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Histamine H3

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https://www.readbyqxmd.com/read/28888822/discovery-of-novel-steroidal-histamine-h3-receptor-antagonists-inverse-agonists
#1
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...
September 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
#2
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
#3
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
#4
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
#5
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
#6
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...
September 1, 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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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