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Histamine receptors

Yu-Na Im, Yu-Dong Lee, Jeong-Soo Park, Hae-Kyoung Kim, Suhn-Young Im, Hwa-Ryung Song, Hern-Ku Lee, Myung-Kwan Han
Many itch mediators activate G-protein coupled receptor (GPCR), and trigger itch via activation of GPCR-mediated signaling pathways. GPCRs are desensitized by G protein-coupled receptor kinases (GRKs). The aim of this study is to explore the role of GRKs in itch response and the linkage between GRKs and glutamine (Gln), an amino acid previously demonstrated as an itching reliever. Itch responses were evoked by histamine, chloroquine (CQ), and dinitrochlorobenzene (DNCB)-induced contact dermatitis (CD). Phosphorylation and protein expression were detected by immunofluorescent staining and Western blotting...
March 9, 2018: Journal of Investigative Dermatology
Sabine Buhner, Hannes Hahne, Kerstin Hartwig, Qin Li, Sheila Vignali, Daniela Ostertag, Chen Meng, Gabriele Hörmannsperger, Breg Braak, Christian Pehl, Thomas Frieling, Giovanni Barbara, Roberto De Giorgio, Ihsan Ekin Demir, Güralp Onur Ceyhan, Florian Zeller, Guy Boeckxstaens, Dirk Haller, Bernhard Kuster, Michael Schemann
BACKGROUND & AIMS: The causes of gastrointestinal complaints in irritable bowel syndrome (IBS) remain poorly understood. Altered nerve function has emerged as an important pathogenic factor as IBS mucosal biopsy supernatants consistently activate enteric and sensory neurons. We investigated the neurally active molecular components of such supernatants from patients with IBS and quiescent ulcerative colitis (UC). METHOD: Effects of supernatants from 7 healthy controls (HC), 20 IBS and 12 UC patients on human and guinea pig submucous neurons were studied with neuroimaging techniques...
2018: PloS One
Carolina Mondillo, María Luisa Varela, Adriana María Belén Abiuso, Ramiro Vázquez
Histamine (HA) is a pleiotropic biogenic amine synthesized exclusively by histidine decarboxylase (HDC) in most mammalian tissues. The literature on the role of HA within the male gonad has expanded over the last years, attracting attention to potential unexpected side-effects of anti-histamines on testicular function. In this regard, HA receptors (HRH1, HRH2 and HRH4) have been described in Leydig cells of different species, including human. Via these receptors, HA has been reported to trigger positive or negative interactions with the LH/hCG signaling pathway depending upon its concentration, thereby contributing to the local control of testicular androgen levels...
March 9, 2018: Reproduction: the Official Journal of the Society for the Study of Fertility
Colin A Nurse, Erin M Leonard, Shaima Salman
Mammalian carotid bodies (CB) are chemosensory organs that mediate compensatory cardiorespiratory reflexes in response to low blood PO2 (hypoxemia) and elevated CO2 /H+ (acid hypercapnia). The chemoreceptors are glomus or type I cells which occur in clusters enveloped by neighboring glial-like type II cells. During chemoexcitation type I cells depolarize, leading to Ca2+ -dependent release of several neurotransmitters, some excitatory and others inhibitory, which help shape the afferent carotid sinus nerve (CSN) discharge...
March 9, 2018: Physiological Genomics
T-W Chuang, S-C Chen, K-T Chen
AIMS: The aim of this study was to explore the recent advances in diagnosis and treatment of gastroesophageal reflux disease (GERD). METHODS: Previous studies were searched using the terms "gastroesophageal reflux disease" and "diagnosis" or "treatment" in Medline and Pubmed. Articles that were not published in the English language, manuscripts without an abstract, reviews, meta-analysis, and opinion articles were excluded from the review...
July 2017: Acta Gastro-enterologica Belgica
Keegan Lutek, Rasmeet Singh Dhaliwal, Terence J Van Raay, Andreas Heyland
Settlement is a rapid process in many marine invertebrate species, transitioning a planktonic larva into a benthic juvenile. In indirectly developing sea urchins, this ecological transition correlates with a morphological, developmental and physiological transition (metamorphosis) during which apoptosis is essential for the resorption and remodelling of larval and juvenile structures. While settlement is initiated by environmental cues (i.e. habitat-specific or benthic substrate cues), metamorphosis is regulated by developmental endocrine signals, such as histamine (HA), thyroid hormones (THs) and nitric oxide (NO)...
March 5, 2018: Scientific Reports
Masaru Ihara, Han Zhang, Seiya Hanamoto, Hiroaki Tanaka
 Pharmaceuticals are widely found in aquatic environments worldwide. Concern about their potential risks to aquatic species has been raised because they are designed to be biologically active. To address this concern, we must know whether biological activity of pharmaceuticals can be detected in waters. Nearly half of all marketed pharmaceuticals act by binding to the G protein-coupled receptor (GPCR). In this study, we measured the physiological activity of GPCR-acting pharmaceuticals in effluent from a wastewater treatment plant (WWTP) and upstream and downstream of its outfall in Japan during 2 years...
2018: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
Qian-Xing Zhuang, Han-Ting Xu, Xu-Juan Lu, Bin Li, Wing-Ho Yung, Jian-Jun Wang, Jing-Ning Zhu
The central histaminergic nervous system, originating from the tuberomammillary nucleus (TMN) of the hypothalamus, widely innervates almost the whole brain, including the basal ganglia. Intriguingly, the histaminergic system is altered in parkinsonian patients. Yet, little is known about the effect and mechanisms of histamine on different types of neurons in the basal ganglia circuitry. Here, by using anterograde tracing, immunostaining, patch clamp recording, and single-cell qPCR techniques, we investigate the histaminergic afferents in the striatum, the major input structure of the basal ganglia, as well as the effect of histamine on the striatal GABAergic medium spiny projection neurons (MSNs)...
March 1, 2018: Molecular Neurobiology
Renee K McAlister, Jonathan Aston, Megan Pollack, Liping Du, Tatsuki Koyama, David D Chism
BACKGROUND: Pazopanib is an oral tyrosine-kinase inhibitor that is approved by the U.S. Food and Drug Administration for treatment of metastatic renal cell carcinoma (mRCC). Pharmacokinetic data have shown that concomitant administration of pazopanib and esomeprazole, a proton pump inhibitor (PPI), leads to decreased area under the curve and thus decreased exposure of pazopanib by 40%. Despite the pharmacokinetic data published to date, the clinical significance and impact on patient outcomes resulting from decreased pazopanib exposure remains unknown...
February 27, 2018: Oncologist
Tobias Atkin, Stefano Comai, Gabriella Gobbi
Although the GABAergic benzodiazepines (BZDs) and Z-drugs (zolpidem, zopiclone, and zaleplon) are FDA-approved for insomnia disorders with a strong evidence base, they have many side effects, including cognitive impairment, tolerance, rebound insomnia upon discontinuation, car accidents/falls, abuse, and dependence liability. Consequently, the clinical use of off-label drugs and novel drugs that do not target the GABAergic system is increasing. The purpose of this review is to analyze the neurobiological and clinical evidence of pharmacological treatments of insomnia, excluding the BZDs and Z-drugs...
April 2018: Pharmacological Reviews
Kun Huang, Dan-Dan Hu, Dong Bai, Ze-Yang Wu, Yi-Yang Chen, Yi-Jun Zhang, Xin Lv, Qing-Xiu Wang, Ling Zhang
Transient extracellular signal-regulated kinase (ERK) activation in the spinal cord triggers histamine-induced acute itch. However, whether persistent ERK activation plays an important role in chronic itch development remains unclear. This study investigated the role of spinal ERK activation in chronic itch. The results showed that repetitive 2,4-dinitrofluorobenzene (DNFB) painting on the nape of mice evoked not only initial scratching but also sustained, spontaneous scratching. In addition, DNFB induced itching rather than nociception, as demonstrated using a cheek model...
February 24, 2018: Journal of Investigative Dermatology
Katarzyna Popiolek-Barczyk, Dorota Łażewska, Gniewomir Latacz, Agnieszka Olejarz, Wioletta Makuch, Holger Stark, Katarzyna Kieć-Kononowicz, Joanna Mika
BACKGROUND AND PURPOSE: The histaminergic system is a promising target for the development of new analgesics, since expression of histamine H3 R and H4 R receptors has been reported in regions related to nociceptive transmission. The aim of our study was to determine the analgesic effects of new H3 R and H4 R antagonists in naive and neuropathic (CCI, chronic constriction injury) male and female mice. EXPERIMENTAL APPROACH: We investigated the effects of newly synthesized H3 R (E-162; 1-(5-(naphthalen-1-yloxy)pentyl)piperidine) and H4 R (TR-7; 4-(4-chlorophenyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) antagonists on mechanical (von Frey) and thermal (cold plate, tail flick) stimuli in naive and CCI-exposed (7 days after injury) animals...
February 27, 2018: British Journal of Pharmacology
Nermin Eissa, Nadia Khan, Shreesh K Ojha, Dorota Łazewska, Katarzyna Kieć-Kononowicz, Bassem Sadek
The role of Histamine H3 receptors (H3Rs) in memory, and the prospective of H3R antagonists in pharmacological control of neurodegenerative disorders, e.g., Alzheimer disease (AD) is well-accepted. For that reason, the procognitive effects of the H3R antagonist DL77 on cognitive impairments induced with MK801 were tested in an inhibitory passive avoidance paradigm (PAP) and novel object recognition (NOR) task in adult male rats, using donepezil (DOZ) as a standard drug. Acute systemic pretreatment with DL77 (2...
2018: Frontiers in Neuroscience
Jun-Kyoung Lee, Sang-Hyun Kim
Perfluorinated compounds (PFC) have widely been used in numerous applications including clothing, food packaging, and nonstick coating. With the widespread use of PFC, concerns regarding potential adverse health effects in humans and wildlife have increased. In spite of the known PFC-mediated immunotoxiciy, correlation with PFC and allergic inflammation still requires elucidation. The aim of this study was to examine the effect of four types of PFC (perfluoroheptanoic acid [PFHpA], perfluorononanoic acid [PFNA], perfluorodecanoic acid [PFDA], and perfluoroundecanoic acid [PFUnA]) on mast cell-mediated allergic inflammation in the presence of high-affinity immunoglobulin (Ig) E receptor (FcεRI) cross-linking...
February 26, 2018: Journal of Toxicology and Environmental Health. Part A
Anna Affini, Stefanie Hagenow, Aleksandra Zivkovic, Jose Marco-Contelles, Holger Stark
The design of multi-targeting ligands was developed in the last decades as an innovative therapeutic concept for Parkinson's disease (PD) and other neurodegenerative disorders. As the monoamine oxidase B (MAO B) and the histamine H3 receptor (H3 R) are promising targets for dopaminergic regulation, we synthetized dual-targeting ligands (DTLs) as non-dopaminergic receptor approach for the treatment of PD. Three series of compounds were developed by attaching the H3 R pharmacophore to indanone-related MAO B motifs, leading to development of MAO B/H3 R DTLs...
February 16, 2018: European Journal of Medicinal Chemistry
Lee-Ming Kow, Donald W Pfaff
This paper reviews early evidence for the existence of rapid, non-genomic effects of estrogens on neurons, and, further, proposes that these rapid effects are often synergistic with later, genomic effects. Finally, suggestions about potential molecular mechanisms underlying the rapid effects of estrogens are offered. A mechanistic step we propose to be common among rapid estrogenic actions includes membrane ER's binding to histamine, and NMDA receptors and subsequent dimerization, and clustering (respectively) in a manner that enhances histamine and NMDA actions...
February 21, 2018: Hormones and Behavior
Benjamin Scally, Jonathan R Emberson, Enti Spata, Christina Reith, Kelly Davies, Heather Halls, Lisa Holland, Kate Wilson, Neeraj Bhala, Christopher Hawkey, Marc Hochberg, Richard Hunt, Loren Laine, Angel Lanas, Carlo Patrono, Colin Baigent
BACKGROUND: Gastroprotectant drugs are used for the prevention and treatment of peptic ulcer disease and might reduce its associated complications, but reliable estimates of the effects of gastroprotectants in different clinical settings are scarce. We aimed to examine the effects of proton-pump inhibitors (PPIs), prostaglandin analogues, and histamine-2 receptor antagonists (H2RAs) in different clinical circumstances by doing meta-analyses of tabular data from all relevant unconfounded randomised trials of gastroprotectant drugs...
February 20, 2018: Lancet. Gastroenterology & Hepatology
Ovadyah Avraham, Michael Biglow
BACKGROUND: Deprescribing is a recommended intervention to reduce morbidity and mortality caused by polypharmacy in older residents. However, a lack of definite deprescription guidelines and evidence of clinically meaningful outcomes complicates or precludes the practicality of such an approach. OBJECTIVE: The objective of the present pilot study is to establish and implement a stepwise taper protocol that can potentially minimize overuse of proton pump inhibitors in a safe, effective, and feasible manner in the nursing home...
February 1, 2018: Annals of Pharmacotherapy
Jane C Bell, Francisco J Schneuer, Christopher Harrison, Lyndal Trevena, Harriet Hiscock, Adam G Elshaug, Natasha Nassar
OBJECTIVES: To evaluate the diagnosis and management of reflux and gastro-oesophageal reflux disease (GORD) in infants aged <1 year presenting to general practitioners (GPs). DESIGN, SETTING AND PARTICIPANTS: A nationally representative, prospective, cross-sectional survey of GP activity in Australia, 2006-2016 (Bettering the Evaluation And Care of Health Study). Annually, a random sample of around 1000 GPs recorded details for 100 consecutive visits with consenting, unidentified patients...
February 22, 2018: Archives of Disease in Childhood
T Werfel, A Wollenberg, T Pumnea, A Heratizadeh
In severe cases of atopic dermatitis (AD) systemic treatment is indicated. So far, cyclosporine and systemic glucocorticosteroids represented the only systemic treatment options approved for the indications of AD in Germany; however, from clinical practice there is increasing evidence for beneficial therapeutic effects in AD by other immunosuppressive or immunomodulatory substances, such as mycophenolate, methotrexate, alitretinoin and ustekinumab. Beyond this, ongoing research activities focus on a better understanding of genetic and immunological aspects of this chronic inflammatory skin disease...
February 22, 2018: Der Hautarzt; Zeitschrift Für Dermatologie, Venerologie, und Verwandte Gebiete
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