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https://www.readbyqxmd.com/read/28228363/efficient-synthesis-of-%C3%AE-fluoromethylhistidine-di-hydrochloride-and-demonstration-of-its-efficacy-as-a-glutathione-s-transferase-inhibitor
#1
Kelly L Considine, Lazaros Stefanidis, Karl G Grozinger, Joseph Audie, Benjamin J Alper
Histidine decarboxylase (HDC) is an enzyme that converts histidine to histamine. Inhibition of HDC has several medical applications, and HDC inhibitors are of considerable interest for the study of histidine metabolism. (S)-α-Fluoromethylhistidine di-hydrochloride (α-FMH) is a potent HDC inhibitor that is commercially available at high cost in small amounts only. Here we report a novel, inexpensive, and efficient method for synthesis of α-FMH using methyl 2-aziridinyl-3-(N-triphenylmethyl-4-imidazolyl) propionate and HF/pyridine, with experimental yield of 57%...
February 14, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28228338/extra-and-intracellular-calcium-signaling-pathway-s-differentially-regulate-histamine-induced-myometrial-contractions-during-early-and-mid-pregnancy-stages-in-buffaloes-bubalus-bubalis
#2
Abhishek Sharma, Udayraj P Nakade, Soumen Choudhury, Rajkumar Singh Yadav, Satish Kumar Garg
This study examines the differential role of calcium signaling pathway(s) in histamine-induced uterotonic action during early and mid-pregnancy stages in buffaloes. Compared to mid pregnancy, tonic contraction, amplitude and mean-integral tension were significantly increased by histamine to produce myometrial contraction during early pregnancy with small effects on phasic contraction and frequency. Although uterotonic action of histamine during both stages of pregnancy is sensitive to nifedipine (a L-type Ca(2+) channels blocker) and NNC55-0396 (T-type Ca(2+) channels blocker), the role of extracellular calcium seems to be more significant during mid-pregnancy as in this stage histamine produced only 9...
February 7, 2017: Animal Reproduction Science
https://www.readbyqxmd.com/read/28226418/omalizumab-for-the-treatment-of-chronic-idiopathic-urticaria-systematic-review-of-the-literature
#3
Alessandro Tonacci, Lucia Billeci, Giovanni Pioggia, Michele Navarra, Sebastiano Gangemi
Omalizumab is recombinant humanized monoclonal antibody to immunoglobulin E. Guidelines for the treatment of chronic idiopathic urticaria (also known as chronic spontaneous urticaria) recommend the use of omalizumab as third-line therapy in addition to high doses of histamine receptor type 1 (H1 ) antihistamines when they are unsuccessful as first- and second-line therapy. We performed a systematic review of the literature to identify studies that evaluated the efficacy of omalizumab for the treatment of chronic idiopathic urticaria, both in controlled and real-world settings, to assess its potential role as a preferred therapy...
February 22, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28223162/the-roles-of-histamine-and-its-receptor-ligands-in-central-nervous-system-disorders-an-update
#4
REVIEW
Weiwei Hu, Zhong Chen
The neurotransmitter histamine receives less attention compared with other biogenic amines, because of its moderate action in the central nervous system (CNS). However, recent evidence suggests that histamine plays an important role in multiple CNS disorders including insomnia, narcolepsy, Parkinson's diseases, schizophrenia, Alzheimer's disease, and cerebral ischemia. New insights are emerging into the potential roles of histamine receptors as targets for the treatment of these diseases. Although some histamine related agents have failed in clinical trials, current preclinical studies suggest that this neurotransmitter may still have extensive applications in treating CNS disorders, however, advanced studies are warranted...
February 18, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28221983/biogenic-amines-and-predictive-models-of-quality-of-rainbow-trout-oncorhynchus-mykiss-fillets-during-storage
#5
Qingzheng Li, Jian Lv, Longteng Zhang, Zehong Dong, Ligeng Feng, Yongkang Luo
To estimate biogenic amines and changes in quality of rainbow trout ( Oncorhynchus mykiss ) fillets at different temperatures, we determined the sensory attributes, total volatile basic nitrogen (TVB-N), total viable counts (TVC), and biogenic amines (BAs) of samples that were untreated (CK) or dry cured with 1.8% salt (T). There was no significant difference between CK and T samples in terms of TVB-N, TVC, and BAs. TVB-N and TVC increased significantly (P < 0.05) with storage time at 3, 9, and 15°C. Putrescine (PUT) and cadaverine (CAD) increased significantly (P < 0...
February 2017: Journal of Food Protection
https://www.readbyqxmd.com/read/28221938/reduction-of-biogenic-amines-during-miso-fermentation-by-lactobacillus-plantarum-as-a-starter-culture
#6
Yi-Chen Lee, Hsien-Feng Kung, Ya-Ling Huang, Chien-Hui Wu, Yu-Ru Huang, Yung-Hsiang Tsai
Lactobacillus plantarum D-103 isolated from a miso product that possesses amine-degrading activity was used as a starter culture in miso fermentation (25°C for 120 days) in this study. The salt content in control samples (without starter culture) and inoculated samples (inoculated with L. plantarum D-103) remained constant at 10.4% of the original salt concentration throughout fermentation, whereas the pH value decreased from 6.2 to 4.6 during fermentation. The inoculated samples had significantly lower (P < 0...
September 2016: Journal of Food Protection
https://www.readbyqxmd.com/read/28221888/histamine-formation-in-a-dry-salted-twaite-shad-alosa-fallax-lacustris-product
#7
Mauro Vasconi, Federica Bellagamba, Cristian Bernardi, Piera Anna Martino, Vittorio Maria Moretti
Landlocked shad is a freshwater clupeid fish ( Alosa fallax lacustris ) whose consumption is associated with the risk of scombrotoxin poisoning. Traditionally, fresh shad are subjected to an artisanal processing procedure, consisting of dry salting and maturation under pressure, to give a fish product named missoltino , which is stored in large metallic barrels and is sold to local consumers and restaurants. In recent years, the introduction of modern food packaging technologies has enabled this product to also be distributed in shops and supermarkets...
January 2017: Journal of Food Protection
https://www.readbyqxmd.com/read/28219065/synergistic-actions-of-histamine-releasing-factor-and-histamine-releasing-factor-reactive-ige-in-chronic-urticaria
#8
Xianqiong Huang, Zhaoyang Li, Renshan Sun
The etiology of chronic urticaria (CU) remains elusive. Histamine-releasing factor (HRF) is reported to have a proinflammatory role in asthma and immediate hypersensitivity of the skin. The aim of this study was to examine the role of HRF in the pathogenesis of CU. Forty patients with CU were enrolled and their serum HRF concentrations were determined by ELISA. The results demonstrated that the concentrations of HRF and HRF-reactive IgE in the CU group were significantly higher than those in the control group, and there was a significant linear correlation between HRF and HRF-reactive IgE concentrations (r = 0...
February 21, 2017: International Archives of Allergy and Immunology
https://www.readbyqxmd.com/read/28218311/s-38093-a-histamine-h3-antagonist-inverse-agonist-promotes-hippocampal-neurogenesis-and-improves-context-discrimination-task-in-aged-mice
#9
Jean-Philippe Guilloux, Benjamin A Samuels, Indira Mendez-David, Alice Hu, Marjorie Levinstein, Charlène Faye, Maryam Mekiri, Elisabeth Mocaer, Alain M Gardier, René Hen, Aurore Sors, Denis J David
Strategies designed to increase adult hippocampal neurogenesis (AHN) may have therapeutic potential for reversing memory impairments. H3 receptor antagonists/inverse agonists also may be useful for treating cognitive deficits. However, it remains unclear whether these ligands have effects on AHN. The present study aimed to investigate the effects of a 28-day treatment with S 38093, a novel brain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (proliferation, maturation and survival) in 3-month-old and in aged 16-month-old mice...
February 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28217875/mechanisms-of-pruritogen-induced-activation-of-itch-nerves-in-isolated-mouse-skin
#10
F Ru, H Sun, D Jurcakova, R A Herbstsomer, J Meixong, X Dong, B J Undem
Chloroquine (CQ) and histamine are pruritogens commonly used to study itch in the mouse. A novel skin-nerve preparation was used to evaluate chloroquine (CQ)- and histamine- induced activation of afferent nerves in the dorsal thoracic skin of the mouse. All CQ sensitive nerves were C-fibres, and were also sensitive to histamine. The response to CQ, but not histamine, was largely absent in mrgpr cluster Δ -/- mice supporting the hypothesis that CQ evokes itch largely via stimulation of MrgprA3 receptors. The CQ-induced action potential discharge was largely absent in phospholipase Cβ3 knockout animals...
February 19, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28216960/pharmacological-evaluation-of-apium-leptophyllum-pers-on-bronchial-asthma
#11
Himanshu Bhusan Sahoo, Rakesh Sagar, Ganesh Patro, Madhulita Panda, Saroj Kumar Sahoo, D Priyadarshini
OBJECTIVE: The present study was to investigate the antiasthmatic potential from the flavonoid fraction of Apium leptophyllum fruit (FFALF) to validate its traditional claim. MATERIALS AND METHODS: The antiasthmatic activity of FFALF was evaluated by histamine or acetylcholine-induced bronchospasm model in guinea pigs, compound 48/80 induced mast cell degranulation in albino rats and histamine-induced tracheal contraction in guinea pig. The preconvulsion dyspnea time at 0(th) and 7(th) day at the dose of 100 and 200 mg/kg in guinea pig's bronchospasm model, the percentage of granulated and degranulated mast cell at the dose of 500, 750, and 1000 μg/ml in rats and tracheal contraction at the dose of 500, 750, and 1000 μg/ml in guinea pig were measured and compared with respective control groups...
October 2016: Journal of Pharmacy & Bioallied Sciences
https://www.readbyqxmd.com/read/28211587/histaminergic-and-non-histaminergic-elicited-itch-is-attenuated-in-capsaicin-evoked-areas-of-allodynia-and-hyperalgesia-a-healthy-volunteer-study
#12
H H Andersen, J Elberling, N Sharma, L E Hauberg, P Gazerani, L Arendt-Nielsen
BACKGROUND: Chronic pain patients with sensitization may exhibit decreased sensitivity to normally pruritogenic sensory stimuli and moreover occasionally perceive these as painful. This study explored the relationship between itch and pain, by evaluating histaminergic and non-histaminergic itch evoked in capsaicin-induced allodynic and hyperalgesic areas. METHODS: In 28 healthy volunteers, capsaicin (100 μg/0.1 mL) was injected intradermally in the volar forearm to establish secondary dysesthesias...
February 17, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28210628/usefulness-of-sweat-management-for-patients-with-adult-atopic-dermatitis-regardless-of-sweat-allergy-a-pilot-study
#13
Sakae Kaneko, Hiroyuki Murota, Susumu Murata, Ichiro Katayama, Eishin Morita
Background. Sweat is an aggravating factor in atopic dermatitis (AD), regardless of age. Sweat allergy may be involved in AD aggravated by sweating. Objective. We investigated whether sweat exacerbates adult AD symptoms and examined the extent of sweat allergy's involvement. Method. We asked 34 AD patients (17 men, 17 women; mean age: 27.8 years) to record the extent to which sweat aggravated their symptoms on a 10-point numerical scale. Participant responses were compared with histamine release tests (HRT)...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28210249/feeding-a-high-concentration-diet-induces-unhealthy-alterations-in-the-composition-and-metabolism-of-ruminal-microbiota-and-host-response-in-a-goat-model
#14
Canfeng Hua, Jing Tian, Ping Tian, Rihua Cong, Yanwen Luo, Yali Geng, Shiyu Tao, Yingdong Ni, Ruqian Zhao
There is limited knowledge about the impact of long-term feeding a high-concentrate (HC) diet on rumen microbiota, metabolome, and host cell functions. In this study, a combination of mass spectrometry-based metabolomics techniques, 454 pyrosequencing of 16S rDNA genes, and RT-PCR was applied to evaluate the changes of ruminal microbiota composition, ruminal metabolites, and related genes expression in rumen epithelial cells of lactating goats received either a 35% concentrate diet or a 65% concentrate diet for 4 or 19 weeks, respectively...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28209924/brain-histamine-and-behavioral-neuroscience
#15
EDITORIAL
Andrea Santangelo, Maria Beatrice Passani, Maurizio Casarrubea
No abstract text is available yet for this article.
February 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28209485/effects-of-clozapine-on-adipokine-secretions-productions-and-lipid-droplets-in-3t3-l1-adipocytes
#16
Tomomi Tsubai, Akira Yoshimi, Yoji Hamada, Makoto Nakao, Hiroshi Arima, Yutaka Oiso, Yukihiro Noda
Clozapine, a second-generation antipsychotic (SGA), is a cause of side effects related to metabolic syndrome. The participation of serotonin 5-HT2C and histamine H1 receptors in the central nervous system has been reported as a mechanism of the weight gain caused by clozapine. In the present study, we investigated the direct pharmacological action of clozapine on the 3T3-L1 adipocytes and compared it to that of blonanserin, an SGA with low affinity for both receptors. Short-term exposure to clozapine decreased secretion and mRNA expression of leptin...
January 28, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28199959/central-neuronal-functions-of-histamine-h4-receptors
#17
EDITORIAL
Maria Domenica Sanna, Nicoletta Galeotti
No abstract text is available yet for this article.
February 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28196712/ipomoea-pes-caprae-l-r-br-convolvulaceae-as-a-topical-herbal-medicine-to-relieve-pain-and-inflammation-promising-tool-against-effects-due-to-toxin-skin-contact
#18
Cristiane da Silva Barth, Hugo Guilherme Tolentino de Souza, Lilian W Rocha, Gislaine Francieli da Silva, Mariana Ferreira Dos Anjos, Veronica D'Avila Pastor, Tania Mari Belle Bresolin, Angelica Garcia Couto, José Roberto Santin, Nara Lins Meira Quintão
ETHNOPHARMACOLOGICAL RELEVANCE: Ipomoea pes-caprae is known as bayhops, beach morning glory or goat's foot, and in Brazil as salsa-de-praia. Its leaves are used in worldwide folk medicine for the relief of jellyfish-stings symptoms. The literature only reports the anti-inflammatory and neutralizing effects of a nonpolar plant derived, without validating the popular use or exploring the mechanism of action. AIM OF THE STUDY: This study aimed to evaluate and validate the topical effects of a semisolid containing hydroethanolic extract obtained from the aerial parts of I...
February 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28196418/automated-algorithm-for-detection-of-transient-adenosine-release
#19
Ryan P Borman, Ying Wang, Michael D Nguyen, Mallikarjunarao Ganesana, Scott T Lee, B Jill Venton
Spontaneous adenosine release events have been discovered in the brain that last only a few seconds. The identification of these adenosine events from fast-scan cyclic voltammetry (FSCV) data is difficult due to the random nature of adenosine release. In this study, we develop an algorithm that automatically identifies and characterizes adenosine transient features, including event time, concentration, and duration. Automating the data analysis reduces analysis time from 10 to 18 h to about 40 min per experiment...
February 15, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28194483/-placebo-effect-in-clinical-trials-with-allergen-specific-immunotherapy-with-inhalant-allergens
#20
B Wedi, D Wieczorek, A Kapp
Placebo effects play an important role in the treatment of allergic diseases. Therefore, in this study, we analysed the described effects of placebo in all double-blind placebo-controlled clinical trials of allergen-specific immunotherapy (ASIT) with inhalant allergens (birch, grass, house dust mites) listed in the tables (updated July 2016) attached to the German S2k guideline on allergen-specific immunotherapy in IgE-mediated allergic diseases. The most common placebo consisted of verum without allergen, but when the subcutaneous route was used, histamine was sometimes added...
February 13, 2017: Der Hautarzt; Zeitschrift Für Dermatologie, Venerologie, und Verwandte Gebiete
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