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Histamine H3

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https://www.readbyqxmd.com/read/27902931/human-presynaptic-receptors
#1
REVIEW
Eberhard Schlicker, Thomas Feuerstein
Presynaptic receptors are sites at which transmitters, locally formed mediators or hormones inhibit or facilitate the release of a given transmitter from its axon terminals. The interest in the identification of presynaptic receptors has faded in recent years and it may therefore be justified to give an overview of their occurrence in the autonomic and central nervous system; this review will focus on presynaptic receptors in human tissues. Autoreceptors are presynaptic receptors at which a given transmitter restrains its further release, though in some instances may also increase its release...
November 27, 2016: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27888416/lesion-remyelinating-activity-of-gsk239512-versus-placebo-in-patients-with-relapsing-remitting-multiple-sclerosis-a-randomised-single-blind-phase-ii-study
#2
Caryl J Schwartzbach, Richard A Grove, Robert Brown, Debra Tompson, Florian Then Bergh, Douglas L Arnold
Histamine H3 receptor blockade may enhance lesion remyelination in multiple sclerosis (MS). The efficacy (using a magnetic resonance imaging marker of myelination, magnetisation transfer ratio [MTR]), safety and pharmacokinetics of GSK239512, a potent and brain penetrant H3 receptor antagonist/inverse agonist on lesion remyelination in relapsing-remitting MS (RRMS) were assessed. This was a phase II, randomised, parallel-group, placebo-controlled, double-blind (sponsor-unblinded), international, multicentre study (NCT01772199)...
November 25, 2016: Journal of Neurology
https://www.readbyqxmd.com/read/27866818/the-discovery-of-quinoline-based-single-ligand-human-h1-and-h3-receptor-antagonists
#3
Panayiotis A Procopiou, Rachael A Ancliff, Paul M Gore, Ashley P Hancock, Simon T Hodgson, Duncan S Holmes, Steven P Keeling, Brian E Looker, Nigel A Parr, James E Rowedder, Robert J Slack
A novel series of potent quinoline-based human H1 and H3 bivalent histamine receptor antagonists, suitable for intranasal administration for the potential treatment of allergic rhinitis associated nasal congestion, were identified. Compound 18b had slightly lower H1 potency (pA2 8.8 vs 9.7 for the clinical goldstandard azelastine), and H3 potency (pKi 9.1vs 6.8 for azelastine), better selectivity over α1A, α1B and hERG, similar duration of action, making 18b a good back-up compound to our previous candidate, but with a more desirable profile...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27864425/isoform-specific-biased-agonism-of-histamine-h3-receptor-agonists
#4
Darren M Riddy, Anna Cook, Natalie A Diepenhorst, Sanja Bosnyak, Ryan Brady, Clotilde Mannoury-la-Cour, Elisabeth Mocaer, Roger J Summers, William Charman, Patrick M Sexton, Arthur Christopoulos, Christopher J Langmead
The human histamine H3 receptor (hH3R) is subject to extensive gene splicing that gives rise to a large number of functional and non-functional isoforms. Despite the general acceptance that G protein-coupled receptors can adopt different ligand-induced conformations that give rise to biased signalling, this has not been studied for the H3R; further, it has unknown whether splice variants of the same receptor engender the same or differential biased signalling. Herein we have profiled the pharmacology of histamine receptor agonists at the two most abundant hH3R splice variants (hH3R445 and hH3R365) across seven signalling endpoints...
November 18, 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27863547/identification-of-histamine-receptors-in-the-canine-gastrointestinal-tract
#5
Alyssa Sullivant, Andrew Mackin, Todd Pharr, Jim Cooley, Robert Wills, Todd Archer
The important role of histamine in chronic gastrointestinal diseases has been increasingly recognized over the last two decades in human medicine. Histamine is released following mast cell activation and exerts its action through binding to four different histamine receptors (H1, H2, H3, and H4). Histamine receptors are dispersed throughout the body, and each different receptor mediates a unique response. Documentation of the presence and type of histamine receptors in the differing sections of the canine gastrointestinal tract will provide additional research opportunities to further explore the role of histamine and its receptors in chronic canine enteropathies, as well as potential therapeutic options...
December 2016: Veterinary Immunology and Immunopathology
https://www.readbyqxmd.com/read/27855565/impact-of-histamine-receptors-h1-and-h3-polymorphisms-on-antipsychotic-induced-weight-gain
#6
Arun K Tiwari, Danning Zhang, Jennie G Pouget, Clement C Zai, Nabilah I Chowdhury, Eva J Brandl, Li Qin, Natalie Freeman, Jeffrey A Lieberman, Herbert Y Meltzer, James L Kennedy, Daniel J Müller
OBJECTIVES: A positive correlation between antipsychotic-induced weight gain (AIWG) and antipsychotic drugs' antagonist effect at histamine H1 receptor (HRH1) as well as agonist effect at histamine H3 receptor (HRH3) in the brain has been consistently demonstrated. We investigated the potential impact of single-nucleotide polymorphisms (SNPs) in HRH1 and HRH3 genes on AIWG. METHODS: We analysed 40 tagSNPs in HRH1 (n = 34) and HRH3 (n = 6) in schizophrenia/schizoaffective disorder patients (n = 193) primarily treated with clozapine or olanzapine for up to 14 weeks...
November 18, 2016: World Journal of Biological Psychiatry
https://www.readbyqxmd.com/read/27853355/anticonvulsant-effects-of-isomeric-nonimidazole-histamine-h3-receptor-antagonists
#7
Bassem Sadek, Ali Saad, Johannes Stephan Schwed, Lilia Weizel, Miriam Walter, Holger Stark
Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands targeting central histamine H3 receptors (H3Rs) for epilepsy might be a promising therapeutic approach. To determine the potential of H3Rs ligands as new AEDs, we recently reported that no anticonvulsant effects were observed for the (S)-2-(4-(3-(piperidin-1-yl)propoxy)benzylamino)propanamide (1)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#8
REVIEW
Danish Mahmood
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain. H3 antagonism may be a novel approach to develop a new class of antipsychotic medications given the gathering evidence reporting therapeutic efficacy in several central nervous system disorders. Several medications such as cariprazine, lurasidone, LY214002, bexarotene, rasagiline, raloxifene, BL-1020 and ITI-070 are being developed to treat the negative symptoms and cognitive impairments of schizophrenia...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27825384/inhibiting-the-proton-pump-mechanisms-benefits-harms-and-questions
#9
Jeffrey K Aronson
Inhibition of the H(+)/K(+)-adenosine triphosphatase (the proton pump) is the final common mechanistic pathway in reducing gastric acid secretion pharmacologically. Proton pump inhibitors are widely used in upper gastrointestinal diseases, including gastric and duodenal ulcers, eradication of Helicobacter pylori in combination with antibiotics, gastroesophageal reflux disease, Zollinger-Ellison syndrome, eosinophilic esophagitis, and prevention of non-steroidal anti-inflammatory drug-induced peptic ulceration...
November 9, 2016: BMC Medicine
https://www.readbyqxmd.com/read/27787717/role-of-the-histamine-h3-receptor-in-the-central-nervous-system
#10
Eberhard Schlicker, Markus Kathmann
The Gi/o protein-coupled histamine H3 receptor is distributed throughout the central nervous system including areas like cerebral cortex, hippocampus and striatum with the density being highest in the posterior hypothalamus, i.e. the area in which the histaminergic cell bodies are located. In contrast to the other histamine receptor subtypes (H1, H2 and H4), the H3 receptor is located presynaptically and shows a constitutive activity. In detail, H3 receptors are involved in the inhibition of histamine release (presynaptic autoreceptor), impulse flow along the histaminergic neurones (somadendritic autoreceptor) and histamine synthesis...
October 28, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27773822/histamine-h3-receptor-antagonist-oup-186-attenuates-the-proliferation-of-cultured-human-breast-cancer-cell-lines
#11
Satoshi Tanaka, Minoru Sakaguchi, Hiroki Yoneyama, Yoshihide Usami, Shinya Harusawa
Histamine is involved in various physiological functions, including its neurotransmitter actions in the central nervous system and its action as a causative agent of inflammation, allergic reactions, and gastric acid secretions. Histamine expression and biosynthesis have been detected in breast cancer cells. It was recently suggested that the histamine H3 receptor (H3R) plays a role in the proliferation of breast cancer cells. We recently developed the non-imidazole H3R antagonist OUP-186 which exhibited a potent and selective human H3R antagonistic activity as well as no activity against the human histamine H4 receptor (H4R)...
October 21, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27744004/histamine-h3-receptor-activation-stimulates-calcium-mobilization-in-a-subpopulation-of-rat-striatal-neurons-in-primary-culture-but-not-in-synaptosomes
#12
Nayeli Rivera-Ramírez, Wilber Montejo-López, María-Cristina López-Méndez, Agustín Guerrero-Hernández, Anayansi Molina-Hernández, Ubaldo García-Hernández, José-Antonio Arias-Montaño
The histamine H3 receptor (H3R) is abundantly expressed in the Central Nervous System where it regulates several functions pre and postsynaptically. H3Rs couple to Gαi/o proteins and trigger or modulate several intracellular signaling pathways, including the cAMP/PKA pathway and the opening of N- and P/Q-type voltage-gated Ca(2+) channels. In transfected cells, activation of the human H3R of 445 amino acids (hH3R445) results in phospholipase C (PLC) stimulation and release of Ca(2+) from intracellular stores...
December 2016: Neurochemistry International
https://www.readbyqxmd.com/read/27704986/structure-based-discovery-and-binding-site-analysis-of-histamine-receptor-ligands
#13
Róbert Kiss, György M Keserű
The application of structure-based drug discovery in histamine receptor projects was previously hampered by the lack of experimental structures. The publication of the first X-ray structure of the histamine H1 receptor has been followed by several successful virtual screens and binding site analysis studies of H1-antihistamines. This structure together with several other recently solved aminergic G-protein coupled receptors (GPCRs) enabled the development of more realistic homology models for H2, H3 and H4 receptors...
October 5, 2016: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/27693797/the-role-of-histamine-h1-h2-and-h3-receptors-of-ventral-posteromedial-nucleus-of-thalamus-in-modulation-of-trigeminal-pain
#14
Esmaeal Tamaddonfard, Amir Erfanparast, Hamid Ghasemi, Farzin Henareh-Chareh, Mansoor Hadidi, Navideh Mirzakhani, Sahar Seyedin, Mina Taati, Reza Salighedar, Sara Salimi, Farshad Safaei
Histamine receptors are involved in supraspinal modulation of pain. In the present study, we investigated the effects of microinjection of histamine H1, H2 and H3 receptor antagonists and agonists into the ventral posteromedial (VPM) nucleus of the thalamus on two models of trigeminal pain. Right and left sides of VPM were implanted with two guide cannulas. Corneal pain was induced by local corneal surface application of hypertonic saline and the number of eye wipes was recorded. The duration of face rubbing, as an orofacial pain measure, was recorded after subcutaneous (s...
September 29, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27592826/efficient-approaches-to-s-alkyl-n-alkylisothioureas-and-application-to-novel-histamine-h3r-antagonists
#15
Hiroki Yoneyama, Daisuke Yamamoto, Atsushi Yamatodani, Shinya Harusawa
S-Alkyl-N-alkylisothiourea compounds, which contain various cyclic amines, were synthesized using 3-phenylpropionyl isothiocyanate (PPI) to discover novel non-imidazole histamine H3 receptor (H3R) antagonists. The synthetic route was improved remarkably by using 2-nitrophenylacetyl isothiocyanate (NPAI). Among the synthesized compounds, N-[4-(4-chlorophenyl)butyl]-S-[3-piperidin-1-yl)propyl]isothiourea (1k, OUP-186) exhibited potent and selective antagonism against human H3R but not human H4R, in vitro. Of particular interest, they did not show antagonism for the histamine release in rat brain microdialysis in vivo, suggesting species-selective differences in antagonist affinities...
2016: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/27592250/ligand-autoradiographical-quantification-of-histamine-h3-receptor-in-human-dementia-with-lewy-bodies
#16
Natasha L Lethbridge, Paul L Chazot
Dementia with Lewy bodies (DLB) is a serious age-dependent human neurodegenerative disease, with multiple debilitating symptoms, including dementia, psychosis and significant motor deficits, but with little or no effective treatments. This comparative ligand autoradiographical study has quantified histamine H3 receptors (H3R) in a series of major cortical and basal ganglia structures in human DLB and Alzheimer's (AD) post-mortem cases using the highly selective radioligand, [(3)H] GSK189254. In the main, the levels of H3 receptor were largely preserved in DLB cases when compared with aged-matched controls...
August 31, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27580212/radiosynthesis-and-quality-control-of-11-c-tasp457-as-a-clinically-useful-pet-ligand-for-imaging-of-histamine-h3-receptors-in-human-brain
#17
Masayuki Hanyu, Kazunori Kawamura, Makoto Takei, Kenji Furutsuka, Satoshi Shiomi, Tomoya Fujishiro, Masanao Ogawa, Nobuki Nengaki, Hiroki Hashimoto, Toshimitsu Fukumura, Ming-Rong Zhang
INTRODUCTION: Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]-1-(6-[(11)C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([(11)C]TASP457, [(11)C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [(11)C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [(11)C]2 for qualifying H3 receptors in human brain. In this paper, we report an efficient radiosynthesis of [(11)C]2 to obtain sufficient radioactivity and high quality for clinical application...
August 10, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27568835/action-of-pitolisant-on-the-stimulant-and-rewarding-effects-of-cocaine-in-mice
#18
Christian Brabant, Yana Charlier, Maria Elisa Serrano Navacerrada, Livia Alleva, Ezio Tirelli
Previous studies have demonstrated that the histamine H3 receptor inverse agonist thioperamide potentiates the stimulant and rewarding effects of cocaine. However, these potentiating effects of thioperamide do not necessarily result from H3 receptor blockade since thioperamide is an imidazole-based compound capable of enhancing plasma cocaine concentrations by blocking cytochrome P450 activity. In contrast, Pitolisant is a non-imidazole H3 receptor inverse agonist that has already been tested in clinical trials but it remains to be determined whether this compound also potentiates the behavioral effects of cocaine...
August 26, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27568232/the-dual-acting-ache-inhibitor-and-h3-receptor-antagonist-uw-md-72-reverses-amnesia-induced-by-scopolamine-or-dizocilpine-in-passive-avoidance-paradigm-in-rats
#19
Bassem Sadek, Nadia Khan, Fouad H Darras, Steffen Pockes, Michael Decker
Both the acetylcholine esterase (AChE) and the histamine H3 receptor (H3R) are involved in the metabolism and modulation of acetylcholine release and numerous other centrally acting neurotransmitters. Hence, dual-active AChE inhibitors (AChEIs) and H3R antagonists hold potential to treat cognitive disorders like Alzheimer's disease (AD). The novel dual-acting AChEI and H3R antagonist 7-(3-(piperidin-1-yl)propoxy)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one (UW-MD-72) shows excellent selectivity profiles over the AChE's isoenzyme butyrylcholinesterase (BChE) as well as high and balanced in-vitro affinities at both AChE and hH3R with IC50 of 5...
October 15, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27567703/involvement-of-mast-cells-and-histamine-in-edema-induced-in-mice-by-scolopendra-viridicornis-centipede-venom
#20
Bianca C L F Távora, Louise F Kimura, Marta M Antoniazzi, Thiago M Chiariello, Eliana L Faquim-Mauro, Katia C Barbaro
Bites caused by Scolopendra viridicornis centipede are mainly characterized by burning pain, paresthesia and edema. On this regard, the aim of this work was to study the involvement of mast cells and histamine in edema induced by Scolopendra viridicornis (Sv) centipede venom. The edema was analyzed on mice paws. The mice were pretreated with cromolyn (mast cell degranulation inhibitor) and antagonists of histamine receptors, such as promethazine (H1R), cimetidine (H2R) and thioperamide (H3/H4R). The analyses were carried out at different times after the injection of Sv venom (15 μg) or PBS in the footpad of mice...
October 2016: Toxicon: Official Journal of the International Society on Toxinology
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