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Histamine H3

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
https://www.readbyqxmd.com/read/28863002/histamine-h3-receptor-antagonists-ameliorate-attention-deficit-hyperactivity-disorder-like-behavioral-changes-caused-by-neonatal-habenula-lesion
#11
Yu-Jeong Kim, Yukiori Goto, Young-A Lee
A partial agonist and a full antagonist of the histamine H3 receptor have been suggested to have therapeutic effects on cognitive deficits in psychiatric disorders. We have previously shown that neonatal habenula lesion (NHL) induces behavioral deficits that resemble the symptoms of attention deficit/hyperactivity disorder (ADHD). In this study, we examined the effects of three H3 antagonists on ADHD-like behavioral changes caused by NHL in rats. Behavioral tests and administration of the H3 receptor antagonists were performed in juvenile rats with NHL...
August 31, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28862769/histamine-and-migraine
#12
Hsiangkuo Yuan, Stephen D Silberstein
BACKGROUND: Histamine is an ancient "tissue amine" preceding multicellular organisms. In the central nervous system (CNS), its fibers originate solely from the tuberomammillary nucleus and travel throughout the brain. It is mainly responsible for wakefulness, energy homeostasis, and memory consolidation. Recently, several studies suggest a potential role of histamine in migraine pathogenesis and management. METHODS: Narrative review of current literature regarding histamine and migraine...
September 1, 2017: Headache
https://www.readbyqxmd.com/read/28861918/multitarget-directed-ligands-combining-cholinesterase-and-monoamine-oxidase-inhibition-with-histamine-h3-r-antagonism-for-neurodegenerative-diseases
#13
Óscar M Bautista-Aguilera, Stefanie Hagenow, Alejandra Palomino-Antolin, Víctor Farré-Alins, Lhassane Ismaili, Pierre-Louis Joffrin, María L Jimeno, Ondřej Soukup, Jana Janočková, Lena Kalinowsky, Ewgenij Proschak, Isabel Iriepa, Ignacio Moraleda, Johannes S Schwed, Alejandro Romero Martínez, Francisco López-Muñoz, Mourad Chioua, Javier Egea, Rona R Ramsay, José Marco-Contelles, Holger Stark
The therapy of complex neurodegenerative diseases requires the development of multitarget-directed drugs (MTDs). Novel indole derivatives with inhibitory activity towards acetyl/butyrylcholinesterases and monoamine oxidases A/B as well as the histamine H3 receptor (H3R) were obtained by optimization of the neuroprotectant ASS234 by incorporating generally accepted H3R pharmacophore motifs. These small-molecule hits demonstrated balanced activities at the targets, mostly in the nanomolar concentration range...
October 2, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28861757/histamine-h3-inverse-agonist-bf-2649-or-antagonist-with-partial-h4-agonist-activity-clobenpropit-reduces-amyloid-beta-peptide-induced-brain-pathology-in-alzheimer-s-disease
#14
Ranjana Patnaik, Aruna Sharma, Stephen D Skaper, Dafin F Muresanu, José Vicente Lafuente, Rudy J Castellani, Ala Nozari, Hari S Sharma
Alzheimer's disease (AD) is one of the leading causes for disability and death affecting millions of people worldwide. Thus, novel therapeutic strategies are needed to reduce brain pathology associated with AD. In view of increasing awareness regarding involvement of histaminergic pathways in AD, we explored the role of one H3 receptor inverse agonist BF 2649 and one selective H3 receptor antagonist with partial H4 agonist activity in amyloid beta peptide (AβP) infusion-induced brain pathology in a rat model...
August 31, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28838882/histamine-regulates-memory-consolidation
#15
REVIEW
Maria Beatrice Passani, Fernando Benetti, Patrizio Blandina, Cristiane R G Furini, Jociane de Carvalho Myskiw, Ivan Izquierdo
Recent findings have reasserted the role of histamine in the regulation of memory consolidation first proposed in 1986 in an inhibitory avoidance task in rats. They indicate that histamine is indeed a major regulator of memory consolidation in various tasks, through H2 receptors in the dorsal hippocampus and through H3 receptors in the basolateral amygdala, depending on the task. In the object recognition task, the memory enhancing effect is mediated by the three receptors (H1, H2, H3) in the dorsal hippocampus...
August 23, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28820054/qsar-modeling-of-histamine-h3r-antagonists-inverse-agonists-as-future-drugs-for-neurodegenerative-diseases
#16
Michelle Fidelis Corrêa, João Paulo Dos Santos Fernandes
Histamine H3 receptor (H3R) is associated with several neuropsychological diseases. It is predominantly expressed in the central nervous system as presynaptic receptor, especially in regions associated with cognition and behavior, and is responsible for modulate the synthesis and release of histamine and other neurotransmitters such as acetylcholine, dopamine and serotonin. Therefore, H3R is an important target involved in several CNS disorders, such as narcolepsy, attention deficit hyperactivity disorder and schizophrenia...
August 17, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28797771/biphenyloxy-alkyl-piperidine-and-azepane-derivatives-as-histamine-h3-receptor-ligands
#17
Dorota Łażewska, Maria Kaleta, J Stephan Schwed, Tadeusz Karcz, Szczepan Mogilski, Gniewomir Latacz, Agnieszka Olejarz, Agata Siwek, Monika Kubacka, Annamaria Lubelska, Ewelina Honkisz, Jadwiga Handzlik, Barbara Filipek, Holger Stark, Katarzyna Kieć-Kononowicz
Novel biphenyloxy-alkyl derivatives of piperidine and azepane were synthesized and evaluated for their binding properties at the human histamine H3 receptor. Two series of compounds were obtained with a meta- and a para-biphenyl moiety. The alkyl chain spacer contained five and six carbon atoms. The highest affinity among all compounds was shown by 1-(6-(3-phenylphenoxy)hexyl)azepane (13) with a Ki value of 18nM. Two para-biphenyl derivatives, 1-(5-(4-phenylphenoxy)pentyl)piperidine (14; Ki=25nM) and 1-(5-(4-phenylphenoxy)pentyl)azepane (16; Ki=34nM), classified as antagonists in a cAMP accumulation assay (IC50=4 and 9nM, respectively), were studied in detail...
October 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28777172/narcolepsy-and-other-central-hypersomnias
#18
Yves Dauvilliers, Lucie Barateau
PURPOSE OF REVIEW: This article focuses on the clinical presentation, pathophysiology, diagnosis, differential diagnosis, and management of narcolepsy type 1 and narcolepsy type 2, idiopathic hypersomnia, Kleine-Levin syndrome, and other central disorders of hypersomnolence, as defined in the International Classification of Sleep Disorders, Third Edition (ICSD-3). RECENT FINDINGS: In ICSD-3, the names of some central disorders of hypersomnolence have been changed: narcolepsy with cataplexy and narcolepsy without cataplexy have been renamed narcolepsy type 1 and narcolepsy type 2, respectively...
August 2017: Continuum: Lifelong Learning in Neurology
https://www.readbyqxmd.com/read/28745208/thiazole-containing-heterocycles-with-cns-activity
#19
Priyanka Kalal, Divyani Gandhi, Prakash Prajapat, Shikha Agarwal
BACKGROUND: Thiazoles are promising scaffolds in the area of medicinal and pharmaceutical chemistry and have accounted to show different pharmacophoric properties. For the last years, thiazole derivatives have focused too much attention to develop different new CNS active agents. It has been broadly used to generate diverse therapeutic agents against various CNS targets. Histamine H3 receptors are seriously involved in the pathophysiology of numerous disorders of the central nervous system...
July 24, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28684785/identification-of-histamine-h3-receptor-ligands-using-a-new-crystal-structure-fragment-based-method
#20
Ida Osborn Frandsen, Michael W Boesgaard, Kimberley Fidom, Alexander S Hauser, Vignir Isberg, Hans Bräuner-Osborne, Petrine Wellendorph, David E Gloriam
Virtual screening offers an efficient alternative to high-throughput screening in the identification of pharmacological tools and lead compounds. Virtual screening is typically based on the matching of target structures or ligand pharmacophores to commercial or in-house compound catalogues. This study provides the first proof-of-concept for our recently reported method where pharmacophores are instead constructed based on the inference of residue-ligand fragments from crystal structures. We demonstrate its unique utility for G protein-coupled receptors, which represent the largest families of human membrane proteins and drug targets...
July 6, 2017: Scientific Reports
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