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Histamine H1 receptors

Wakchaure Padmaja D, Ravichandiran Velayutham, Kuldeep K Roy
We report herein detailed structural insights into the ligand recognition modes guiding bromodomain selectivity, enrichment analysis and docking-based database screening for the identification of the FDA-approved drugs that have potential to be the human BRD4 inhibitors. Analysis of multiple X-ray structures prevailed that the lysine-recognition sites are highly conserved, and apparently, the dynamic ZA loop guides the specific ligand-recognition. The protein-ligand interaction profiling revealed that both BRD2 and BRD4 shared hydrophobic interaction of bound ligands with PRO-98/PRO-82, PHE-99/PHE-83, LEU-108/LEU-92, and direct H-bonding with ASN-156/ASN-140 (BRD2/BRD4), while on the other hand the water-mediated H-bonding of bound ligands with PRO-82, GLN-85, PRO-86, VAL-87, ASP-88, LEU-92, TYR-97 and MET-132, and aromatic π - π stacking with TRP-81 prevailed as unique interaction in BRD4, and were not observed in BRD2...
August 6, 2018: Journal of Biomolecular Structure & Dynamics
K N Strygin
The article analyzes the anatomy, morphological and neurochemical connections and functions of the brain histaminergic system, one of the leading systems in the mechanism maintaining wakefulness. The possibilities of histaminergic system modulating for the treatment of various sleep/wake cycle disorders are discussed. The data of clinical trials on the influence of the histamine H1 receptor antagonist doxylamine on sleep in healthy volunteers and patients with insomnia are considered. The evidence-based efficacy of the drug in sleep disorders is discussed...
2018: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Yuya Tabakawa, Takuya Ohta, Soichiro Yoshikawa, Elisabeth J Robinson, Kayoko Yamaji, Kenji Ishiwata, Yohei Kawano, Kensuke Miyake, Yoshinori Yamanishi, Hiroshi Ohtsu, Takahiro Adachi, Naohiro Watanabe, Hirotaka Kanuka, Hajime Karasuyama
Ticks are blood-feeding arthropods that can transmit pathogens to humans and animals, leading to serious infectious diseases such as Lyme disease. After single or multiple tick infestation, some animal species develop resistance to tick feeding, leading to reduced risk of pathogen transmission. In mice infested with larval Haemaphysalis longicornis ticks, both mast cells and basophils reportedly play key roles in the manifestation of acquired tick resistance (ATR), but it remains ill-defined how they contribute to it...
2018: Frontiers in Immunology
Susanne Mommert, Derya Aslan, Lisanne Ratz, Holger Stark, Ralf Gutzmer, Thomas Werfel
The anaphylatoxin C3a triggers inflammation by binding to its specific G-protein-coupled C3a receptor (C3aR). Since the number of C3aR, which is expressed on the cell surface, affects the response to C3a, we investigated the expression levels of C3aR on human M2 macrophages in allergic situations where high levels of the Th2 cytokine IL-4 and histamine are present in a local microenvironment. The histamine H1 receptor (H1R), H2R and the H4R mRNA expressions were induced or up-regulated during the differentiation process of M2 macrophages...
July 20, 2018: Journal of Innate Immunity
Michael J Haas, Marilu Jurado-Flores, Ramadan Hammoud, Gabriela Plazarte, Luisa Onstead-Haas, Norman C W Wong, Arshag D Mooradian
AIMS: Earlier it had been found by us that apolipoprotein A-I (apo A-I) is suppressed by histamine in HepG2 cells. Histamine has been shown to regulate NF-κB activity, though not in hepatocytes. Therefore we examined the role of the histamine receptors and NF-κB in histamine-mediated apo A-I gene expression in HepG2 liver cells. MAIN METHODS: The effect of histamine on histamine H1 receptor expression, and NF-κB p65 and p50 subunits was examined by Western blot...
July 14, 2018: Life Sciences
Emad Khalilzadeh, Farzin Azarpey, Reza Hazrati, Gholamreza Vafaei Saiah
It seems that histamine release in the site of neuronal injury could contribute to the neuropathic pain mechanism. In the present study, we investigated the anti-allodynic effects of chronic administration of different classes of histamine H1 and H2 receptor antagonists on neuropathic nociceptive behavior following tibial nerve transection (TNT) in rats. Peripheral neuropathy was induced by TNT surgery. We performed acetone tests (AT) to record cold allodynia, Von Frey tests (VFT) to measure mechanical allodynia, double plate test (DPT) to evaluate thermal place preference/avoidance and open field test (OFT) for evaluation of animal activity...
July 27, 2018: European Journal of Pharmacology
Yuichi Hattori
Sepsis is the leading cause of death in critically ill patients, and its incidence continues to rise. Sepsis is now defined as life-threatening organ dysfunction due to a dysregulated host response to infection. Histamine assumes a critical role as a major mediator of many pathologic disorders with inflammation and immune reactions. However, direct evidence has not been provided showing the involvement of histamine in the development of multiple organ dysfunction or failure in sepsis. We have found that sepsis-induced major end-organ (lung, liver, and kidney) injury is attenuated in histidine decarboxylase (HDC) gene knockout mice...
2018: Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
Dahlia R Weiss, Joel Karpiak, Xi-Ping Huang, Maria F Sassano, Jiankun Lyu, Bryan L Roth, Brian K Shoichet
To investigate large library docking's ability to find molecules with joint activity against on-targets and selectivity versus antitargets, the dopamine D2 and serotonin 5-HT2A receptors were targeted, seeking selectivity against the histamine H1 receptor. In a second campaign, κ-opioid receptor ligands were sought with selectivity versus the μ-opioid receptor. While hit rates ranged from 40% to 63% against the on-targets, they were just as good against the antitargets, even though the molecules were selected for their putative lack of binding to the off-targets...
July 24, 2018: Journal of Medicinal Chemistry
Adam Schafer, Han Cheng, Rui Xiong, Veronica Soloveva, Cary Retterer, Feiyan Mo, Sina Bavari, Gregory Thatcher, Lijun Rong
Ebola and Marburg are filoviruses and biosafety level 4 pathogens responsible for causing severe hemorrhagic fevers in humans with mortality rates up to 90%. The most recent outbreak in West Africa resulted in approximately 11,310 deaths in 28,616 reported cases. Currently there are no FDA-approved vaccines or therapeutics to treat infections of these deadly viruses. Recently we screened an FDA-approved drug library and identified numerous G protein-coupled receptor (GPCR) antagonists including antihistamines possessing anti-filovirus properties...
July 4, 2018: Antiviral Research
Richard D Rainbow, Sean Brennan, Robert Jackson, Alison J Beech, Amal Bengreed, Helen V Waldschmidt, John Jg Tesmer, Ra John Challiss, Jonathon M Willets
Vasoconstrictor-driven G protein-coupled receptor (GPCR)/phospholipase C (PLC) signalling increases intracellular Ca2+ concentration to mediate arterial contraction. To counteract vasoconstrictor-induced contraction, GPCR/PLC signalling can be desensitized by G protein-coupled receptor kinases (GRKs), with GRK2 playing a predominant role in isolated arterial smooth muscle cells. Here, we utilize an array of GRK2 inhibitors to assess their effects on the desensitization of UTP and angiotensin II-mediated arterial contractions...
July 6, 2018: Molecular Pharmacology
Thi Thu Ha Nguyen, Anne Roussin, Vanessa Rousseau, Jean-Louis Montastruc, François Montastruc
BACKGROUND: The association between antidepressant exposure and type 2 diabetes mellitus is still debated. Moreover, the pharmacological mechanisms remain unknown. OBJECTIVE: The objective of this study was to investigate this putative relationship with the role of antidepressant pharmacological targets using the 'pharmacoepidemiological-pharmacodynamic' method. METHODS: First, we performed case/non-case analyses in VigiBase® (the World Health Organization international database of suspected adverse drug reactions) to examine a signal of increased type 2 diabetes reporting (expressed as the reporting odds ratio and its 95% confidence interval) for antidepressants in general; examine and rank type 2 diabetes signals between the different pharmacological classes of antidepressants and the different antidepressants (58 in total)...
June 28, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
Spyridon Siafis, Georgios Papazisis
AIMS: Recent data suggest that antidepressants are associated with incident diabetes but the possible pharmacological mechanism is still questioned. The aim of the present study was to evaluate antidepressant's risk for reporting diabetes using disproportionality analysis of the FDA adverse events spontaneous reporting system (FAERS) database and to investigate possible receptor/transporter mechanisms involved. METHODS: Data from 2004 to 2017 were analysed using OpenVigil2 and adjusted reporting odds ratio (aROR) for reporting diabetes was calculated for 22 antidepressants...
June 28, 2018: British Journal of Clinical Pharmacology
Cong-Yu Jin, Hong Wei, Kaj Karlstedt, Antti Pertovaara
Aims Among brain structures receiving efferent projections from the histaminergic tuberomammillary nucleus is the pontine locus coeruleus (LC), a structure involved in descending noradrenergic control of pain. Here we studied whether histamine in the LC is involved in descending regulation of neuropathic hypersensitivity. Methods Peripheral neuropathy was induced by unilateral spinal nerve ligation (SNL) in the rat with a chronic intracerebral and intrathecal catheter for drug administrations. Mechanical hypersensitivity in the injured limb was assessed by monofilaments...
December 29, 2017: Scandinavian Journal of Pain
M Saarnilehto, M Pekkanen-Mattila, K Aalto-Setälä, O Silvennoinen, A Koivisto
Aims Aim of the study was to characterize functional ion channel and GPCR responses by using selective pharmacological tools and intracellular calcium imaging from human inducible pluripotent stem cell-derived sensory neurons. Methods Sensory neurons were generated from human keratinocytes that were reprogrammed to inducible pluripotent stem cells by using standard Yamanaka factors. Inducible pluripotent stem cells were differentiated into sensory neurons by using 2 differentiation protocols (small molecule and PA6 co-culture)...
December 29, 2017: Scandinavian Journal of Pain
Loránd Barthó, Zsolt Sándor, Timea Bencsik
Aqueous extract of the spines of the brown bullhead catfish (Ameiurus nebulosus Lesueur, 1819) caused contraction of the guinea-pig small intestine in vitro, a widely-used preparation in pharmacology. The action is dependent on extracellular Ca2+ , and probably takes place on the smooth muscle cells. Mouse gastrointestinal preparations were also contracted by the extract. Stings by the spines of this fish species causes a painful sensation in man. We tested the effect of an extract of spines in isolated organ experiments on innervated smooth muscle preparations...
June 2018: Acta Biologica Hungarica
Fei-Hong Liang, Xun-Rui Hou, Li-Hong Li, Xin Liang, Yu-Wei Lu, Hong Yang, Yuan Zhang
OBJECTIVE: To observe the effect of acupoint injection at "Yingxiang"(LI 20) and "Yintang"(GV 29) on nasal allergic reactions and the expression of histamine receptor H 1 and H 4 in nasal mucosa of allergic rhinitis (AR) rats, so as to reveal its mechanism underlying improvement of AR. METHODS: SD rats were randomized into normal, model, non-acupoint injection and acupoint injection groups ( n =8 in each). The AR model was established by intraperitoneal (i...
April 25, 2018: Zhen Ci Yan Jiu, Acupuncture Research
Tomoya Hirano, Takashi Fujiwara, Hideaki Niwa, Michitake Hirano, Kasumi Ohira, Yusuke Okazaki, Shin Sato, Takashi Umehara, Yuki Maemoto, Akihiro Ito, Minoru Yoshida, Hiroyuki Kagechika
The histone methyltransferase SET7/9 methylates not only histone but also non-histone proteins as substrates, and therefore, SET7/9 inhibitors are considered candidates for the treatment of diseases. Previously, our group identified cyproheptadine, used clinically as a serotonin receptor antagonist and histamine receptor (H1) antagonist, as a novel scaffold of the SET7/9 inhibitor. In this work, we focused on dibenzosuberene as a substructure of cyproheptadine and synthesized derivatives with various functional groups...
June 7, 2018: ChemMedChem
Ivan Shirinsky, Valery Shirinsky
BACKGROUND: There is growing evidence that mast cells (MCs) play a role in knee osteoarthritis (OA). H1 -antihistamines block H1 -receptors of histamine, which is an important mediator of MCs. There is a lack of data on whether H1 -antihistamines can influence OA. We hypothesized that the use of H1 -antihistamines may be linked to the reduced prevalence of knee OA. METHODS: Baseline data from the Osteoarthritis Initiative cohort were analysed cross-sectionally. Unadjusted and adjusted logistic regression models were performed to compare the prevalence of knee OA in H1 -antihistamine users and non-users...
June 7, 2018: Arthritis Research & Therapy
Angel Jemima Ebenezer, Kavya Prasad, Sanjana Rajan, Elden Berla Thangam
CONTEXT: Mast cell (MC) activation through H4R releases various inflammatory mediators which are associated with allergic asthma. OBJECTIVES: To investigate the siRNA-mediated gene silencing effect of H4R on human mast cells (HMCs) functions and the activation of stress-activated protein kinases (SAPK)/jun amino-terminal kinases (JNK) signaling pathways for the release of ineterleukin-1β (IL-1β) in HMCs. MATERIALS AND METHODS: H4R expression was analyzed by RT-PCR and western blotting in human mast cell line-1 (HMC-1) cells and H4RsiRNA transfected cells...
June 2018: Journal of Receptor and Signal Transduction Research
Anikó Kárpáti, Takeo Yoshikawa, Tadaho Nakamura, Tomomitsu Iida, Takuro Matsuzawa, Haruna Kitano, Ryuichi Harada, Kazuhiko Yanai
Astrocytes play key roles in regulating brain homeostasis and neuronal activity. This is, in part, accomplished by the ability of neurotransmitters in the synaptic cleft to bind astrocyte membrane receptors, activating signalling cascades that regulate concentration of intracellular Ca2+ ([Ca2+ ]i ) and gliotransmitter release, including ATP and glutamate. Gliotransmitters contribute to dendrite formation and synaptic plasticity, and in some cases, exacerbate neurodegeneration. The neurotransmitter histamine participates in several physiological processes, such as the sleep-wake cycle and learning and memory...
May 16, 2018: Journal of Pharmacological Sciences
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