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https://www.readbyqxmd.com/read/28209485/effects-of-clozapine-on-adipokine-secretions-productions-and-lipid-droplets-in-3t3-l1-adipocytes
#1
Tomomi Tsubai, Akira Yoshimi, Yoji Hamada, Makoto Nakao, Hiroshi Arima, Yutaka Oiso, Yukihiro Noda
Clozapine, a second-generation antipsychotic (SGA), is a cause of side effects related to metabolic syndrome. The participation of serotonin 5-HT2C and histamine H1 receptors in the central nervous system has been reported as a mechanism of the weight gain caused by clozapine. In the present study, we investigated the direct pharmacological action of clozapine on the 3T3-L1 adipocytes and compared it to that of blonanserin, an SGA with low affinity for both receptors. Short-term exposure to clozapine decreased secretion and mRNA expression of leptin...
January 28, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28199959/central-neuronal-functions-of-histamine-h4-receptors
#2
EDITORIAL
Maria Domenica Sanna, Nicoletta Galeotti
No abstract text is available yet for this article.
February 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28196712/ipomoea-pes-caprae-l-r-br-convolvulaceae-as-a-topical-herbal-medicine-to-relieve-pain-and-inflammation-promising-tool-against-effects-due-to-toxin-skin-contact
#3
Cristiane da Silva Barth, Hugo Guilherme Tolentino de Souza, Lilian W Rocha, Gislaine Francieli da Silva, Mariana Ferreira Dos Anjos, Veronica D'Avila Pastor, Tania Mari Belle Bresolin, Angelica Garcia Couto, José Roberto Santin, Nara Lins Meira Quintão
ETHNOPHARMACOLOGICAL RELEVANCE: Ipomoea pes-caprae is known as bayhops, beach morning glory or goat's foot, and in Brazil as salsa-de-praia. Its leaves are used in worldwide folk medicine for the relief of jellyfish-stings symptoms. The literature only reports the anti-inflammatory and neutralizing effects of a nonpolar plant derived, without validating the popular use or exploring the mechanism of action. AIM OF THE STUDY: This study aimed to evaluate and validate the topical effects of a semisolid containing hydroethanolic extract obtained from the aerial parts of I...
February 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28194132/molecular-imaging-markers-to-track-huntington-s-disease-pathology
#4
REVIEW
Heather Wilson, Rosa De Micco, Flavia Niccolini, Marios Politis
Huntington's disease (HD) is a progressive, monogenic dominant neurodegenerative disorder caused by repeat expansion mutation in the huntingtin gene. The accumulation of mutant huntingtin protein, forming intranuclear inclusions, subsequently leads to degeneration of medium spiny neurons in the striatum and cortical areas. Genetic testing can identify HD gene carriers before individuals develop overt cognitive, psychiatric, and chorea symptoms. Thus, HD gene carriers can be studied in premanifest stages to understand and track the evolution of HD pathology...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28193449/histamine-and-mast-cell-activator-compound-48-80-are-safe-but-inefficient-systemic-adjuvants-for-gilthead-seabream-vaccination
#5
N E Gómez González, I Cabas, J Montero, A García Alcázar, V Mulero, A García Ayala
Histamine has a key role in the regulation of inflammatory and innate immune responses in vertebrates. Gilthead seabream (Sparus aurata L.), a marine hermaphrodite teleost of great commercial value, was the first fish species shown to possess histamine-containing mast cells (MCs) at mucosal tissues. MCs are highly abundant in the peritoneal exudate of gilthead seabream and compound 48/80 (Co 48/80), often used to promote MC activation and histamine release, is able to promote histamine release from gilthead seabream MCs in vitro and in vivo...
February 10, 2017: Developmental and Comparative Immunology
https://www.readbyqxmd.com/read/28193102/identification-of-predictors-for-treatment-failure-in-hepatitis-c-virus-patients-treated-with-ledipasvir-and-sofosbuvir
#6
Jeffrey W Jansen, Gillian M Powderly, Travis W Linneman
BACKGROUND: New hepatitis C virus (HCV) therapies report cure rates of ~90% but are expensive. Identification of predictors for treatment failure could help decrease health care costs, limit unnecessary drug exposure and adverse events, and prevent drug-drug interactions. Failure to achieve rapid viral response (RVR), defined as detectable viral load at 4 weeks, has previously been identified as a predictor of treatment failure with some previous HCV therapies. OBJECTIVE: To evaluate RVR, and other potential variables, as predictors of treatment failure in patients treated with ledipasvir and sofosbuvir (LDV/SOF)...
February 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28191683/immediate-type-allergic-and-protease-mediated-reactions-are-involved-in-scratching-behavior-induced-by-topical-application-of-dermatophagoides-farinae-extract-in-nc-nga-mice
#7
Yoshihito Yamada, Yuhki Ueda, Aki Nakamura, Shoji Kanayama, Rie Tamura, Kei Hashimoto, Tatsumi Matsumoto, Ritsuko Ishii
Atopic dermatitis (AD)-like dermatitis can be induced by repeated topical application of an ointment containing Dermatophagoides farinae body (Dfb) extract in NC/Nga mice. This AD-like murine model also exhibits a biphasic increase in the number of scratching behavior after topical application of Dfb ointment. In this study, we investigated the possible mechanisms underlying the scratching behavior in each phase. An increase in the content of mast cell derived mediators such as histamine and 5-hydroxytryptamine in the lesional skin and increased vascular permeability were observed in the early phase after the Dfb ointment application...
February 13, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28191674/induced-histamine-regulates-ni-elution-from-an-implanted-ni-wire-in-mice-by-downregulating-neutrophil-migration
#8
Yu Kishimoto, Sanki Asakawa, Taiki Sato, Takayuki Takano, Takahisa Nakajyo, Natsumi Mizuno, Ryosuke Segawa, Takeo Yoshikawa, Masahiro Hiratsuka, Kazuhiko Yanai, Hiroshi Ohtsu, Noriyasu Hirasawa
Histamine regulates various inflammatory reactions. We have reported that the expression of histidine decarboxylase (HDC) was induced by subcutaneous implantation of nickel (Ni) wire. However, the source and functions of histamine in Ni elution and Ni wire-induced inflammation have not completely studied. We aimed to elucidate the effects of de novo synthesized histamine on leukocyte infiltration and Ni elution. Implantation of Ni wire induced an increase in the Ni ion content of the surrounding tissues and serum and in the mRNA levels of HDC, a histamine-producing enzyme, macrophage inflammatory protein-2 (MIP-2), a chemoattractant for neutrophils, and monocyte chemoattractant protein-1 (MCP-1), a chemoattractant for monocytes...
February 13, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28190755/quantitative-prediction-of-histamine-h1-receptor-occupancy-by-the-sedative-and-non-sedative-antagonists-in-the-human-central-nervous-system-based-on-systemic-exposure-and-preclinical-data
#9
Kayoko Kanamitsu, Yoshitane Nozaki, Yoko Nagaya, Yuichi Sugiyama, Hiroyuki Kusuhara
Significant histamine H1 receptor occupation in the central nervous system (CNS) is associated with sedation. Here we examined the time profiles of the H1 receptor occupancy (RO) in the CNS using sedative (diphenhydramine and ketotifen) and non-sedative (bepotastine and olopatadine) antagonists at their therapeutic doses by integrating in vitro and animal data. A pharmacokinetic model was constructed to associate plasma concentrations and receptor binding in the brain. Dissociation and association rate constants with the H1 receptor and plasma and brain unbound fractions were determined in vitro...
November 18, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28190472/gastroprotective-and-anti-secretory-mechanisms-of-2-phenylquinoline-an-alkaloid-isolated-from-galipea-longiflora
#10
Eduardo Breviglieri, Luisa Mota da Silva, Thaise Boeing, Lincon Bordignon Somensi, Benhur Judah Cury, Alberto Gimenez, Valdir Cechinel Filho, Sérgio Faloni de Andrade
BACKGROUND: We previously described the gastroprotective effect of 2-phenylquinoline (2-PQ), the main alkaloid isolated from the bark of Galipea longiflora (Rutaceae). However, despite the significant and promising results, the pharmacological mechanisms of the gastroprotection induced by 2-PQ have not been investigated. PURPOSE: To evaluate the mechanisms underlying the gastroprotective effects of 2-PQ. STUDY DESIGN: We used an in vivo mouse ulcer model and in vitro methodologies involving H⁺/K⁺-ATPase and L929 murine fibroblasts...
February 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28188977/lack-of-incremental-effect-of-histamine-receptor-antagonists-over-proton-pump-inhibitors-on-the-risk-of-neoplastic-progression-in-patients-with-barrett-s-esophagus-a-cohort-study
#11
Prashanthi N Thota, Kaveh Hajifathalian, Tanmayee Benjamin, Ashok Runkana, Rocio Lopez, Madhusudhan R Sanaka
AIMS: Long-term acid suppression lowers the risk of progression to esophageal adenocarcinoma (EAC) in patients with Barrett's esophagus (BE). With the recent reports about harmful effects of chronic proton pump inhibitor (PPI) use, there is renewed interest about alternative methods of acid suppression. Hence, our aim was to study the effect of H2 receptor antagonists (H2RA) on the risk of progression to neoplasia in our BE cohort. METHODS: This is a retrospective analysis of prospectively collected data of patients in our BE Registry from 2002 to 2015...
February 11, 2017: Journal of Digestive Diseases
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
#12
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...
February 11, 2017: Hippocampus
https://www.readbyqxmd.com/read/28185047/histaminergic-h1-and-h2-receptors-mediate-the-effects-of-propofol-on-the-noradrenalin-inhibited-neurons-in-rat-ventrolateral-preoptic-nucleus
#13
Yang Liu, Yu Zhang, Kun Qian, Lin Zhang, Tian Yu
The ventrolateral preoptic nucleus is a sleep-promoting nucleus located in the basal forebrain. A commonly used intravenous anesthetic, propofol, had been reported to induce sleep spindles and augment the firing rate of neurons in ventrolateral preoptic nucleus, but the underlining mechanism is yet to be known. By using patch clamp recording on neuron in acute brain slice, present study tested if histaminergic H1 and H2 receptors play a role in the effect of propofol on the noradrenalin-inhibited neurons in ventrolateral preoptic nucleus...
February 9, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28181493/natural-amines-inhibit-activation-of-human-plasmacytoid-dendritic-cells-through-cxcr4-engagement
#14
Nikaïa Smith, Nicolas Pietrancosta, Sophia Davidson, Jacques Dutrieux, Lise Chauveau, Pasquale Cutolo, Michel Dy, Daniel Scott-Algara, Bénédicte Manoury, Onofrio Zirafi, Isabelle McCort-Tranchepain, Thierry Durroux, Françoise Bachelerie, Olivier Schwartz, Jan Münch, Andreas Wack, Sébastien Nisole, Jean-Philippe Herbeuval
Plasmacytoid dendritic cells (pDC) are specialized in secretion of type I interferon in response to pathogens. Here we show that natural monoamines and synthetic amines inhibit pDC activation by RNA viruses. Furthermore, a synthetic analogue of histamine reduces type I interferon production in a mouse model of influenza infection. We identify CXC chemokine receptor 4 (CXCR4) as a receptor used by amines to inhibit pDC. Our study establishes a functional link between natural amines and the innate immune system and identifies CXCR4 as a potential 'on-off' switch of pDC activity with therapeutic potential...
February 9, 2017: Nature Communications
https://www.readbyqxmd.com/read/28178593/the-role-of-histamine-in-the-regulation-of-the-viability-proliferation-and-transforming-growth-factor-%C3%AE-1-secretion-of-rat-wound-fibroblasts
#15
Monika Wolak, Ewa Bojanowska, Teresa Staszewska, Joanna Ciosek, Marlena Juszczak, Jacek Drobnik
BACKGROUND: Inflammation mediators play a regulatory role in repair processes. The study will examine the influence of histamine on wound fibroblast metabolic activity, viability, proliferation, and TGFβ1 secretion. The study also will identify the histamine receptor involved in regulation of the tested repair processes. METHODS: Fibroblasts were obtained from the granulation tissue of wounds or intact dermis of rats. The MTT and BrdU assays were used to examine the effect of histamine (10(-8)M-10(-4)M) on the viability and metabolic activity of fibroblasts, and on their proliferative capacity...
November 15, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28173961/a-screen-for-modulators-reveals-that-orexin-a-rapidly-stimulates-thyrotropin-releasing-hormone-expression-and-release-in-hypothalamic-cell-culture
#16
Antonieta Cote-Vélez, Anabel Martínez Báez, Leticia Lezama, Rosa María Uribe, Patricia Joseph-Bravo, Jean-Louis Charli
In the paraventricular nucleus of the mammalian hypothalamus, hypophysiotropic thyrotropin releasing hormone (TRH) neurons integrate metabolic information and control the activity of the thyroid axis. Additional populations of TRH neurons reside in various hypothalamic areas, with poorly defined connections and functions, albeit there is evidence that some may be related to energy balance. To establish extracellular modulators of TRH hypothalamic neurons activity, we performed a screen of neurotransmitters effects in hypothalamic cultures...
February 2, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28173624/evidence-for-the-role-of-histaminergic-pathways-in-neuroprotective-mechanism-of-ischemic-postconditioning-in-mice
#17
Indresh Kaur, Amit Kumar, Amteshwar S Jaggi, Nirmal Singh
The present study has been designed to investigate the possible role of histaminergic pathway in neuroprotective mechanism of ischemic postconditioning (iPoCo). Bilateral carotid artery occlusion (BCAO) for 12 min followed by reperfusion for 24 hr was employed to produce I/R induced cerebral injury in NIH mice. iPoCo involving three episodes of carotid artery occlusion and reperfusion of 10 sec each, was instituted immediately after BCAO just before prolonged reperfusion. Cerebral infarct size was measured using triphenyltetrazolium chloride staining...
February 7, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28168839/histamine-h3-receptor-antagonist-prevents-memory-deficits-and-synaptic-plasticity-disruption-following-isoflurane-exposure
#18
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/28167332/chemoreception-to-aggregation-pheromones-in-the-common-bed-bug-cimex-lectularius
#19
Feng Liu, Caixing Xiong, Nannan Liu
The common bed bug, Cimex lectularius, is an obligate blood-feeding insect that is resurgent worldwide, posing a threat to human beings through its biting nuisance and disease transmission. Bed bug aggregation pheromone is considered a very promising attractant for use in the monitoring and management of bed bugs, but as yet little is known regarding the sensory physiology of bed bugs related to this pheromone. This study examined how the individual components of aggregation pheromone are perceived by the olfactory receptor neurons (ORNs) housed in different types of olfactory sensilla in bed bugs and the molecular basis for the ORNs' responses to the aggregation pheromone...
February 3, 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28160941/the-topological-phase-diagram-of-cimetidine-a-case-of-overall-monotropy
#20
R Céolin, I B Rietveld
Cimetidine is a histamine H2-receptor antagonist used against peptic ulcers. It is known to exhibit crystalline polymorphism. Forms A and D melt within 0.35 degrees from each other and the enthalpies of fusion are similar as well. The present paper demonstrates how to construct a pressure-temperature phase diagram with only calorimetric and volumetric data available. The phase diagram provides the stability domains and the phase equilibria for the phases A, D, the liquid and the vapor. Cimetidine is overall monotropic with form D the only stable solid phase...
February 1, 2017: Annales Pharmaceutiques Françaises
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