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Histamine H1 receptors

M Keerthana, M Vidyavathi
Loratadine is a selective inverse agonist of peripheral histamine H1-receptors. Microbial biotransformation gained a lot of attention for its ability to convert molecules to valuable medicinally active substances. The main objective of the present research was to investigate the ability of different fungi to biotransform the drug loratadine to its active metabolite desloratadine, because desloratadine is four times more potent, possess longer duration of action than loratadine and is effective at low doses...
December 2018: Journal of Biosciences
Raghunath Singh, Yashika Bansal, Bikash Medhi, Anurag Kuhad
Atypical antipsychotics (AAPs) are the drug of choice in the management of mental illnesses by virtue of their advantage over typical antipsychotics i.e. least tendency of producing extrapyramidal motor symptoms (EPS) or pseudoparkinsonism. Despite the clinical efficacy, AAPs produces troublesome adverse effects, particularly hyperphagia, hyperglycemia, dyslipidemia weight gain, diabetes mellitus, insulin resistance and QT prolongation which further develops metabolic and cardiac complications with subsequent reduction in life expectancy, poor patient compliance, and sudden death...
December 7, 2018: European Journal of Pharmacology
Christian A Söldner, Anselm H C Horn, Heinrich Sticht
Binding of histamine to the G-protein coupled histamine H1 receptor plays an important role in the context of allergic reactions; however, no crystal structure of the resulting complex is available yet. To deduce the histamine binding site, we performed unbiased molecular dynamics (MD) simulations on a microsecond time scale, which allowed to monitor one binding event, in which particularly the residues of the extracellular loop 2 were involved in the initial recognition process. The final histamine binding pose in the orthosteric pocket is characterized by interactions with Asp1073...
November 29, 2018: Journal of Molecular Modeling
Wen-Jun Su, Ting Zhang, Chun-Lei Jiang, Wei Wang
Backgrounds: Abundant reports indicate that neuroinflammatory signaling contributes to behavioral complications associated with depression and may be related to treatment response. The glial cells, especially microglia and astrocytes in brain regions of hippocampus and medial prefrontal cortex (mPFC), are major components of CNS innate immunity. Moreover, purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) was recently reckoned as a pivotal regulator in central immune system. Besides, it was pointed out that clemastine, a first-generation histamine receptor H1 (HRH1) antagonist with considerable safety profile and pharmacological effect, may suppress immune activation through modulating P2X7R...
2018: Frontiers in Cellular Neuroscience
Olga Y Gasheva, Irina Tsoy Nizamutdinova, Laura Hargrove, Cassidy Gobbell, Maria Troyanova-Wood, Sally F Alpini, Sarit Pal, Christina Du, Angie R Hitt, Vlad V Yakovlev, M Karen Newell-Rogers, David Carl Zawieja, Cynthia J Meininger, Gianfranco D Alpini, Heather Francis, Anatoliy A Gashev
This study aimed to establish mechanistic links between the prolonged intake of desloratadine, a common H1 receptor blocker (i.e. antihistamine), and development of obesity and metabolic syndrome. Male Sprague-Dawley rats were treated orally for 16 weeks with desloratadine. We analyzed the dynamics of body weight gain; tissue fat accumulation/density; contractility of isolated mesenteric lymphatic vessels; levels of blood lipids, glucose and insulin; together with parameters of liver function. Prolonged intake of desloratadine induced development of an obesity-like phenotype and signs of metabolic syndrome...
November 26, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
Tetsuya Tachibana, Wataru Ueoka, Md Sakirul Islam Khan, Ryosuke Makino, Mark A Cline
Infectious conditions are associated with reduced food passage through the digestive tract in both mammals and chicks; however, the precise mechanism mediating this response in chicks remains unclear. The purpose of the present study was to determine if mast cells, a blood cell type which plays an important role in the immune system, might affect food passage through the digestive tract in chicks. Specifically, we performed intraperitoneal (IP) injections of compound 48/80, an inducer of mast cell degranulation, and measured crop emptying...
October 23, 2018: Domestic Animal Endocrinology
Zhongcheng Shi, Robert Steven Fultz, Melinda A Engevik, Chunxu Gao, Anne Hall, Angela Major, Yuko Mori-Akiyama, James Versalovic
Inflammatory bowel disease (IBD) is a well-known risk factor for the development of colorectal cancer. Prior studies have demonstrated that microbial histamine can ameliorate intestinal inflammation in mice. We tested the hypothesis whether microbe-derived luminal histamine suppresses inflammation-associated colon cancer in Apcmin/+ mice. Mice were colonized with the human-derived Lactobacillus reuteri. Chronic inflammation was induced by repeated cycles of low-dose dextran sulfate sodium (DSS). Mice that were given histamine-producing L...
November 21, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
Katrin Schaper-Gerhardt, Kristine Rossbach, Eirini Nikolouli, Thomas Werfel, Ralf Gutzmer, Susanne Mommert
Atopic dermatitis (AD) and psoriasis are common skin diseases with a high negative impact on patients´ quality of life. Both diseases are mediated by a pro-inflammatory infiltrate consisting of various cell types like T cells, antigen presenting cells and granulocytes and display disturbed keratinocyte differentiation. Given the fact that histamine levels are also highly elevated in inflamed skin, it is likely that histamine plays a relevant role in disease pathology. However, antagonists blocking histamine H1 receptor (HRH1) and HRH2 are largely ineffective in reducing chronic symptoms in AD and psoriasis...
November 21, 2018: British Journal of Pharmacology
Madhulika A Gupta, Branka Vujcic, Daiana R Pur, Aditya K Gupta
Antipsychotic drugs can be beneficial in dermatology because of their both central nervous system and peripheral effects. All antipsychotic drugs have a central postsynaptic dopamine D2 receptor blocking effect, which underlies their antipsychotic action. The antipsychotic drugs have varying degrees of histamine H1-receptor, cholinergic muscarinic receptor, and α1-adrenergic receptor blocking effects, which can affect cutaneous perception and the autonomic reactivity of the skin and can be potentially beneficial in the management of certain histamine or sympathetically mediated dermatologic manifestations (eg, urticaria, pruritus, hyperhidrosis)...
November 2018: Clinics in Dermatology
Xudong Cao, Yifang Zhang, Yin Chen, Yinli Qiu, Minquan Yu, Xiangqing Xu, Xin Liu, Bi-Feng Liu, Liangren Zhang, Guisen Zhang
Herein, a novel series of multireceptor ligands was developed as polypharmacological antipsychotic agents using the designed multiple ligand approach between dopamine receptors and serotonin receptors. Among them, compound 47 possessed unique pharmacological features, exhibiting high affinities for D2 , D3 , 5-HT1A , 5-HT2A , and 5-HT6 receptors and low efficacy at the off-target receptors (5-HT2C , histamine H1 , and adrenergic α1 receptor). Compound 47 showed dose-dependent inhibition of apomorphine- and MK-801-induced motor behavior, and the conditioned avoidance response with low cataleptic effect...
November 9, 2018: Journal of Medicinal Chemistry
Ekaterini Tiligada, Madeleine Ennis
Histamine has been one of the most studied substances in medicine, playing a major role in diverse (patho) physiological processes. It elicits its multifaceted modulatory functions by activating four types of G-protein-coupled receptors, designated as H1-4 . Despite the heterogeneity and the complexity of histamine receptor pharmacology, many discoveries over the past 100 years resulted in the development of H1 antihistamines and H2 -targeting 'blockbuster' therapeutics for the management of allergies and gastrointestinal disorders, respectively...
October 19, 2018: British Journal of Pharmacology
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
Rezwanul Islam, Hiroyuki Mizuguchi, Aurpita Shaha, Kohei Nishida, Masami Yabumoto, Hisashi Ikeda, Hiromichi Fujino, Yoshiaki Kitamura, Hiroyuki Fukui, Noriaki Takeda
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
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