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Histamine H3

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https://www.readbyqxmd.com/read/28797771/biphenyloxy-alkyl-piperidine-and-azepane-derivatives-as-histamine-h3-receptor-ligands
#1
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...
July 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28777172/narcolepsy-and-other-central-hypersomnias
#2
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
#3
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
#4
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
https://www.readbyqxmd.com/read/28626527/systematic-data-mining-reveals-synergistic-h3r-mchr1-ligands
#5
David Schaller, Stefanie Hagenow, Gina Alpert, Alexandra Naß, Robert Schulz, Marcel Bermudez, Holger Stark, Gerhard Wolber
In this study, we report a ligand-centric data mining approach that guided the identification of suitable target profiles for treating obesity. The newly developed method is based on identifying target pairs for synergistic positive effects and also encompasses the exclusion of compounds showing a detrimental effect on obesity treatment (off-targets). Ligands with known activity against obesity-relevant targets were compared using fingerprint representations. Similar compounds with activities to different targets were evaluated for the mechanism of action since activation or deactivation of drug targets determines the pharmacological effect...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28564538/mechanism-of-off-target-interactions-and-toxicity-of-tamoxifen-and-its-metabolites
#6
Maria Flynn, Kali Amelia Heale, Laleh Alisaraie
Tamoxifen is an estrogen modulator that acts to competitively inhibit the binding of endogenous estrogens. It is widely used for treatment of breast cancer; however, analogous with many antineoplastic agents, tamoxifen is associated with numerous adverse effects, most prominently nausea. We have identified several off-target receptors of tamoxifen and 22 of its metabolites that include histamine H1 and H3, and muscarinic M1, M4, and M5 subtypes, and dopamine D2 receptor. We have shown how they are associated with tamoxifen and its metabolites' toxicity through a comprehensive computational analysis of their interaction modes, which were also compared to that of the related endogenous substrates of each receptor...
June 14, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28526411/jnj10181457-a-histamine-h3-receptor-inverse-agonist-regulates-in%C3%A2-vivo-microglial-functions-and-improves-depression-like-behaviours-in-mice
#7
Tomomitsu Iida, Takeo Yoshikawa, Anikó Kárpáti, Takuro Matsuzawa, Haruna Kitano, Asuka Mogi, Ryuichi Harada, Fumito Naganuma, Tadaho Nakamura, Kazuhiko Yanai
Brain histamine acts as a neurotransmitter and regulates various physiological functions, such as learning and memory, sleep-wake cycles, and appetite regulation. We have recently shown that histamine H3 receptor (H3R) is expressed in primary mouse microglia and has a strong influence on critical functions in microglia, including chemotaxis, phagocytosis, and cytokine secretion in vitro. However, the importance of H3R in microglial activity in vivo remains unknown. Here, we examined the effects of JNJ10181457 (JNJ), a selective and potent H3R inverse agonist, on microglial functions ex vivo and in vivo...
May 16, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28501482/ciproxifan-improves-cholinergic-transmission-attenuates-neuroinflammation-and-oxidative-stress-but-does-not-reduce-amyloid-level-in-transgenic-mice
#8
Vasudevan Mani, Siti Murnirah Jaafar, Nur Syamimi Mohd Azahan, Kalavathy Ramasamy, Siong Meng Lim, Long Chiau Ming, Abu Bakar Abdul Majeed
AIM: The present study is aimed to investigate the ability of ciproxifan, a histamine H3 receptor antagonist to inhibit β-amyloid (Aβ)-induced neurotoxicity in SK-N-SH cells and APP transgenic mouse model. MATERIALS AND METHODS: In vitro studies was designed to evaluate the neuroprotective effects of ciproxifan in Aβ25-35 - induced SK-N-SH cells. For the in vivo study, ciproxifan (1 and 3mg/kg, i.p.) was administrated to transgenic mice for 15days and behaviour was assessed using the radial arm maze (RAM)...
July 1, 2017: Life Sciences
https://www.readbyqxmd.com/read/28465562/activation-of-the-ileal-neuroendocrine-tumor-cell-line-p-sts-by-acetylcholine-is-amplified-by-histamine-role-of-h3r-and-h4r
#9
Beatrix Pfanzagl, Diana Mechtcheriakova, Anastasia Meshcheryakova, Stephan W Aberle, Roswitha Pfragner, Erika Jensen-Jarolim
Neuroendocrine tumors may present with pseudoallergic reactions like diarrhea and idiopathic anaphylaxis. Here we present the P-STS human ileal neuroendocrine cell line as a model cell line for these tumors. Neuroendocrine markers and changes in cytoplasmic calcium concentration ([Ca(2+)]i) in response to several possible activators of 5-hydroxytryptamine (5-HT) release were analyzed. P-STS cells still expressed chromogranin A and synaptophysin after 2 years of culture. Tryptophan hydroxylase 1 mRNA and a low amount of 5-HT were also detected...
May 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28458281/role-of-histamine-releasing-factor-in-allergic-inflammatory-reactions
#10
REVIEW
Jun-Ichi Kashiwakura, Tomoaki Ando, Toshiaki Kawakami
 Mast cells are effector cells in immunoglobulin E (IgE)-mediated immediate hypersensitivity and allergic diseases such as asthma and food allergy. Mast cells are activated by the aggregation of the IgE-bound high-affinity IgE receptor FcεRI with multivalent antigen. Activated mast cells secrete proinflammatory mediators such as histamine, serotonin, and proteases and produce cytokines and chemokines. However, it has been reported that mast cells are activated by crosslinking of FcεRI with monomeric IgE in the absence of antigen...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28449891/the-european-medicines-agency-review-of-pitolisant-for-treatment-of-narcolepsy-summary-of-the-scientific-assessment-by-the-committee-for-medicinal-products-for-human-use
#11
Marta Kollb-Sielecka, Pierre Demolis, Joseph Emmerich, Greg Markey, Tomas Salmonson, Manuel Haas
On 31 March 2016, the European Commission issued a decision for a marketing authorisation valid throughout the European Union (EU) for pitolisant (Wakix) for the treatment of narcolepsy with or without cataplexy in adults. Pitolisant is an antagonist/inverse agonist of the human histamine H3 receptor. The dose should be selected using an up-titration scheme depending on individual patient response and tolerance and should not exceed 36 mg/day. The main evidence of efficacy of pitolisant was based on two Phase III clinical trials...
May 2017: Sleep Medicine
https://www.readbyqxmd.com/read/28438982/the-histaminergic-system-is-involved-in-psychological-stress-induced-hyperthermia-in-rats
#12
Battuvshin Lkhagvasuren, Takakazu Oka
The histaminergic system modulates numerous physiological functions such as wakefulness, circadian rhythm, feeding, and thermoregulation. However, it is not yet known if this system is also involved in psychological stress-induced hyperthermia (PSH) and, if so, which histamine (H) receptor subtype mediates the effect. Therefore, we investigated the effects of pretreatments with intraperitoneal injections of mepyramine (an H1 receptor inverse agonist), cimetidine (an H2 receptor antagonist), and ciproxifan (an H3 receptor inverse agonist) on cage-exchange stress-induced hyperthermia (a model of PSH) by monitoring core body temperature (Tc) during both light (10:00 am-12:00 pm) and dark (10:00 pm-12:00 am) phases in conscious, freely moving rats...
April 2017: Physiological Reports
https://www.readbyqxmd.com/read/28398338/the-histamine-h3-receptor-antagonist-thioperamide-rescues-circadian-rhythm-and-memory-function-in-experimental-parkinsonism
#13
D Masini, C Lopes-Aguiar, A Bonito-Oliva, D Papadia, R Andersson, A Fisahn, G Fisone
Parkinson's disease (PD) is a common neurodegenerative disorder, characterized by motor impairment and a wide range of non-motor symptoms, including sleep disorders and cognitive and affective deficits. In this study, we used a mouse model of PD based on 6-hydroxydopamine (6-OHDA) to examine the effect of thioperamide, a histamine H3 receptor antagonist, on circadian activity, recognition memory and anxiety. A partial, bilateral 6-OHDA lesion of the striatum reduces motor activity during the active phase of the 24 h cycle...
April 11, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28372935/synthesis-and-biological-activity-of-novel-tert-amylphenoxyalkyl-homo-piperidine-derivatives-as-histamine-h3r-ligands
#14
Kamil J Kuder, Dorota Łażewska, Maria Kaleta, Gniewomir Latacz, Tim Kottke, Agnieszka Olejarz, Tadeusz Karcz, Andrzej Fruziński, Katarzyna Szczepańska, Janina Karolak-Wojciechowska, Holger Stark, Katarzyna Kieć-Kononowicz
As a continuation of our search for novel histamine H3 receptor ligands a series of twenty new tert-amyl phenoxyalkylamine derivatives (2-21) was synthesized. Compounds of four to eight carbon atoms spacer alkyl chain were evaluated on their binding properties at human histamine H3 receptor (hH3R). The highest affinities were observed for pentyl derivatives 6-8 (Ki=8.8-23.4nM range) and among them piperidine derivative 6 with Ki=8.8nM. Structures 6, 7 were also classified as antagonists in cAMP accumulation assay (with EC50=157 and 164nM, respectively)...
May 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28336400/mechanistic-characterization-of-s-38093-a-novel-inverse-agonist-at-histamine-h3-receptors
#15
Aurore Sors, Fany Panayi, Lionel Bert, Dominique Favale, Olivier Nosjean, Valérie Audinot, Jean-Michel Arrang, Bruno Buisson, Esther Steidl, Jean-Marie Delbos, Tuulia Huhtala, Outi Kontkanen, Anne-Marie Chollet, Patrick Casara, Pierre Lestage
Histaminergic H3 inverse agonists, by stimulating central histamine release, represent attractive drug candidates to treat cognitive disorders. The present studies aimed to describe the mechanistic profile of S 38093 a novel H3 receptors inverse agonist. S 38093 displays a moderate affinity for rat, mouse and human H3 receptors (Ki=8.8, 1.44 and 1.2µM, respectively) with no affinity for other histaminergic receptors. In cellular models, the compound was able to antagonize mice H3 receptors (KB=0.65µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0...
May 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315340/in-vivo-pharmacological-profile-of-s-38093-a-novel-histamine-h3-receptor-inverse-agonist
#16
Fany Panayi, Aurore Sors, Lionel Bert, Brigitte Martin, Gaelle Rollin-Jego, Rodolphe Billiras, Isabelle Carrié, Karine Albinet, Laurence Danober, Nathalie Rogez, Jean-Yves Thomas, Luigi Pira, Valérie Bertaina-Anglade, Pierre Lestage
S 38093, a novel histamine H3 receptor inverse agonist, was tested in a series of neurochemical and behavioral paradigms designed to evaluate its procognitive and arousal properties. In intracerebral microdialysis studies performed in rats, S 38093 dose-dependently increased histamine extracellular levels in the prefrontal cortex and facilitated cholinergic transmission in the prefrontal cortex and hippocampus of rats after acute and chronic administration (10mg/kg i.p.). Acute oral administration of S 38093 at 0...
May 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28218311/s-38093-a-histamine-h3-antagonist-inverse-agonist-promotes-hippocampal-neurogenesis-and-improves-context-discrimination-task-in-aged-mice
#17
Jean-Philippe Guilloux, Benjamin A Samuels, Indira Mendez-David, Alice Hu, Marjorie Levinstein, Charlène Faye, Maryam Mekiri, Elisabeth Mocaer, Alain M Gardier, René Hen, Aurore Sors, Denis J David
Strategies designed to increase adult hippocampal neurogenesis (AHN) may have therapeutic potential for reversing memory impairments. H3 receptor antagonists/inverse agonists also may be useful for treating cognitive deficits. However, it remains unclear whether these ligands have effects on AHN. The present study aimed to investigate the effects of a 28-day treatment with S 38093, a novel brain-penetrant antagonist/inverse agonist of H3 receptors, on AHN (proliferation, maturation and survival) in 3-month-old and in aged 16-month-old mice...
February 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28188663/histamine-facilitates-gabaergic-transmission-in-the-rat-entorhinal-cortex-roles-of-h1-and-h2-receptors-na-permeable-cation-channels-and-inward-rectifier-k-channels
#18
Nicholas I Cilz, Saobo Lei
In the brain, histamine (HA) serves as a neuromodulator and a neurotransmitter released from the tuberomammillary nucleus (TMN). HA is involved in wakefulness, thermoregulation, energy homeostasis, nociception, and learning and memory. The medial entorhinal cortex (MEC) receives inputs from the TMN and expresses HA receptors (H1 , H2 , and H3 ). We investigated the effects of HA on GABAergic transmission in the MEC and found that HA significantly increased the frequency of spontaneous inhibitory postsynaptic currents (sIPSCs) with an EC50 of 1...
May 2017: Hippocampus
https://www.readbyqxmd.com/read/28168839/histamine-h3-receptor-antagonist-prevents-memory-deficits-and-synaptic-plasticity-disruption-following-isoflurane-exposure
#19
Tao Luo, Ying Wang, Jian Qin, Zhi-Gang Liu, Min Liu
BACKGROUND: Exposure to pharmacological concentration of inhaled anesthetics such as isoflurane can cause short- or long-term cognitive impairments in preclinical studies. The selective antagonists of the histamine H3 receptors are considered as a promising group of novel therapeutic agents for the treatment of cognitive disorders. In this study, we investigated whether ciproxifan, a nonimidazole antagonist of H3 histamine receptors, could overcome the functional and electrophysiological sequela associated with isoflurane anesthesia...
February 6, 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/28137965/correction-to-isoform-specific-biased-agonism-of-histamine-h3-receptor-agonists
#20
(no author information available yet)
No abstract text is available yet for this article.
March 2017: Molecular Pharmacology
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