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Histamine H3

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
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
Niels J Hauwert, Tamara A M Mocking, Daniel Da Costa Pereira, Albert J Kooistra, Lisa M Wijnen, Gerda Vreeker, Noortje W E Verweij, Bert H De Boer, Martine J Smit, Chris de Graaf, Henry F Vischer, Iwan J P De Esch, Maikel Wijtmans, Rob Leurs
Non-invasive methods to modulate G protein-coupled receptors (GPCRs) with temporal and spatial precision are in great demand. Photopharmacology uses photons to control in situ the biological properties of photoswitchable small-molecule ligands which bodes well for chemical biological precision approaches. Integrating the light-switchable configurational properties of an azobenzene into the ligand core, we developed a bi-directional antagonist toolbox for an archetypical family A GPCR, the histamine H3 receptor (H3R)...
February 22, 2018: Journal of the American Chemical Society
Elvia Mena-Avila, Ricardo Márquez-Gómez, Guillermo Aquino-Miranda, Gustavo Nieto-Alamilla, José-Antonio Arias-Montaño
BACKGROUND: Clobenpropit, a potent antagonist/inverse agonist at the histamine H3 receptor (H3R), reduced the cytotoxic action of 6-hydroxydopamine (6-OHDA) in neuroblastoma SH-SY5Y cells transfected with the human H3R. We therefore set out to study whether this effect involved a receptor-independent action on dopamine transport. METHODS: The uptake of [3H]-dopamine was assayed in SH-SY5Y cells and rat striatal or cerebro-cortical isolated nerve terminals (synaptosomes)...
August 30, 2017: Pharmacological Reports: PR
Hyunju Kim, Minsu Jang, Rackhyun Park, Daum Jo, Inho Choi, Joonho Choe, Won Keun Oh, Junsoo Park
Conessine, a steroidal alkaloid, is a potent histamine H3 antagonist with anti-malarial activity. We recently reported that conessine treatment interferes with H₂O₂-induced cell death by regulating autophagy. However, the cellular signaling pathways involved in conessine treatment are not fully understood. Here, we report that conessine reduces muscle atrophy by interfering with the expression of atrophy-related ubiquitin ligases MuRF-1 and atrogin-1. Promoter reporter assay revealed that conessine treatment inhibits FoxO3a-dependent transcription, NF-kappaB-dependent transcription and p53-dependent transcription...
February 1, 2018: Journal of Microbiology and Biotechnology
Rafael Koerich Varaschin, Guillaume Osterstock, Charles Ducrot, Sakari Leino, Marie-Josée Bourque, Marco A M Prado, Vania Ferreira Prado, Outi Salminen, Saara Rannanpää Née Nuutinen, Louis-Eric Trudeau
Histamine H3 receptors are widely distributed Gi-coupled receptors whose activation reduces neuronal activity and inhibits release of numerous neurotransmitters. Although these receptors are abundantly expressed in the striatum, their modulatory role on activity-dependent dopamine release is not well understood. Here, we observed that histamine H3 receptor activation indirectly diminishes dopamine overflow in the ventral striatum by reducing cholinergic interneuron activity. Acute brain slices from C57BL/6 or channelrhodopsin-2-transfected DAT-cre mice were obtained, and dopamine transients evoked either electrically or optogenetically were measured by fast-scan cyclic voltammetry...
January 24, 2018: Neuroscience
Dorota Łażewska, Katarzyna Kieć-Kononowicz
Since years, ligands blocking histamine H3 receptor (H3R) activity (antagonists/inverse agonists) are interesting targets in the search for new cures for CNS disorders. Intensive works done by academic and pharmaceutical company researchers have led to many potent and selective H3R antagonists/inverse agonists. Some of them have reached to clinical trials. Areas covered: Patent applications from January 2013 to September 2017 and the most important topics connected with H3R field are analysed. Espacenet, Patentscope, Pubmed, GoogleScholar or Cochrane Library online databases were principially used to collect all the materials...
January 15, 2018: Expert Opinion on Therapeutic Patents
Rafael K Varaschin, Nyika A Allen, Martina J Rosenberg, C Fernando Valenzuela, Daniel D Savage
BACKGROUND: We have reported that prenatal alcohol exposure (PAE)-induced deficits in dentate gyrus, long-term potentiation (LTP), and memory are ameliorated by the histamine H3 receptor inverse agonist ABT-239. Curiously, ABT-239 did not enhance LTP or memory in control offspring. Here, we initiated an investigation of how PAE alters histaminergic neurotransmission in the dentate gyrus and other brain regions employing combined radiohistochemical and electrophysiological approaches in vitro to examine histamine H3 receptor number and function...
December 5, 2017: Alcoholism, Clinical and Experimental Research
Hooman Heidarzadeh, Morteza Zendehdel, Vahab Babapour, Hasan Gilanpour
The present study was designed to determine the effect of central injection of Nesfatin-1 and corticotropin and histaminergic systems on food intake in neonatal meat-type chicks. In this study, 7 experiments were designed, each with 4 treatment groups. In experiment 1, four groups of chicks received the ICV injection of (A) phosphate-buffered saline (PBS), (B) Nesfatin-1 (10 ng), (C) Nesfatin-1 (20 ng) and (D) Nesfatin-1 (40 ng). In experiment 2, (A) PBS, (B) Astressin-B (CRF1/CRF2 receptors antagonist; 30 µg), (C) Nesfatin-1 (40 ng) and (D) Nesfatin-1 + Astressin-B were injected...
December 26, 2017: Veterinary Research Communications
Savina Apolloni, Paola Fabbrizio, Susanna Amadio, Giulia Napoli, Veronica Verdile, Giovanna Morello, Rosario Iemmolo, Eleonora Aronica, Sebastiano Cavallaro, Cinzia Volonté
Amyotrophic lateral sclerosis (ALS) is a late-onset motor neuron disease where activated glia release pro-inflammatory cytokines that trigger a vicious cycle of neurodegeneration in the absence of resolution of inflammation. Given the well-established role of histamine as a neuron-to-glia alarm signal implicated in brain disorders, the aim of this study was to investigate the expression and regulation of the histaminergic pathway in microglial activation in ALS mouse model and in humans. By examining the contribution of the histaminergic system to ALS, we found that particularly via H1 and H4 receptors, histamine promoted an anti-inflammatory profile in microglia from SOD1-G93A mice by modulating their activation state...
2017: Frontiers in Immunology
H L Haas
No abstract text is available yet for this article.
March 2018: Acta Physiologica
Ricardo Márquez-Gómez, Meridith T Robins, Citlaly Gutiérrez-Rodelo, Juan-Manuel Arias, Jesús-Alberto Olivares-Reyes, Richard M van Rijn, José-Antonio Arias-Montaño
In the striatum, histamine H3 receptors (H3 Rs) are co-expressed with adenosine A2A receptors (A2A Rs) in the cortico-striatal glutamatergic afferents and the GABAergic medium-sized spiny neurons that originate the indirect pathway of the basal ganglia. This location allows H3 Rs and A2A Rs to regulate the striatal GABAergic and glutamatergic transmission. However, whether these receptors can physically interact has not yet been assessed. To test this hypothesis, a heteromer-selective in vitro assay was used to detect functional complementation between a chimeric A2A R302 -Gαqi4 and wild-type H3 Rs in transfected HEK-293T cells...
March 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Michelle F Corrêa, Álefe J R Barbosa, Larissa B Teixeira, Diego A Duarte, Sarah C Simões, Lucas T Parreiras-E-Silva, Aleksandro M Balbino, Richardt G Landgraf, Michel Bouvier, Claudio M Costa-Neto, João P S Fernandes
The histamine receptors (HRs) are traditional G protein-coupled receptors of extensive therapeutic interest. Recently, H3 R and H4 R subtypes have been targeted in drug discovery projects for inflammation, asthma, pain, cancer, Parkinson's, and Alzheimer's diseases, which includes searches for dual acting H3 R/H4 R ligands. In the present work, nine 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazine (LINS01 series) molecules were synthesized and evaluated as H3 R and H4 R ligands. Our data show that the N -allyl-substituted compound LINS01004 bears the highest affinity for H3 R (p K i 6...
2017: Frontiers in Pharmacology
Katarzyna Szczepanska, Kamil Kuder, Katarzyna Kiec-Kononowicz
Since its' discovery in 1983, followed by gene cloning in 1999, the histamine H3 receptor served as an outstanding target for drug discovery. The wide spectrum of possible therapeutic implications make H3R's one of the most researched areas in the vast GPCR ligands field - started from imidazole containing ligands, through various successful imidazole replacements, with recent introduction of Wakix® to pharmaceutical market. One of such replacements is piperazine moiety, a significant versatile scaffold in rational drug design for most of the GPCR ligands...
November 23, 2017: Current Medicinal Chemistry
Hiroki Takei, Kiyofumi Yamamoto, Yong-Chul Bae, Tetsuo Shirakawa, Masayuki Kobayashi
Histamine H3 receptors are autoreceptors that regulate histamine release from histaminergic neuronal terminals. The cerebral cortex, including the insular cortex (IC), expresses abundant H3 receptors; however, the functions and mechanisms of H3 receptors remain unknown. The aim of this study was to elucidate the functional roles of H3 in synaptic transmission in layer V of the rat IC. Unitary excitatory and inhibitory postsynaptic currents (uEPSCs and uIPSCs) were obtained through paired whole-cell patch-clamp recording in cerebrocortical slice preparations...
2017: Frontiers in Neural Circuits
Ana-Maricela García-Gálvez, Juan Escamilla-Sánchez, Catalina Flores-Maldonado, Rubén-Gerardo Contreras, Juan-Manuel Arias, José-Antonio Arias-Montaño
Histamine H3 receptors (H3 Rs) signal through Gαi/o proteins and are found in neuronal cells as auto- and hetero-receptors. Alternative splicing of the human H3 R (hH3 R) originates 20 isoforms, and the mRNAs of two receptors of 445 and 365 amino acids (hH3 R445 and hH3 R365 ) are widely expressed in the human brain. We previously showed that the hH3 R445 stably expressed in CHO-K1 cells experiences homologous desensitization. The hH3 R365 lacks 80 residues in the third intracellular loop, and in this work we therefore studied whether this isoform also experiences homologous desensitization and the possible differences with the hH3 R445 ...
January 2018: Neurochemistry International
Luciana Lyra Casais-E-Silva, Catarina Teixeira
BACKGROUND/AIMS: Micrurus is one of the four snake genera of medical importance in Brazil. Coral snakes have a broad geographic distribution from the southern United States to Argentina. Micrurine envenomation is characterized by neurotoxic symptoms leading to dyspnea and death. Moreover, various local manifestations, including edema formation, have been described in patients bitten by different species of Micrurus. Thus, we investigated the ability of Micrurus lemniscatus venom (MLV) to induce local edema...
November 2017: PLoS Neglected Tropical Diseases
Hari S Sharma, Ranjana Patnaik, Dafin F Muresanu, José V Lafuente, Asya Ozkizilcik, Z Ryan Tian, Ala Nozari, Aruna Sharma
The possibility that histamine influences the spinal cord pathophysiology following trauma through specific receptor-mediated upregulation of neuronal nitric oxide synthase (nNOS) was examined in a rat model. A focal spinal cord injury (SCI) was inflicted by a longitudinal incision into the right dorsal horn of the T10-11 segments. The animals were allowed to survive 5h. The SCI significantly induced breakdown of the blood-spinal cord barrier to protein tracers, reduced the spinal cord blood flow at 5h, and increased the edema formation and massive upregulation of nNOS expression...
2017: International Review of Neurobiology
Alaa Alachkar, Dorota Łażewska, Katarzyna Kieć-Kononowicz, Bassem Sadek
The involvement of histamine H3 receptors (H3Rs) in memory is well known, and the potential of H3R antagonists in therapeutic management of neuropsychiatric diseases, e.g., Alzheimer disease (AD) is well established. Therefore, the effects of histamine H3 receptor (H3R) antagonist E159 (2.5-10 mg/kg, i.p.) in adult male rats on dizocilpine (DIZ)-induced memory deficits were studied in passive avoidance paradigm (PAP) and in novel object recognition (NOR) using pitolisant (PIT) and donepezil (DOZ) as standard drugs...
2017: Frontiers in Pharmacology
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