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https://www.readbyqxmd.com/read/28398338/the-histamine-h3-receptor-antagonist-thioperamide-rescues-circadian-rhythm-and-memory-function-in-experimental-parkinsonism
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
(no author information available yet)
No abstract text is available yet for this article.
March 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28132918/ciproxifan-a-histamine-h3-receptor-antagonist-and-inverse-agonist-presynaptically-inhibits-glutamate-release-in-rat-hippocampus
#9
Cheng-Wei Lu, Tzu-Yu Lin, Chia-Ying Chang, Shu-Kuei Huang, Su-Jane Wang
Ciproxifan is an H3 receptor antagonist and inverse agonist with antipsychotic effects in several preclinical models; its effect on glutamate release has been investigated in the rat hippocampus. In a synaptosomal preparation, ciproxifan reduced 4-aminopyridine (4-AP)-evoked Ca(2+)-dependent glutamate release and cytosolic Ca(2+) concentration elevation but did not affect the membrane potential. The inhibitory effect of ciproxifan on 4-AP-evoked glutamate release was prevented by the Gi/Go-protein inhibitor pertussis toxin and Cav2...
January 27, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28129985/safety-and-efficacy-of-pitolisant-on-cataplexy-in-patients-with-narcolepsy-a-randomised-double-blind-placebo-controlled-trial
#10
Zoltan Szakacs, Yves Dauvilliers, Vladimir Mikhaylov, Irina Poverennova, Sergei Krylov, Slavko Jankovic, Karel Sonka, Philippe Lehert, Isabelle Lecomte, Jeanne-Marie Lecomte, Jean-Charles Schwartz
BACKGROUND: Histaminergic neurons are crucial to maintain wakefulness, but their role in cataplexy is unknown. We assessed the safety and efficacy of pitolisant, a histamine H3 receptor inverse agonist, for treatment of cataplexy in patients with narcolepsy. METHODS: For this randomised, double-blind, placebo-controlled trial we recruited patients with narcolepsy from 16 sleep centres in nine countries (Bulgaria, Czech Republic, Hungary, Macedonia, Poland, Russia, Serbia, Turkey, and Ukraine)...
March 2017: Lancet Neurology
https://www.readbyqxmd.com/read/28126588/the-naturally-occurring-mutation-y197c-does-not-affect-the-expression-or-signaling-of-the-human-histamine-h3-receptor
#11
Cecilia Flores-Clemente, Juan Escamilla-Sánchez, Juan-Manuel Arias, José-Antonio Arias-Montaño
There is evidence for genetic polymorphism within the human histamine H3 receptor (hH3R), and a Tyr to Cys exchange at position 197 (Y197C), located in the amino terminus of the fifth transmembrane domain, has been reported. In this work we compared the expression and the pharmacological and signaling properties of wild-type (hH3RWT) and mutant (hH3RY197C) receptors transiently expressed in CHO-K1 cells. The hH3RY197C cDNA was created by overlap extension PCR amplification. Receptor expression and affinity were assessed by N-α-[methyl-(3)H]-histamine binding to cell membranes and intact cells...
January 23, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28117842/histamine-h3r-receptor-activation-in-the-dorsal-striatum-triggers-stereotypies-in-a-mouse-model-of-tic-disorders
#12
M Rapanelli, L Frick, V Pogorelov, H Ohtsu, H Bito, C Pittenger
Tic disorders affect ~5% of the population and are frequently comorbid with obsessive-compulsive disorder, autism, and attention deficit disorder. Histamine dysregulation has been identified as a rare genetic cause of tic disorders; mice with a knockout of the histidine decarboxylase (Hdc) gene represent a promising pathophysiologically grounded model. How alterations in the histamine system lead to tics and other neuropsychiatric pathology, however, remains unclear. We found elevated expression of the histamine H3 receptor in the striatum of Hdc knockout mice...
January 24, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/27986539/antihistamines-as-promising-drugs-in-cancer-therapy
#13
REVIEW
Ana I Faustino-Rocha, Rita Ferreira, Adelina Gama, Paula A Oliveira, Mário Ginja
Histamine is a biogenic amine, synthetized and released by mast cells, which acts as a vasodilator in several pathologic processes, namely in allergies and conjunctivitis. Its role on cancer is not fully understood. High levels of histamine have been associated with a bivalent behavior in regulation of several tumors (i.e. cervical, ovarian, vaginal, uterine, vulvar, colorectal cancer, and melanoma), promoting or inhibiting their growth. Histamine receptors (H1, H2, H3 and H4) are present in a vast group of cells, including tumor cells, making them sensitive to histamine variations...
March 1, 2017: Life Sciences
https://www.readbyqxmd.com/read/27975177/involvement-of-histaminergic-and-noradrenergic-receptors-in-the-oxytocin-induced-food-intake-in-neonatal-meat-type-chicks
#14
Seyed Vahid Mirnaghizadeh, Morteza Zendehdel, Vahab Babapour
Oxytocin neurons have a physiological role in food intake and energy balance. Several studies have shown that central histaminergic and adrenergic systems synapse on oxytocin neurons but there is no information for their interaction on food intake regulation in birds. The purpose of this study was to examine the effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (histamine H1 receptors antagonist), famotidine (histamine H2 receptors antagonist), thioperamide (histamine H3 receptors antagonist), prazosin (α1 receptor antagonist), yohimbine (α2 receptor antagonist), metoprolol (β1 adrenergic receptor antagonist), ICI 118,551 (β2 adrenergic receptor antagonist) and SR59230R (β3 adrenergic receptor antagonist) on oxytocin-induced hypophagia in 3-h food-deprived (FD3) neonatal broiler chicken...
March 2017: Veterinary Research Communications
https://www.readbyqxmd.com/read/27932863/non-imidazole-based-histamine-h3-receptor-antagonists-with-anticonvulsant-activity-in-different-seizure-models-in-male-adult-rats
#15
Bassem Sadek, Ali Saad, Gniewomir Latacz, Kamil Kuder, Agnieszka Olejarz, Tadeusz Karcz, Holger Stark, Katarzyna Kieć-Kononowicz
A series of twelve novel non-imidazole-based ligands (3-14) was developed and evaluated for its in vitro binding properties at the human histamine H3 receptor (hH3R). The novel ligands were investigated for their in vivo protective effects in different seizure models in male adult rats. Among the H3R ligands (3-14) tested, ligand 14 showed significant and dose-dependent reduction in the duration of tonic hind limb extension in maximal electroshock (MES)-induced seizure model subsequent to acute systemic administration (5, 10, and 20 mg/kg, intraperitoneally), whereas ligands 4, 6, and 7 without appreciable protection in MES model were most promising in pentylenetetrazole (PTZ) model...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27902931/human-presynaptic-receptors
#16
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
#17
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)...
February 2017: Journal of Neurology
https://www.readbyqxmd.com/read/27866818/the-discovery-of-quinoline-based-single-ligand-human-h1-and-h3-receptor-antagonists
#18
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
#19
Darren M Riddy, Anna E Cook, Natalie A Diepenhorst, Sanja Bosnyak, Ryan Brady, Clotilde Mannoury la Cour, Elisabeth Mocaer, Roger J Summers, William N 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 nonfunctional isoforms. Despite the general acceptance that G protein-coupled receptors can adopt different ligand-induced conformations that give rise to biased signaling, this has not been studied for the H3R; further, it is unknown whether splice variants of the same receptor engender the same or differential biased signaling. Herein, we profiled the pharmacology of histamine receptor agonists at the two most abundant hH3R splice variants (hH3R445 and hH3R365) across seven signaling endpoints...
February 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/27863547/identification-of-histamine-receptors-in-the-canine-gastrointestinal-tract
#20
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
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