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Histamine receptors

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https://www.readbyqxmd.com/read/28449186/the-risk-of-lower-gastrointestinal-bleeding-in-low-dose-aspirin-users
#1
W-C Chen, K-H Lin, Y-T Huang, T-J Tsai, W-C Sun, S-K Chuah, D-C Wu, P-I Hsu
BACKGROUND: Aspirin increases the risk of gastrointestinal bleeding. AIM: To investigate the risk of lower gastrointestinal bleeding (LGIB) in aspirin users. METHODS: Low-dose (75-325 mg daily) aspirin users and controls matched by age, gender and enrollment time in a 1:5 ratio were selected from 1 million randomly sampled subjects in the National Health Insurance Research Database of Taiwan. Cox proportional hazard regression models were developed to evaluate the predictors of LGIB with adjustments for age, gender, comorbidities including coronary artery disease, ischaemic stroke, diabetes, hypertension, chronic kidney disease, liver cirrhosis, chronic obstructive pulmonary disease, dyslipidemia, uncomplicated peptic ulcer disease, history of peptic ulcer bleeding, and concomitant use of clopidogrel, ticlopidine, warfarin, nonsteroidal anti-inflammatory drugs (NSAIDs), cyclooxygenase-2 inhibitors, steroids, proton pump inhibitors (PPIs), histamine-2 receptor antagonists (H2RAs), nitrates, alendronate, selective serotonin reuptake inhibitors (SSRIs) and calcium channel blockers...
April 27, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28448991/participation-of-antidiuretic-hormone-adh-in-asthma-exacerbations-induced-by-psychological-stress-via-pka-pkc-signal-pathway-in-airway-related-vagal-preganglionic-neurons-avpns
#2
Lili Hou, Lei Zhu, Min Zhang, Xingyi Zhang, Guoqing Zhang, Zhenwei Liu, Qiang Li, Xin Zhou
AIMS: Present study was performed to examine whether ADH was implicated in psychological stress asthma and to explore the underlying molecular mechanism. METHODS: We not only examined ADH levels in the cerebrospinal fluid (CSF) via radioimmunoassay, but also measured ADH receptor (ADHR) expression in airway-related vagal preganglionic neurons (AVPNs) through real-time PCR in all experimental mice. Western blotting was performed to evaluate the relationship between ADH and PKA/PKC in psychological stress asthma...
April 25, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28446753/histamine-and-histamine-h4-receptor-promotes-osteoclastogenesis-in-rheumatoid-arthritis
#3
Kyoung-Woon Kim, Bo-Mi Kim, Kyung-Ann Lee, Sang-Heon Lee, Gary S Firestein, Hae-Rim Kim
Histamine H4 receptor (H4R) has immune-modulatory and chemotaxic effects in various immune cells. This study aimed to determine the osteoclastogenic role of H4R in rheumatoid arthritis (RA). The concentration of histamine in synovial fluid (SF) and sera in patients with RA was measured using ELISA. After RA SF and peripheral blood (PB) CD14+ monocytes were treated with histamine, IL-17, IL-21 and IL-22, and a H4R antagonist (JNJ7777120), the gene expression H4R and RANKL was determined by real-time PCR. Osteoclastogenesis was assessed by counting TRAP-positive multinucleated cells in PB CD14+ monocytes cultured with histamine, Th17 cytokines and JNJ7777120...
April 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28444767/the-dual-orexin-receptor-antagonist-dora-22-lowers-histamine-levels-in-the-lateral-hypothalamus-and-prefrontal-cortex-without-lowering-hippocampal-acetylcholine
#4
Lihang Leon Yao, Andres Ramirez, Anthony J Roecker, Steven Fox, Jason Uslaner, Sean M Smith, Robert Hodgson, Paul J Coleman, John J Renger, Christopher J Winrow, Anthony L Gotter
Chronic insomnia is defined as a persistent difficulty with sleep initiation maintenance or non-restorative sleep. The therapeutic standard of care for this condition is treatment with gamma-aminobutyric acid (GABA)A receptor modulators, which promote sleep but are associated with a panoply of side effects, including cognitive and memory impairment. Dual orexin receptor antagonists (DORAs) have recently emerged as an alternative therapeutic approach that acts via a distinct and more selective wake-attenuating mechanism with the potential to be associated with milder side effects...
April 26, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28443506/catestain-a-master-regulator-of-cardiovascular-functions
#5
Sushil K Mahata, Malapaka Kiranmayi, Nitish R Mahapatra
Cardiovascular disease (CVD), the most common cause of death globally, accounts for ~30% of all deaths worldwide. Hypertension is a common contributor to morbidity and mortality from CVD. The plasma concentration of chromogranin A (CgA) is elevated in patients with CVD as well as patients with established human essential hypertension and heart failure (HF). In contrast, the plasma level of the CgA-derived peptide catestatin (CST) is diminished in human essential hypertension. Low conversion of CgA-to-CST has been associated with increased mortality in patients hospitalized with acute HF...
April 24, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28442805/proton-pump-inhibitors-are-associated-with-a-reduced-likelihood-for-sexually-transmitted-diseases-in-women-in-the-emergency-department
#6
Johnathan Michael Sheele, Nathan Morris, Donald Byars, Frank Counselman
BACKGROUND: Proton pump inhibitors (PPIs) have been shown in cell culture to kill Trichomonas vaginalis (TV) at lower half maximal inhibitory concentration values than metronidazole (Flagyl), the most common medication used to treat the infection. However, there have been no previous clinical investigations to determine if PPIs are associated with reduced risk for TV. MATERIALS AND METHODS: We examined the records of female patients who received testing in the emergency department for TV, Neisseria gonorrhoea (GC), and Chlamydia trachomatis (CT) between 2010 and 2014 at two academic medical centers to determine if PPI and histamine type 2 receptor antagonist (H2RA) drugs were associated with TV and GC/CT infections...
January 2017: Indian Journal of Sexually Transmitted Diseases
https://www.readbyqxmd.com/read/28441580/the-computer-aided-discovery-of-novel-family-of-the-5-ht6-serotonin-receptor-ligands-among-derivatives-of-4-benzyl-1-3-5-triazine
#7
Dorota Łażewska, Rafał Kurczab, Małgorzata Więcek, Katarzyna Kamińska, Grzegorz Satała, Magdalena Jastrzębska-Więsek, Anna Partyka, Andrzej J Bojarski, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
The work describes a discovery of new chemical family of potent ligands for the 5-HT6 serotonin receptors. During the search for new histamine H4 receptor antagonists among 1,3,5-triazine derivatives, compound 2 (4-benzyl-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) was found. Compound 2, weakly active for the H4 receptor but fitted in 3/4 of pharmacophore features of the 5-HT6R ligand, occurred to be a moderate 5-HT6R agent, useful as a lead structure for further modifications. A series of new derivatives (3-19) of the lead 2 was synthesized, evaluated in the radioligand binding assay (RBA) and explored in comprehensive molecular modelling, including both pharmacophore- and structure-based approaches with docking to the homology model of 5-HT6R...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28438982/the-histaminergic-system-is-involved-in-psychological-stress-induced-hyperthermia-in-rats
#8
Battuvshin Lkhagvasuren, Takakazu Oka
The histaminergic system modulates numerous physiological functions such as wakefulness, circadian rhythm, feeding, and thermoregulation. However, it is not yet known if this system is also involved in psychological stress-induced hyperthermia (PSH) and, if so, which histamine (H) receptor subtype mediates the effect. Therefore, we investigated the effects of pretreatments with intraperitoneal injections of mepyramine (an H1 receptor inverse agonist), cimetidine (an H2 receptor antagonist), and ciproxifan (an H3 receptor inverse agonist) on cage-exchange stress-induced hyperthermia (a model of PSH) by monitoring core body temperature (Tc) during both light (10:00 am-12:00 pm) and dark (10:00 pm-12:00 am) phases in conscious, freely moving rats...
April 2017: Physiological Reports
https://www.readbyqxmd.com/read/28436624/-mechanisms-of-histamine-ameliorating-memory-impairment-induced-by-pentylenetetrazole-kindling-epilepsy-in-rats
#9
Lisan Zhang, Guanfeng Chen, Jiefang Chen, Xudong He, Xingyue Hu
Objective: To investigate the effects of neuronal histamine on spatial memory acquisition impairment in rats with pentylenetetrazole-kindling epilepsy, and to explore its mechanisms. Methods: A subconvulsive dose of pentylenetetrazole (35 mg/kg) was intraperitoneally injected in rats every 48 h to induce chemical kindling until fully kindled. Morris water maze was used to measure the spatial memory acquisition of the rats one week after fully pentylenetetrazole-kindled, and the histamine contents in different brain areas were measured spectrofluorometrically...
January 25, 2017: Zhejiang da Xue Xue Bao. Yi Xue Ban, Journal of Zhejiang University. Medical Sciences
https://www.readbyqxmd.com/read/28430398/impact-of-acid-reducing-agents-on-the-pharmacokinetics-of-palbociclib-a-weak-base-with-ph-dependent-solubility-with-different-food-intake-conditions
#10
Wan Sun, Karen J Klamerus, Lisa M Yuhas, Sylvester Pawlak, Anna Plotka, Melissa O'Gorman, Leonid Kirkovsky, Maha Kosa, Diane Wang
Palbociclib free base capsule is a weak base drug with highly pH-dependent solubility. In vitro and in vivo studies evaluated the impact of acid-reducing agents on exposure of palbociclib and determined whether the impact, if any, can be mitigated by food. A drug-drug interaction study (study 1) was conducted first under fasted conditions and showed that coadministration of multiple doses of the proton-pump inhibitor rabeprazole substantially reduced palbociclib mean area under the concentration-time curve from time 0 to infinity and maximum observed plasma concentration by 62% and 80%, respectively...
April 21, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28419984/topical-histamine-stimulates-repigmentation-of-nonsegmental-vitiligo-by-a-receptor-dependent-mechanism
#11
Jun Liu, Yan Xu, Tzu-Kai Lin, Chengzhi Lv, Peter M Elias, Mao-Qiang Man
BACKGROUND: Though vitiligo is a common depigmentary disorder, it still represents a substantial therapeutic challenge. Therapeutic options are limited in part due to its uncertain etiology. OBJECTIVE: Because recent studies suggest that histamine stimulates melanogenesis in vitro, we determined here whether topical histamine stimulates repigmentation in patients with stable, nonsegmental vitiligo. METHODS: A total of 23 otherwise normal volunteers with vitiligo, including 14 males and 9 females aged 6-59 years (mean age 29...
April 19, 2017: Skin Pharmacology and Physiology
https://www.readbyqxmd.com/read/28417934/expression-of-adenosine-a2b-receptor-and-adenosine-deaminase-in-rabbit-gastric-mucosa-ecl-cells
#12
Rosa María Arin, Ana Isabel Vallejo, Yuri Rueda, Olatz Fresnedo, Begoña Ochoa
Adenosine is readily available to the glandular epithelium of the stomach. Formed continuously in intracellular and extracellular locations, it is notably produced from ATP released in enteric cotransmission. Adenosine analogs modulate chloride secretion in gastric glands and activate acid secretion in isolated parietal cells through A2B adenosine receptor (A2BR) binding. A functional link between surface A2BR and adenosine deaminase (ADA) was found in parietal cells, but whether this connection is a general feature of gastric mucosa cells is unknown...
April 12, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28412413/activation-of-muscarinic-receptors-prevents-tnf-%C3%AE-mediated-intestinal-epithelial-barrier-disruption-through-p38-mapk
#13
Junsuke Uwada, Takashi Yazawa, Md Tariqul Islam, Md Rafiqul Islam Khan, Susanne M Krug, Michael Fromm, Shin-Ichiro Karaki, Yuichi Suzuki, Atsukazu Kuwahara, Hatsumi Yoshiki, Kiyonao Sada, Ikunobu Muramatsu, Takanobu Taniguchi
Intestinal epithelial cells form a tight barrier to act as selective physical barriers, repelling hostile substances. Tumor necrosis factor-α (TNF-α) is a well characterized pro-inflammatory cytokine which can compromise intestinal barrier function and the suppression of TNF-α function is important for treatment of inflammatory bowel disease (IBD). In this study, we investigated the contribution of G-protein-coupled receptor (GPCR)-induced signalling pathways to the maintenance of epithelial barrier function...
April 12, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28401082/vaccinium-angustifolium-root-extract-suppresses-fc%C3%A9-ri-expression-in-human-basophilic-ku812f-cells
#14
Sun Yup Shim, Kyung Dong Lee, Mina Lee
Vaccinium angustifolium, commonly known as the lowbush blueberry, is a rich source of flavonoids, with which various human physiological activities have been associated. The present study focuses on the investigation of the effect of the methanolic extract of V. angustifolium root extract (VAE) on high affinity immunoglobulin E receptor (FcɛRI) α chain antibody (CRA-1)-induced allergic reaction in human basophilic KU812F cells. The total phenolic content of VAE was found to be 170±1.9 mg gallic acid equivalents/g...
March 2017: Preventive Nutrition and Food Science
https://www.readbyqxmd.com/read/28400155/histaminergic-gene-polymorphisms-associated-with-sedation-in-clozapine-treated-patients
#15
Anssi Solismaa, Olli Kampman, Leo-Pekka Lyytikäinen, Niko Seppälä, Merja Viikki, Nina Mononen, Terho Lehtimäki, Esa Leinonen
Sedation is a common adverse effect of clozapine treatment, which may be partly related to clozapine binding to histamine receptors in the central nervous system. The objective of this study was to investigate whether single nucleotide polymorphisms (SNPs) in the histaminergic system are associated with sedation in clozapine-treated patients. The study population comprised 237 clozapine-treated, Finnish, Caucasian patients that were diagnosed with schizophrenia and 176 were genotyped using Illumina HumanCoreExome-12 BeadChip...
April 8, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28398338/the-histamine-h3-receptor-antagonist-thioperamide-rescues-circadian-rhythm-and-memory-function-in-experimental-parkinsonism
#16
D Masini, C Lopes-Aguiar, A Bonito-Oliva, D Papadia, R Andersson, A Fisahn, G Fisone
Parkinson's disease (PD) is a common neurodegenerative disorder, characterized by motor impairment and a wide range of non-motor symptoms, including sleep disorders and cognitive and affective deficits. In this study, we used a mouse model of PD based on 6-hydroxydopamine (6-OHDA) to examine the effect of thioperamide, a histamine H3 receptor antagonist, on circadian activity, recognition memory and anxiety. A partial, bilateral 6-OHDA lesion of the striatum reduces motor activity during the active phase of the 24 h cycle...
April 11, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28392699/comparison-of-prophylactic-effect-of-ugib-and-effects-on-platelet-function-between-ppis-and-h2ras-combined-with-dapt-systematic-review-and-meta-analysis
#17
Zhan-Miao Yi, Ting-Ting Qiu, Yuan Zhang, Zhi-Yan Liu, Suo-Di Zhai
OBJECTIVE: We compared prophylactic effects of proton pump inhibitors (PPIs) and histamine-2 receptor antagonists (H2RAs) on upper gastrointestinal bleeding (UGIB) associated with dual antiplatelet therapy (DAPT) and explored this influence on platelet function. METHODS: Randomized controlled trials and cohort studies comparing PPIs with H2RAs in adults receiving DAPT were collected from PubMed, EMBASE and Cochrane databases. Dichotomous data were pooled to obtain risk ratios (RRs) for UGIB, major adverse cardiovascular events (MACEs), poor responders to clopidogrel and rehospitalization, and continuous data were pooled to obtain mean differences (MDs) for P2Y12 reaction units (PRUs), with 95% confidence intervals (CIs)...
2017: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/28391980/histamine-h1-and-h4-receptor-expression-on-the-ocular-surface-of%C3%A2-patients-with-chronic-allergic-conjunctival-diseases
#18
Noriko Inada, Jun Shoji, Yukiko Shiraki, Hiroshi Aso, Satoru Yamagami
BACKGROUND: This study investigated the histamine H1 and H4 receptors mRNA (H1R and H4R, respectively) expression on the ocular surface of patients with chronic forms of allergic conjunctival diseases to determine whether they can serve as biomarkers for allergic inflammation in the conjunctiva. METHODS: We examined 19 patients with vernal or atopic keratoconjunctivitis (AKC/VKC group) and 15 healthy volunteers (control group). The AKC/VKC group was divided into active and stable stage subgroups...
April 5, 2017: Allergology International: Official Journal of the Japanese Society of Allergology
https://www.readbyqxmd.com/read/28391591/syrian-hamster-neuroplasticity-mechanisms-fail-as-temperature-declines-to-15%C3%A2-%C3%A2-c-but-histaminergic-neuromodulation-persists
#19
Jock S Hamilton, Sat M Chau, Kevin J Malins, Giancarlo G Ibanez, John M Horowitz, Barbara A Horwitz
Previous research suggests that hippocampal neurons in mammalian hibernators shift their major function from memory formation at euthermic brain temperatures (T b = ~37 °C) to modulation of hibernation bout duration as T b decreases. This role of hippocampal neurons during torpor is based in part on in vivo studies showing that histamine (HA) infused into ground squirrel hippocampi lengthened torpor bouts by ~50%. However, it was unclear if HA acted directly on hippocampal neurons or on downstream brain regions via HA spillover into lateral ventricles...
April 9, 2017: Journal of Comparative Physiology. B, Biochemical, Systemic, and Environmental Physiology
https://www.readbyqxmd.com/read/28391162/quantitative-electrophysiological-monitoring-of-anti-histamine-drug-effects-on-live-cells-via-reusable-sensor-platforms
#20
Viet Anh Pham Ba, Dong-Guk Cho, Daesan Kim, Haneul Yoo, Van-Thao Ta, Seunghun Hong
We demonstrated the quantitative electrophysiological monitoring of histamine and anti-histamine drug effects on live cells via reusable sensor platforms based on carbon nanotube transistors. This method enabled us to monitor the real-time electrophysiological responses of a single HeLa cell to histamine with different concentrations. The measured electrophysiological responses were attributed to the activity of histamine type 1 receptors on a HeLa cell membrane by histamine. Furthermore, the effects of anti-histamine drugs such as cetirizine or chlorphenamine on the electrophysiological activities of HeLa cells were also evaluated quantitatively...
March 31, 2017: Biosensors & Bioelectronics
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