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Histamine H3

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https://www.readbyqxmd.com/read/29729290/anticonvulsant-evaluation-of-novel-non-imidazole-histamine-h-3-r-antagonists-in-different-convulsion-models-in-rats
#1
Alaa Alachkar, Gniewomir Latacz, Agata Siwek, Annamaria Lubelska, Ewelina Honkisz, Anna Gryboś, Dorota Łażewska, Jadwiga Handzlik, Holger Stark, Katarzyna Kiec-Kononowicz, Bassem Sadek
Novel non-imidazole histamine H3 receptor (H3R) antagonists (2-8) were developed and assessed for in-vitro antagonist binding affinities at the human histamine H1-H4R. These novel H3R antagonists (2-8) were examined in-vivo for anticonvulsant effects in three different convulsion models in male adult rats. Compound 6 significantly and dose-dependently exhibited decreased duration of tonic hind limb extension (THLE) in the maximal electroshock (MES)- and fully protected animals against pentylenetetrazole (PTZ)-induced convulsion, following acute systemic administration (5, 10, and 20 mg/kg, i...
May 2, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29724080/conessine-treatment-reduces-dexamethasone-induced-muscle-atrophy-by-regulating-murf1-and-atrogin-1-expression
#2
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 antimalarial 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-κB-dependent transcription, and p53-dependent transcription...
April 28, 2018: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/29723785/synthesis-and-biological-activity-of-novel-tert-butyl-and-tert-pentylphenoxyalkyl-piperazine-derivatives-as-histamine-h-3-r-ligands
#3
Katarzyna Szczepańska, Tadeusz Karcz, Szczepan Mogilski, Agata Siwek, Kamil J Kuder, Gniewomir Latacz, Monika Kubacka, Stefanie Hagenow, Annamaria Lubelska, Agnieszka Olejarz, Magdalena Kotańska, Bassem Sadek, Holger Stark, Katarzyna Kieć-Kononowicz
As a continuation of our search for novel histamine H3 receptor ligands, a series of twenty four new tert-butyl and tert-pentyl phenoxyalkylamine derivatives (2-25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer were evaluated for their binding properties at human histamine H3 receptor (hH3 R). The highest affinities were observed for 4-pyridyl derivatives 4, 10, 16 and 22 (Ki  = 16.0-120 nM). As it has been shown in docking studies, those specific heteroaromatic 4-N piperazine substituents might interact with one of the key receptor interacting amino acids...
April 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29701013/visualization-of-the-activation-of-the-histamine-h3-receptor-h3r-using-novel-fluorescence-resonance-energy-transfer-biosensors-and-their-potential-application-to-the-study-of-h3r-pharmacology
#4
Ying Liu, Hong Zeng, John D Pediani, Richard J Ward, Lu-Yao Chen, Nan Wu, Li Ma, Mei Tang, Yang Yang, Su An, Xiao-Xi Guo, Qian Hao, Tian-Rui Xu
Activation of the Histamine-3 receptor (H3R) is involved in memory processes and cognitive action, whilst blocking H3R activation can slow the progression of neurological disorders such as Alzheimer's disease, schizophrenia and narcolepsy. To date however no direct way to examine the activation of H3R has been utilised. Here, we describe a novel biosensor which can visualise the activation of H3R through an intramolecular Fluorescence Resonance Energy Transfer (FRET) signal. To achieve this, we constructed an intramolecular H3R FRET sensor with cyan fluorescent protein (CFP) attached at the C-terminus and yellow fluorescent protein (YFP) inserted into the third intracellular loop...
April 26, 2018: FEBS Journal
https://www.readbyqxmd.com/read/29681486/novel-naphthyloxy-derivatives-potent-histamine-h-3-receptor-ligands-synthesis-and-pharmacological-evaluation
#5
Dorota Łażewska, Maria Kaleta, Stefanie Hagenow, Szczepan Mogilski, Gniewomir Latacz, Tadeusz Karcz, Annamaria Lubelska, Ewelina Honkisz, Jadwiga Handzlik, David Reiner, Grzegorz Satała, Barbara Filipek, Holger Stark, Katarzyna Kieć-Kononowicz
A series of 1- and 2-naphthyloxy derivatives were synthesized and evaluated for histamine H3 receptor affinity. Most compounds showed high affinities with Ki values below 100 nM. The most potent ligand, 1-(5-(naphthalen-1-yloxy)pentyl)azepane (11) displayed high affinity for the histamine H3 receptor with a Ki value of 21.9 nM. The antagonist behaviour of 11 was confirmed both in vitro in the cAMP assay (IC50  = 312 nM) and in vivo in the rat dipsogenia model (ED50  = 3.68 nM). Moreover, compound 11 showed positive effects on scopolamine induced-memory deficits in mice (at doses of 10 and 15 mg/kg) and an analgesic effect in the formalin test in mice with ED50  = 30...
April 11, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29675928/differential-cardiac-sympatho-inhibitory-responses-produced-by-the-agonists-b-ht-933-quinpirole-and-immepip-in-normoglycemic-and-diabetic-pithed-rats
#6
Eduardo Rivera-Mancilla, Alain H Altamirano-Espinoza, Guadalupe Manrique-Maldonado, Belinda Villanueva-Castillo, Carlos M Villalón
This study compared the cardiac sympatho-inhibitory responses produced by agonists at α2 -adrenergic (B-HT 933), dopamine D2 -like (quinpirole) and histamine H3 /H4 (immepip) receptors between normoglycemic and streptozotocin-pretreated (diabetic) pithed rats. Intravenous (i.v.) continuous infusions of B-HT 933, quinpirole or immepip were used in normoglycemic and diabetic pithed rats to analyse their sympatho-inhibitory effects on the electrically-stimulated cardioaccelerator sympathetic outflow. Both in normoglycemic and diabetic animals, B-HT 933 (until 100 μg/kg...
April 19, 2018: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29557708/differential-expression-and-signaling-of-the-human-histamine-h-3-receptor-isoforms-of-445-and-365-amino-acids-expressed-in-human-neuroblastoma-sh-sy5y-cells
#7
Gustavo Nieto-Alamilla, Juan Escamilla-Sánchez, María-Cristina López-Méndez, Anayansi Molina-Hernández, Agustín Guerrero-Hernández, José-Antonio Arias-Montaño
In stably-transfected human neuroblastoma SH-SY5Y cells, we have compared the effect of activating two isoforms of 445 and 365 amino acids of the human histamine H3 receptor (hH3 R445 and hH3 R365 ) on [35 S]-GTPγS binding, forskolin-induced cAMP formation, depolarization-induced increase in the intracellular concentration of Ca2+ ions ([Ca2+ ]i) and depolarization-evoked [3  H]-dopamine release. Maximal specific binding (Bmax ) of [3  H]-N-methyl-histamine to cell membranes was 953 ± 204 and 555 ± 140 fmol/mg protein for SH-SY5Y-hH3 R445 and SH-SY5Y-hH3 R365 cells, respectively, with similar dissociation constants (Kd , 0...
March 20, 2018: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/29554815/liquid-chromatography-tandem-mass-spectrometry-method-for-the-quantification-of-a-potent-h-3-receptor-antagonist-conessine-in-serum-and-its-application-to-pharmacokinetic-studies
#8
Mahendra Shukla, Femi M Francis, Jawahar Lal
Conessine, a steroidal alkaloid obtained from the bark and seeds of the plant species of Apocynaceae family, elicits a histamine antagonistic action, selectively for the H3 histaminergic receptors. This alkaloid is used mainly for the treatment of dysentery and helminthic disorders. For the quantification of conessine in serum, a liquid chromatography-tandem mass spectrometry method was developed. Chromatographic separation was achieved on a Zorbax SB-CN column (100 × 4.6 mm, 3.5 µm), and a mobile phase consisting of 90% methanol in aqueous ammonium acetate buffer (pH 3...
January 1, 2018: European Journal of Mass Spectrometry
https://www.readbyqxmd.com/read/29486058/antinociceptive-effects-of-novel-histamine-h-3-r-and-h-4-r-receptor-antagonists-and-their-influence-on-morphine-analgesia-of-neuropathic-pain-in-the-mouse
#9
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
https://www.readbyqxmd.com/read/29483860/the-histamine-h3-receptor-antagonist-dl77-ameliorates-mk801-induced-memory-deficits-in-rats
#10
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
https://www.readbyqxmd.com/read/29477889/novel-indanone-derivatives-as-mao-b-h-3-r-dual-targeting-ligands-for-treatment-of-parkinson-s-disease
#11
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...
March 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29470065/synthesis-and-characterization-of-a-bidirectional-photoswitchable-antagonist-toolbox-for-real-time-gpcr-photopharmacology
#12
Niels J Hauwert, Tamara A M Mocking, Daniel Da Costa Pereira, Albert J Kooistra, Lisa M Wijnen, Gerda C M Vreeker, Eléonore W E Verweij, Albertus H De Boer, Martine J Smit, Chris De Graaf, Henry F Vischer, Iwan J P de Esch, Maikel Wijtmans, Rob Leurs
Noninvasive 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 bidirectional antagonist toolbox for an archetypical family A GPCR, the histamine H3 receptor (H3 R)...
March 28, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29414147/clobenpropit-a-histamine-h-3-receptor-antagonist-inverse-agonist-inhibits-3-h-dopamine-uptake-by-human-neuroblastoma-sh-sy5y-cells-and-rat-brain-synaptosomes
#13
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 (H3 R), reduced the cytotoxic action of 6-hydroxydopamine (6-OHDA) in neuroblastoma SH-SY5Y cells transfected with the human H3 R. We therefore set out to study whether this effect involved a receptor-independent action on dopamine transport. METHODS: The uptake of [3 H]-dopamine was assayed in SH-SY5Y cells and rat striatal or cerebro-cortical isolated nerve terminals (synaptosomes)...
February 2018: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29385661/conessine-treatment-reduces-dexamethasone-induced-muscle-atrophy-by-regulating-murf1-and-atrogin-1-expression
#14
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
https://www.readbyqxmd.com/read/29374538/histamine-h-3-receptors-decrease-dopamine-release-in-the-ventral-striatum-by-reducing-the-activity-of-striatal-cholinergic-interneurons
#15
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...
April 15, 2018: Neuroscience
https://www.readbyqxmd.com/read/29334795/progress-in-the-development-of-histamine-h-3-receptor-antagonists-inverse-agonists-a-patent-review-2013-2017
#16
REVIEW
Dorota Łażewska, Katarzyna Kieć-Kononowicz
Since years, ligands blocking histamine H3 receptor (H3 R) 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 H3 R 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 H3 R field are analysed. Espacenet, Patentscope, Pubmed, GoogleScholar or Cochrane Library online databases were principially used to collect all the materials...
March 2018: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29315624/prenatal-alcohol-exposure-increases-histamine-h-3-receptor-mediated-inhibition-of-glutamatergic-neurotransmission-in-rat-dentate-gyrus
#17
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...
February 2018: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29280084/the-effect-of-nesfatin-1-on-food-intake-in-neonatal-chicks-role-of-crf-1-crf2-and-h1-h3-receptors
#18
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...
March 2018: Veterinary Research Communications
https://www.readbyqxmd.com/read/29250069/histamine-regulates-the-inflammatory-profile-of-sod1-g93a-microglia-and-the-histaminergic-system-is-dysregulated-in-amyotrophic-lateral-sclerosis
#19
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
https://www.readbyqxmd.com/read/29230959/fishing-for-histamine-h3-receptor-functions
#20
EDITORIAL
H L Haas
No abstract text is available yet for this article.
March 2018: Acta Physiologica
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