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Histamine H1 receptors

Alessandra Misto, Gustavo Provensi, Valentina Vozella, Maria Beatrice Passani, Daniele Piomelli
The conversion of lipolysis-derived fatty acids into ketone bodies (ketogenesis) is a crucial metabolic adaptation to prolonged periods of food scarcity. The process occurs primarily in liver mitochondria and is initiated by fatty-acid-mediated stimulation of the ligand-operated transcription factor, peroxisome proliferator-activated receptor-α (PPAR-α). Here, we present evidence that mast cells contribute to the control of fasting-induced ketogenesis via a paracrine mechanism that involves secretion of histamine into the hepatic portal circulation, stimulation of liver H1 receptors, and local biosynthesis of the high-affinity PPAR-α agonist, oleoylethanolamide (OEA)...
October 4, 2018: Cell Metabolism
Arvind Kumar, Harpreet Singh, Amrita Mishra, Arun K Mishra
OBJECTIVE: Aripiprazole,a synthetic compound, obtained by chemical modification of the structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole. DEVELOPMENT: Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U.S. Food and Drug Administration (USFDA) in the end months of 2002 to with an aim to treat patients with schizophrenia...
October 8, 2018: Current Drug Discovery Technologies
Tatsuya Fujii, Yoshiaki Kitamura, Hiroyuki Mizuguchi, Kentaro Okamoto, Nanae Sanada, Takuya Yamada, Manabu Sugiyama, Shotaro Michinaga, Mika Kitayama, Hiroyuki Fukui, Noriaki Takeda
Narrowband-ultraviolet B (NB-UVB) phototherapy is used for the treatment of atopic dermatitis. Previously, we reported that irradiation with 200 mJ/cm2 of 310 nm NB-UVB suppressed phorbol-12-myristate-13-acetate (PMA)-induced up-regulation of histamine H1 receptor (H1R) gene expression without induction of apoptosis in HeLa cells. However, the effect of NB-UVB irradiation on nasal symptoms is still unclear. Here, we show that low dose irradiation with 310 nm NB-UVB alleviates nasal symptoms in toluene 2,4-diisocyanate (TDI)-sensitized allergy model rats...
September 10, 2018: Journal of Pharmacological Sciences
Islam Rezwanul, Mizuguchi Hiroyuki, Shaha Aurpita, Nishida Kohei, Yabumoto Masami, Ikeda Hisashi, Fujino Hiromichi, Kitamura Yoshiaki, Fukui Hiroyuki, Takeda Noriaki
As expression level of allergic disease-sensitive genes are correlated with allergic symptom severity, suppression of these gene expressions could be good therapeutics. We have demonstrated that PKCδ signaling and NFAT signaling, involve in histamine H1 receptor (H1R) and IL-9 gene expressions, respectively, are responsible for the pathogenesis of allergic rhinitis. We explore anti-allergic compounds that suppress these signaling pathways and found that wild grape (WG) contains such compounds. Here, we investigated the effect of WG hot water extract (WGE) on the signaling pathways for PKCδ-mediated H1R and NFAT-mediated IL-9 gene expressions...
2018: Journal of Medical Investigation: JMI
Amin Kanani, Stephen D Betschel, Richard Warrington
Urticaria (hives) is a common disorder that often presents with angioedema (swelling that occurs beneath the skin). It is generally classified as acute or chronic. Second-generation, non-sedating, non-impairing histamine type 1 (H1)-receptor antihistamines represent the mainstay of therapy for both acute and chronic urticaria. Angioedema can occur in the absence of urticaria and can be broadly divided into histamine-mediated and non-histamine-mediated angioedema. Histamine-mediated angioedema can be allergic, pseudoallergic or idiopathic...
2018: Allergy, Asthma, and Clinical Immunology
Gareth J Sanger, Paul L R Andrews
The origins of the major classes of current anti-emetics are examined. Serendipity is a recurrent theme in discovery of their anti-emetic properties and repurposing from one indication to another is a continuing trend. Notably, the discoveries have occurred against a background of company mergers and changing anti-emetic requirements. Major drug classes include: (i) Muscarinic receptor antagonists -originated from historical accounts of plant extracts containing atropine and hyoscine with development stimulated by the need to prevent sea-sickness among soldiers during beach landings; (ii) Histamine receptor antagonists -searching for replacements for the anti-malaria drug quinine, in short supply because of wartime shipping blockade, facilitated the discovery of histamine (H1 ) antagonists (e...
2018: Frontiers in Pharmacology
Evelyn M Guilherme, Bruna Silva-Marques, Carlos Eduardo M Fernandes, Thiago L Russo, Rosana Mattioli, Anna C Gianlorenço
The neural histaminergic system innervates the cerebellum, with a high density of fibers in the vermis and flocculus. The cerebellum participates in motor functions, but the role of the histaminergic system in this function is unclear. In the present study, we investigated the effects of intracerebellar histamine injections and H1, H2 and H3 receptor antagonist injections (chlorpheniramine, ranitidine, and thioperamide, respectively) and H4 receptor agonist (VUF-8430) on locomotor and exploratory behaviors in mice...
September 12, 2018: Neuroscience Letters
Han Zhang, Masaru Ihara, Seiya Hanamoto, Norihide Nakada, Monika D Jürgens, Andrew C Johnson, Hiroaki Tanaka
While pharmaceuticals are now routinely detected in aquatic environments, we know little of the biological activity their presence might provoke. It is estimated that nearly 40% of all marketed pharmaceuticals are G protein-coupled receptors (GPCRs) acting pharmaceuticals. Here, we applied an in-vitro assay, called the TGFα shedding assay, to measure the biological activities of GPCRs-acting pharmaceuticals present in effluents from municipal wastewater treatment plants in the United Kingdom (UK) and Japan from 2014 to 2016...
September 28, 2018: Environmental Science & Technology
T E Schwasinger-Schmidt, M Macaluso
This chapter addresses the following FDA-approved medications for the treatment of major depressive disorder available for use in the United States including bupropion, mirtazapine, trazodone, vortioxetine, and vilazodone. These medications do not belong to one of the previously featured classes of antidepressants discussed in the preceding chapters. Each medication featured in this chapter has a unique structure and properties that target diverse receptors in the central nervous system. These diverse targets are distinct from other classes of medications used to treat major depressive disorder...
September 8, 2018: Handbook of Experimental Pharmacology
Aurpita Shaha, Hiroyuki Mizuguchi, Yoshiaki Kitamura, Hiromichi Fujino, Masami Yabumoto, Noriaki Takeda, Hiroyuki Fukui
The significant correlation between nasal symptom scores and level of histamine H1 receptor (H1R) mRNA in nasal mucosa was observed in patients with pollinosis, suggesting that H1R gene is an allergic disease sensitive gene. We demonstrated that H1R and interleukin (IL)-9 gene are the allergic rhinitis (AR)-sensitive genes and protein kinase Cδ (PKCδ) signaling and nuclear factor of activated T-cells (NFAT) signaling are involved in their expressions, respectively. Honey bee products have been used to treat allergic diseases...
2018: Biological & Pharmaceutical Bulletin
Jin-Tao Chu
H1-antihistamine has been shown to be effective in treating patients with allergic rhinitis (AR), but its mechanism is still uncertain. We investigated effects of histamine H1 receptor (HRH1) gene polymorphisms on the efficacy of oral H1-antihistamine in perennial patients with AR caused by mites in the Chinese Han population for the first time. A total of 224 Han Chinese patients with AR and 165 Han Chinese healthy volunteers were selected. Genotype and allele frequency distribution of -17C/T in HRH1 gene in patients with AR, serum levels of eosinophil cationic protein (ECP), total immunoglobulin E (IgE), and specific IgE were detected...
August 30, 2018: Journal of Cellular Biochemistry
Linda J Kay, S Kim Suvarna, Peter T Peachell
The diverse effects of histamine are mediated by discrete histamine receptors. The principal repository of histamine in the body is the mast cell. However, the effects of histamine on mast cells, especially those of human origin, have not been fully elucidated. In this study, the expression of histamine receptors in human lung mast cells was evaluated. Moreover, the effects of histamine receptor engagement on both mediator release and chemotaxis were investigated. Mast cells were isolated and purified from human lung tissue...
August 24, 2018: European Journal of Pharmacology
Miao-Jin Ji, Xiao-Yang Zhang, Xiao-Chun Peng, Yang-Xun Zhang, Zi Chen, Lei Yu, Jian-Jun Wang, Jing-Ning Zhu
The ventral pallidum (VP) is a crucial component of the limbic loop of the basal ganglia and participates in the regulation of reward, motivation, and emotion. Although the VP receives afferent inputs from the central histaminergic system, little is known about the effect of histamine on the VP and the underlying receptor mechanism. Here, we showed that histamine, a hypothalamic-derived neuromodulator, directly depolarized and excited the GABAergic VP neurons which comprise a major cell type in the VP and are responsible for encoding cues of incentive salience and reward hedonics...
August 25, 2018: Neuroscience Bulletin
Nasir Niaz, Gokcen Guvenc, Burcin Altinbas, Mehmed Berk Toker, Begum Aydin, Duygu Udum-Kucuksen, Selim Alcay, Elif Gokce, Burcu Ustuner, Murat Yalcin
Brain histamine holds a key position in the regulation of behavioral states, biological rhythms, body weight, energy metabolism, thermoregulation, fluid balance, stress and reproduction in female animals. However, it is not clear whether central histamine exerts any effect on hypothalamic-pituitary-testicular in male rats and if so, the involvement of type of central histamine receptors. The current study was designed to determine the effect of centrally administrated histamine on plasma gonadotropin hormone-releasing hormone (GnRH), luteinizing hormone (LH), follicle stimulating hormone (FSH) and testosterone level, and sperm parameters, and to show the mediation of the central histaminergic H1, H2 and H3/H4 receptors on histamine-evoked hormonal and sperm parameters' effects...
August 18, 2018: Brain Research
Yuyang Zhou, Chengshan Gao, Hongshan Wang, Lei Liu, Zhenfeng Huang, Xianen Fa
Oxidized LDL (ox-LDL) is one of the major risk factors of atherosclerosis. Endothelial dysfunction caused by ox-LDL is an early event in the pathogenesis of cardiovascular diseases. Preclinical studies have been performed to explore efficient means of preventing endothelial abnormalities. In this study, we revealed that loratadine, a histamine H1 type receptor specific antagonist, possesses a protective effect by relieving ox-LDL-induced endothelial inflammation. Treatment of endothelial cells with ox-LDL induces expression of the H1 receptor...
October 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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...
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...
September 1, 2018: Life Sciences
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