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Histamine H3

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https://www.readbyqxmd.com/read/29315624/prenatal-alcohol-exposure-increases-histamine-h3-receptor-mediated-inhibition-of-glutamatergic-neurotransmission-in-rat-dentate-gyrus
#1
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
https://www.readbyqxmd.com/read/29280084/the-effect-of-nesfatin-1-on-food-intake-in-neonatal-chicks-role-of-crf1-crf2-and-h1-h3-receptors
#2
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
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
#3
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
#4
EDITORIAL
Helmut Haas
Puttonen et al. (this issue) report behavioral features and abnormalities of zebrafish lacking the histamine H3 receptor, which regulates the release of several neurotransmitters, including GABA, glutamate, histamine, serotonin, noradrenaline and dopamine1 . Despite normal morphological development, mutant larvae show faster locomotor adaptation to sudden darkness than control larvae, whereas there are no differences in basic locomotor activity during daytime and night. Zebrafish sleep, defined by immobility for a period of longer than 1 min, is normal in hrh3 KO larvae...
December 12, 2017: Acta Physiologica
https://www.readbyqxmd.com/read/29217157/functional-histamine-h3-and-adenosine-a2a-receptor-heteromers-in-recombinant-cells-and-rat-striatum
#5
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 (H3Rs) are co-expressed with adenosine A2A receptors (A2ARs) in the cortico-striatal glutamatergic afferents and the GABAergic medium-sized spiny neurons that originate from the indirect pathway of the basal ganglia. This location allows H3Rs and A2ARs 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 A2AR302-Gαqi4 and wild-type H3Rs in transfected HEK-293 cells...
December 4, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29184503/pharmacological-characterization-of-5-substituted-1-2-3-dihydro-1-benzofuran-2-yl-methyl-piperazines-novel-antagonists-for-the-histamine-h3-and-h4-receptors-with-anti-inflammatory-potential
#6
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, H3R and H4R 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 H3R/H4R ligands. In the present work, nine 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazine (LINS01 series) molecules were synthesized and evaluated as H3R and H4R ligands. Our data show that the N-allyl-substituted compound LINS01004 bears the highest affinity for H3R (pKi 6...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29173145/histamine-h3-receptor-ligands-in-the-group-of-homo-piperazine-derivatives
#7
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
https://www.readbyqxmd.com/read/29170631/histamine-h3-heteroreceptors-suppress-glutamatergic-and-gabaergic-synaptic-transmission-in-the-rat-insular-cortex
#8
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
https://www.readbyqxmd.com/read/29162484/differential-homologous-desensitization-of-the-human-histamine-h3-receptors-of-445-and-365-amino-acids-expressed-in-cho-k1-cells
#9
Ana-Maricela García-Gálvez, Juan Escamilla-Sánchez, Catalina Flores-Maldonado, Rubén-Gerardo Contreras, Juan-Manuel Arias, José-Antonio Arias-Montaño
Histamine H3 receptors (H3Rs) signal through Gαi/o proteins and are found in neuronal cells as auto- and hetero-receptors. Alternative splicing of the human H3R (hH3R) originates 20 isoforms, and the mRNAs of two receptors of 445 and 365 amino acids (hH3R445 and hH3R365) are widely expressed in the human brain. We previously showed that the hH3R445 stably expressed in CHO-K1 cells experiences homologous desensitization. The hH3R365 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 hH3R445...
November 18, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/29161255/neurogenic-mediators-contribute-to-local-edema-induced-by-micrurus-lemniscatus-venom
#10
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 21, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29132544/histaminergic-receptors-modulate-spinal-cord-injury-induced-neuronal-nitric-oxide-synthase-upregulation-and-cord-pathology-new-roles-of-nanowired-drug-delivery-for-neuroprotection
#11
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
https://www.readbyqxmd.com/read/29075190/the-histamine-h3-receptor-antagonist-e159-reverses-memory-deficits-induced-by-dizocilpine-in-passive-avoidance-and-novel-object-recognition-paradigm-in-rats
#12
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
https://www.readbyqxmd.com/read/29067314/sar110894-a-potent-histamine-h3-receptor-antagonist-displays-disease-modifying-activity-in-a-transgenic-mouse-model-of-tauopathy
#13
Philippe Delay-Goyet, Véronique Blanchard, Nathalie Schussler, Mati Lopez-Grancha, Jean Ménager, Véronique Mary, Eric Sultan, Armelle Buzy, Jean-Claude Guillemot, Jeanne Stemmelin, Philippe Bertrand, Thomas Rooney, Laurent Pradier, Pascal Barnéoud
INTRODUCTION: Tau hyperphosphorylation and neurofibrillary tangles are histopathologic hallmarks of tauopathies. Histamine H3-receptor antagonists have been proposed to reduce tau hyperphosphorylation in preclinical models. METHODS: We evaluated the ability of SAR110894, a selective histamine H3-receptor antagonist, to inhibit tau pathology and prevent cognitive deficits in a tau transgenic mouse model (THY-Tau22). RESULTS: SAR110894 treatment for 6 months (but not 2 weeks) in THY-Tau22 mice decreased both tau hyperphosphorylation at pSer396-pSer404 (AD2 signal) in the hippocampus and the number of AT8 (pSer199/202-Thr205) positive cells in the cortex and decreased the formation of neurofibrillary tangles in the cortex, hippocampus, and amygdala...
November 2016: Alzheimer's & Dementia: Translational Research & Clinical Interventions
https://www.readbyqxmd.com/read/29044927/knock-out-of-histamine-receptor-h3-alters-adaptation-to-sudden-darkness-and-monoamine-levels-in-the-zebrafish
#14
Henri A J Puttonen, Maria Sundvik, Svetlana Semenova, Yukako Shirai, Yu-Chia Chen, Pertti Panula
AIM: Histamine receptor H3 has substantial neuropharmacological potential. Currently, knock-out models of this receptor have been investigated only in mice. We characterized the expression of this receptor in the zebrafish and generated a zebrafish histamine receptor H3 knock-out line. Using this model, we studied the role of histamine receptor H3 in important behaviours. We also analyzed the effect of histamine receptor H3 knock-out on monoaminergic systems, which has not been thoroughly studied in any animal model...
October 16, 2017: Acta Physiologica
https://www.readbyqxmd.com/read/28982153/hybrid-approach-to-structure-modeling-of-the-histamine-h3-receptor-multi-level-assessment-as-a-tool-for-model-verification
#15
Jakub Jończyk, Barbara Malawska, Marek Bajda
The crucial role of G-protein coupled receptors and the significant achievements associated with a better understanding of the spatial structure of known receptors in this family encouraged us to undertake a study on the histamine H3 receptor, whose crystal structure is still unresolved. The latest literature data and availability of different software enabled us to build homology models of higher accuracy than previously published ones. The new models are expected to be closer to crystal structures; and therefore, they are much more helpful in the design of potential ligands...
2017: PloS One
https://www.readbyqxmd.com/read/28964277/expression-and-localization-of-histamine-h1-h2-and-h3-receptors-in-rat-olfactory-epithelium
#16
Chao Yu, Li Li, Qingjie Xia, Yuedi Tang
OBJECTIVE: Histamine is an important chemical mediator in the development of allergic rhinitis and plays a key role in eliciting the nasal symptoms of the disorder. Histamine may also affect smell as a neurotransmitter. However, whether histamine receptors are present in the mammalian olfactory epithelium has not yet been examined. The aim of this study was to investigate the expression and distribution of histamine H1, H2, and H3 receptors in rat olfactory epithelium. METHODS: Real-time quantitative PCR and immunohistochemical staining were performed to examine the mRNA level and protein expression and localization of histamine receptors (H1, H2, and H3) in rat olfactory epithelium...
October 2017: International Journal of Pediatric Otorhinolaryngology
https://www.readbyqxmd.com/read/28939039/hyperosmolarity-evokes-histamine-release-from-ileum-mucosa-by-stimulating-a-cholinergic-pathway
#17
Banqin Wang, Ning An, Abdul Sami Shaikh, Haoyi Wang, Ling Xiao, Hongwei Liu, Jingxin Li, Dongbo Zhao
Changes in extracellular osmolarity lead to alteration in cellular volume. In the study, we examined the effects of hyperosmolarity on short-circuit currents (Isc) in the rat ileum using the Ussing chamber technique. Mucosal exposure to 20 mM glucose evoked a decrease of ISC in the rat ileum, which was antagonized by the stretch-activated channel blocker GdCl3, TTX and atropine, respectively. In contrast, it was not blocked by phlorizin, a Na(+)-glucose cotransporter SGLT1 inhibitor. Furthermore, the unabsorbed substances, such as sucrose, lactulose or urea, also induced a decrease of ISC in rat ileum...
November 18, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28888822/discovery-of-novel-steroidal-histamine-h3-receptor-antagonists-inverse-agonists
#18
Istvan Ledneczki, Pál Tapolcsányi, Eszter Gábor, János Éles, István Greiner, Éva Schmidt, Zsolt Némethy, Rita Soukupné Kedves, Ottilia Balázs, Viktor Román, György Lévay, Sándor Mahó
Emerging from an HTS campaign, novel steroid-based histamine H3 receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in compound 4 as lead molecule. During the lead optimization due to the versatile modifications of diamino steroid derivatives, several in vitro potent compounds with subnanomolar binding affinities to histamine H3 receptors were found. The unfavorable binding to rat muscarinic receptors was successfully reduced by tuning the basicity...
October 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28886461/time-dependent-effects-of-olanzapine-treatment-on-the-expression-of-histidine-decarboxylase-h1-and-h3-receptor-in-the-rat-brain-the-roles-in-olanzapine-induced-obesity
#19
Meng He, Qingsheng Zhang, Chao Deng, Tiantian Jin, Xueqin Song, Hongqing Wang, Xu-Feng Huang
Antipsychotic treatment, particularly olanzapine and clozapine, induces severe obesity. The Histamine H1 receptor is considered to be an important contributor to olanzapine-induced obesity, however how olanzapine modulates the histaminergic system is not sufficiently understood. This study examined the effect of olanzapine on key molecules of the histaminergic system, including histidine decarboxylase (HDC), H1 receptor (H1R) and H3 receptor (H3R), in the brain at different stages of olanzapine-induced obesity...
August 24, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28877402/effects-of-s-38093-an-antagonist-inverse-agonist-of-histamine-h3-receptors-in-models-of-neuropathic-pain-in-rats
#20
T Chaumette, E Chapuy, E Berrocoso, M Llorca-Torralba, L Bravo, J A Mico, M Chalus, A Eschalier, D Ardid, F Marchand, A Sors
BACKGROUND: Histamine H3 receptors are mainly expressed on CNS neurons, particularly along the nociceptive pathways. The potential involvement of these receptors in pain processing has been suggested using H3 receptor inverse agonists. METHODS: The antinociceptive effect of S 38093, a novel inverse agonist of H3 receptors, has been evaluated in several neuropathic pain models in rat and compared with those of gabapentin and pregabalin. RESULTS: While S 38093 did not change vocalization thresholds to paw pressure in healthy rats, it exhibited a significant antihyperalgesic effect in the Streptozocin-induced diabetic (STZ) neuropathy model after acute and chronic administration and, in the chronic constriction injury (CCI) model only after chronic administration, submitted to the paw-pressure test...
September 6, 2017: European Journal of Pain: EJP
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