.readbyqxmd.com/read/28919798/comparative-effects-of-the-%C3%AF-3-polyunsaturated-fatty-acid-derivatives-resolvins-e1-and-d1-and-protectin-dx-in-models-of-inflammation-and-pain
#2
Flávia Cs Fonseca, Ricardo M Orlando, Regina Mm Turchetti-Maia, Janetti Nogueira de Francischi
PURPOSE: Specialized pro-resolving lipid mediators (SPMs), also known as lipoxins, resolvins (Rvs), protectins and maresins, have been implicated in the resolution of the inflammatory process. However, a systematic comparison of their activity in the relief of inflammation and pain models is still lacking. MATERIALS AND METHODS: The effects of Rvs E1 and D1 and protectin DX (PDX) were assessed in rat paws inflamed by the standard proinflammatory stimulus carrageenan or by histamine, 5-hydroxytryptamine, substance P or prostaglandin E2...
2017: Journal of Inflammation Research
https://www.readbyqxmd.com/read/28919488/mast-cells-derived-from-human-induced-pluripotent-stem-cells-are-useful-for-allergen-tests
#3
Akira Igarashi, Yasuhiro Ebihara, Tomoaki Kumagai, Hiroyuki Hirai, Kinya Nagata, Kohichiro Tsuji
BACKGROUND: Several methods have been developed to detect allergen-specific IgE in sera. The passive IgE sensitization assay using human IgE receptor-expressing rat cell line RBL-2H3 is a powerful tool to detect biologically active allergen-specific IgE in serum samples. However, one disadvantage is that RBL-2H3 cells are vulnerable to high concentrations of human sera. Only a few human cultured cell lines are easily applicable to the passive IgE sensitization assay. However, the use of human induced pluripotent stem cells (iPSCs) to generate human mast cells (MCs) has not yet been reported...
September 14, 2017: Allergology International: Official Journal of the Japanese Society of Allergology
https://www.readbyqxmd.com/read/28916845/pharmacological-investigations-on-mast-cell-stabilizer-and-histamine-receptor-antagonists-in-vincristine-induced-neuropathic-pain
#4
Amteshwar Singh Jaggi, Gunjanpreet Kaur, Anjana Bali, Nirmal Singh
The present study was designed to investigate the role of mast cells and mast cell-derived histamine in vincristine-induced neuropathic pain. Neuropathic pain was induced by administration of vincristine (100 μg/kg, i.p.) over a period of 10 days, with a break of 2 days, and pain behavioural estimations including pin prick, hot plate and acetone spray tests were performed to assess mechanical and heat hyperalgesia and cold allodynia, respectively, on days 0, 14 and 28. Mast cell stabilizer, sodium cromoglycate, H1 receptor antagonist promethazine and H2 receptor antagonist ranitidine were administered over a period of 12 days...
September 15, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28912446/an-injectable-hydrogel-enhances-tissue-repair-after-spinal-cord-injury-by-promoting-extracellular-matrix-remodeling
#5
Le Thi Anh Hong, Young-Min Kim, Hee Hwan Park, Dong Hoon Hwang, Yuexian Cui, Eun Mi Lee, Stephanie Yahn, Jae K Lee, Soo-Chang Song, Byung Gon Kim
The cystic cavity that develops following injuries to brain or spinal cord is a major obstacle for tissue repair in central nervous system (CNS). Here we report that injection of imidazole-poly(organophosphazenes) (I-5), a hydrogel with thermosensitive sol-gel transition behavior, almost completely eliminates cystic cavities in a clinically relevant rat spinal cord injury model. Cystic cavities are bridged by fibronectin-rich extracellular matrix. The fibrotic extracellular matrix remodeling is mediated by matrix metalloproteinase-9 expressed in macrophages within the fibrotic extracellular matrix...
September 14, 2017: Nature Communications
https://www.readbyqxmd.com/read/28894313/need-for-a-randomized-controlled-trial-of-stress-ulcer-prophylaxis-in-critically-ill-children-a-canadian-survey
#6
Mark Duffett, Karen Choong, Jennifer Foster, Elaine Gilfoyle, Jacques Lacroix, Deborah J Cook
BACKGROUND: Stress ulcer prophylaxis is commonly used in pediatric critical care, to prevent upper gastrointestinal bleeding. The most frequently used agents are histamine-2 receptor antagonists (H2RAs) and proton pump inhibitors (PPIs). The risk-benefit ratio for stress ulcer prophylaxis is uncertain, because data from randomized clinical trials (RCTs) on the effectiveness and harms of prophylaxis in children are limited. OBJECTIVE: To describe the views of Canadian pediatric intensivists about a future RCT of stress ulcer prophylaxis...
July 2017: Canadian Journal of Hospital Pharmacy
https://www.readbyqxmd.com/read/28892404/mechanisms-underlying-metabolic-disturbances-associated-with-psychosis-and-antipsychotic-drug-treatment
#7
Gavin P Reynolds, Olga O McGowan
The increase in cardiovascular disease and reduced life expectancy in schizophrenia likely relate to an increased prevalence of metabolic disturbances. Such metabolic risk factors in schizophrenia may result from both symptom-related effects and aetiological factors. However, a major contributory factor is that of treatment with antipsychotic drugs. These drugs differ in effects on body weight; the underlying mechanisms are not fully understood and may vary between drugs, but may include actions at receptors associated with the hypothalamic control of food intake...
August 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28888822/discovery-of-novel-steroidal-histamine-h3-receptor-antagonists-inverse-agonists
#8
Istvan Ledneczki, Pál Tapolcsányi, Eszter Gábor, János Éles, István Greiner, Éva Schmidt, Zsolt Némethy, Rita Soukupné Kedves, Ottilia Balázs, Viktor Román, György Lévay, Sándor Mahó
Emerging from an HTS campaign, novel steroid-based histamine H3 receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in compound 4 as lead molecule. During the lead optimization due to the versatile modifications of diamino steroid derivatives, several in vitro potent compounds with subnanomolar binding affinities to histamine H3 receptors were found. The unfavorable binding to rat muscarinic receptors was successfully reduced by tuning the basicity...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28888712/simultaneous-optimization-of-ph-and-binary-organic-composition-by-grid-form-modeling-of-the-retention-behavior-in-reversed-phase-ultra-high-performance-liquid-chromatography
#9
Tsukasa Sasaki, Kenichiro Todoroki, Toshimasa Toyo'oka
A novel computer-assisted methodology for the simultaneous optimization of aqueous pH and binary organic eluent composition through a broad range of analytical conditions of reversed-phase ultra high-performance liquid chromatography is proposed. Two of nonlinear prediction models were employed to fit into the retention time (tR) on a linear gradient elution with a predefined slope. One model was derived from Bernoulli-type probability distribution to predict the value of tR against the pH value of the aqueous eluent...
September 1, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28887947/therapeutic-pipeline-for-atopic-dermatitis-end-of-the-drought
#10
REVIEW
Amy S Paller, Kenji Kabashima, Thomas Bieber
Until the past year, our therapeutic armamentarium for treating atopic dermatitis (AD) was still primarily topical corticosteroids and, for more severe disease, systemic immunosuppressants. The pipeline of more targeted topical and systemic therapies is expanding based on our growing understanding of the mechanism for AD and is particularly focused on suppressing the skewed immune activation. Most agents are in phase 2 clinical trials. Crisaborole, a topical phosphodiesterase 4 (PDE4) inhibitor, became available in late 2016 in the United States for mild-to-moderate AD, with other PDE4 inhibitors, an agonist of the aryl hydrocarbon receptor, Janus kinase inhibitors, and commensal organisms also in trials for topical application...
September 2017: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28887671/histamine-2-receptor-antagonism-elicits-protection-against-doxorubicin-induced-cardiotoxicity-in-rodent-model
#11
Sundar Kumar Kondru, Ajay Godwin Potnuri, Lingesh Allakonda, Prasad Konduri
Doxorubicin (DOX), an anthracycline-based antibiotic, is regularly used in the management of carcinomas, and haematological malignancies have been downplayed in chemotherapy because of its ability to induce dilated cardiomyopathy (DCM). Dexrazoxane is approved to combat the cardiotoxicity, but limited by its adverse effects. Redox imbalance and reactive oxygen species generation plays major role in DOX-induced cardiotoxicity. Histamine, known to mediate various cardiovascular effects, but nevertheless the role of histamine or its receptors in DOX-induced DCM is remained obscure...
September 8, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28886461/time-dependent-effects-of-olanzapine-treatment-on-the-expression-of-histidine-decarboxylase-h1-and-h3-receptor-in-the-rat-brain-the-roles-in-olanzapine-induced-obesity
#12
Meng He, Qingsheng Zhang, Chao Deng, Tiantian Jin, Xueqin Song, Hongqing Wang, Xu-Feng Huang
Antipsychotic treatment, particularly olanzapine and clozapine, induces severe obesity. The Histamine H1 receptor is considered to be an important contributor to olanzapine-induced obesity, however how olanzapine modulates the histaminergic system is not sufficiently understood. This study examined the effect of olanzapine on key molecules of the histaminergic system, including histidine decarboxylase (HDC), H1 receptor (H1R) and H3 receptor (H3R), in the brain at different stages of olanzapine-induced obesity...
August 24, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28885223/prescription-audit-of-nsaids-and-gastroprotective-strategy-in-elderly-in-primary-care
#13
Khalid Ahmed Jassim Al Khaja, Sindhan Veeramuthu, Husain Ahmed Isa, Reginald Paul Sequeira
BACKGROUND: The use of non-steroidal anti-inflammatory drug (NSAIDs) is deemed a major risk factor for peptic ulcer disease in elderly population that requires concomitant therapy with gastroprotective agents (GPAs). OBJECTIVE: This study evaluated the rational prescribing of NSAIDs and GPAs, and extent of adherence to the guideline recommendations in primary care. METHODS: Nationwide audit of prescriptions issued to elderly patients (≥65 years) with hypertension or diabetic hypertension in primary care...
2017: International Journal of Risk & Safety in Medicine
https://www.readbyqxmd.com/read/28884989/hydroxychloroquine-in-the-treatment-of-anti-histamine-refractory-chronic-spontaneous-urticaria-randomized-single-blinded-placebo-controlled-trial-and-an-open-label-comparison-study
#14
T Boonpiyathad, A Sangasapaviliya
Background. The management of anti-histamine refractory chronic spontaneous urticaria (CSU) has poorly defined therapeutic options. Some patients with CSU respond poorly to a fourfold increase in dosage of H1-anti-histamines treatment. Aim. The objective of this study was to determine the effect of an adjunct treatment of hydroxychloroquine (HCQ) on remission rate and reduction of urticarial symptoms. Methods. Sixty subjects with anti-histamine refractory CSU were randomly assigned to 400 mg of HCQ daily or placebo for 12 weeks in a single blind placebo controlled trial...
September 2017: European Annals of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28878769/protective-role-of-mast-cells-in-primary-systemic-vasculitis-a-perspective
#15
Jason M Springer, Vineesh V Raveendran, Selina A Gierer, Mehrdad Maz, Kottarappat N Dileepan
Mast cells are important cells of the immune system. Although traditionally considered as key players in allergic and hypersensitivity reactions, emerging evidence suggests that mast cells have many complex roles in vascular disease. These include regulation of vasodilation, angiogenesis, activation of matrix metalloproteinases, apoptosis of smooth muscle cells, and activation of the renin angiotensin system. Mast cells are also known to play an immunomodulatory role via modulation of regulatory T-cell (Treg), macrophage and endothelial cell functions...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28877931/prostaglandin-e2-inhibits-histamine-evoked-ca2-release-in-human-aortic-smooth-muscle-cells-through-hyperactive-camp-signalling-junctions-and-protein-kinase-a
#16
Emily J A Taylor, Evangelia Pantazaka, Kathryn L Shelley, Colin W Taylor
In human aortic smooth muscle cells (ASMC), prostaglandin E2 (PGE2) stimulates adenylyl cyclase (AC) and attenuates the increase in intracellular free Ca(2+) concentration ([Ca(2+)]i) evoked by activation of histamine H1 receptors. The mechanisms are not resolved. We show that cAMP mediates inhibition of histamine-evoked Ca(2+) signals by PGE2 Exchange proteins activated by cAMP (EPACs) were not required, but the effects were attenuated by inhibition of cAMP-dependent protein kinase (PKA). PGE2 had no effect on the Ca(2+) signals evoked by protease-activated receptors, heterologously expressed muscarinic M3 receptors, or by direct activation of inositol 1,4,5-trisphosphate (IP3) receptors by photolysis of caged IP3 The rate of Ca(2+) removal from the cytosol was unaffected by PGE2, but PGE2 attenuated histamine-evoked IP3 accumulation...
September 6, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28877402/effects-of-s-38093-an-antagonist-inverse-agonist-of-histamine-h3-receptors-in-models-of-neuropathic-pain-in-rats
#17
T Chaumette, E Chapuy, E Berrocoso, M Llorca-Torralba, L Bravo, J A Mico, M Chalus, A Eschalier, D Ardid, F Marchand, A Sors
BACKGROUND: Histamine H3 receptors are mainly expressed on CNS neurons, particularly along the nociceptive pathways. The potential involvement of these receptors in pain processing has been suggested using H3 receptor inverse agonists. METHODS: The antinociceptive effect of S 38093, a novel inverse agonist of H3 receptors, has been evaluated in several neuropathic pain models in rat and compared with those of gabapentin and pregabalin. RESULTS: While S 38093 did not change vocalization thresholds to paw pressure in healthy rats, it exhibited a significant antihyperalgesic effect in the Streptozocin-induced diabetic (STZ) neuropathy model after acute and chronic administration and, in the chronic constriction injury (CCI) model only after chronic administration, submitted to the paw-pressure test...
September 6, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28872471/lung-xenotransplantation
#18
Hisashi Sahara, Hironosuke Watanabe, Thomas Pomposelli, Kazuhiko Yamada
PURPOSE OF REVIEW: This review describes the most recent progress in xeno lung transplantation (XLTx) to date. It describes the potential mechanisms of early xeno lung graft loss, as well as the latest therapeutic strategies to overcome them. RECENT FINDINGS: Using ex-vivo perfusion models of porcine lungs with human blood, the use of genetically modified pig lungs along with novel pharmaceutical approaches has recently been studied. Strategies that have demonstrated improved lung survival include the knockout of known xenoantigens (GalTKO and N-glycolylneuraminic acid-KO), genes that regulate complement activation (hCD46 and hCD55), as well as the inflammation/coagulation cascade (human leukocyte antigen-E, human thrombomodulin, human endothelial protein C receptor, hCD47, hCD39, hCD73 and heme oxygenase-1)...
September 1, 2017: Current Opinion in Organ Transplantation
https://www.readbyqxmd.com/read/28867718/role-of-mast-cells-in-bronchial-contraction-in-nonallergic-obstructive-lung-pathology
#19
Nataliya A Kuzubova, Elena S Lebedeva, Olga N Titova, Anatoliy N Fedin, Ivetta V Dvorakovskaya
The role of mast cells in contractile bronchial smooth muscle activity has been evaluated in a model of chronic obstructive pulmonary disease induced in rats that were intermittently exposed to nitrogen dioxide (NO2) for 60 days. Starting from the 31st day, one group of rats inhaled sodium cromoglycate before exposure to NO2 to stabilize mast cell membranes. The second group (control) was not treated. Isometric smooth muscle contraction was analysed in isolated bronchial samples in response to nerve and smooth muscle stimulation...
2017: Journal of Smooth Muscle Research, Nihon Heikatsukin Gakkai Kikanshi
https://www.readbyqxmd.com/read/28867637/sinomenine-induced-histamine-release-like-anaphylactoid-reactions-are-blocked-by-tranilast-via-inhibiting-nf-%C3%AE%C2%BAb-signaling
#20
Lufen Huang, Yan Dong, Jianlin Wu, Peixun Wang, Hua Zhou, Ting Li, Liang Liu
Zhengqing Fengtongning (ZQFTN), the pharmaceutical preparation of sinomenine (SIN) derived from the medicinal plant Sinmenium acutum, is well-known in China as an effective treatment for rheumatoid arthritis (RA). However, its histamine-release anaphylactoid reactions (HRARs) occur often in some patients. Therefore, it is desirable to establish effective clinical protocols to manage such HRARs. In the study, rat models with systemic HRARs and local HRARs of the skin were established. The level of vascular permeability and mast cell numbers was determined by quantitative analysis using Evans blue dye and histological assays...
August 31, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
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