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https://www.readbyqxmd.com/read/29089046/the-novel-isoxazoline-ectoparasiticide-lotilaner-credelio%C3%A2-a-non-competitive-antagonist-specific-to-invertebrates-%C3%AE-aminobutyric-acid-gated-chloride-channels-gabacls
#1
Lucien Rufener, Vanessa Danelli, Daniel Bertrand, Heinz Sager
BACKGROUND: The isoxazolines are a novel class of parasiticides that are potent inhibitors of γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and, to a lesser extent, of inhibitory glutamate-gated chloride channels (GluCls). Lotilaner (Credelio™), a novel representative of this chemical class, is currently evaluated for its excellent ectoparasiticide properties. METHODS: In this study, we investigated the molecular mode of action and pharmacology of lotilaner...
November 1, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28981821/sodium-carbonate-is-saltier-than-sodium-chloride-to-sodium-depleted-rats
#2
Steven J St John, Anya M McBrayer, Erin E Krauskopf
In a series of behavioral experiments in the 1960s, G.R. Morrison identified several unique features of the taste of Na2CO3 to rats; namely, it is 1) considerably more intense than NaCl at isomolar concentrations, 2) avoided at 10 times lower concentrations than NaCl to thirsty rats, 3) preferred at 10 times lower concentrations than NaCl in sodium-depleted rats. He also demonstrated its qualitatively similarity to NaCl. In Experiment 1, we confirmed and extended many of Morrison's observations. Rats were injected with furosemide on 3 occasions to stimulate a sodium appetite...
October 1, 2017: Chemical Senses
https://www.readbyqxmd.com/read/28981681/resistance-status-and-resistance-mechanisms-in-a-strain-of-aedes-aegypti-diptera-culicidae-from-puerto-rico
#3
Alden S Estep, Neil D Sanscrainte, Christy M Waits, Jessica E Louton, James J Becnel
Puerto Rico (PR) has a long history of vector-borne disease and insecticide-resistant Aedes aegypti (L.). Defining contributing mechanisms behind phenotypic resistance is critical for effective vector control intervention. However, previous studies from PR have each focused on only one mechanism of pyrethroid resistance. This study examines the contribution of P450-mediated enzymatic detoxification and sodium channel target site changes to the overall resistance phenotype of Ae. aegypti collected from San Juan, PR, in 2012...
November 7, 2017: Journal of Medical Entomology
https://www.readbyqxmd.com/read/28955034/microrna-9-downregulates-the-ano1-chloride-channel-and-contributes-to-cystic-fibrosis-lung-pathology
#4
Florence Sonneville, Manon Ruffin, Christelle Coraux, Nathalie Rousselet, Philippe Le Rouzic, Sabine Blouquit-Laye, Harriet Corvol, Olivier Tabary
Cystic fibrosis results from reduced cystic fibrosis transmembrane conductance regulator protein activity leading to defective epithelial ion transport. Ca(2+)-activated Cl(-) channels mediate physiological functions independently of cystic fibrosis transmembrane conductance regulator. Anoctamin 1 (ANO1/TMEM16A) was identified as the major Ca(2+)-activated Cl(-) channel in airway epithelial cells, and we recently demonstrated that downregulation of the anoctamin 1 channel in cystic fibrosis patients contributes to disease severity via an unknown mechanism...
September 27, 2017: Nature Communications
https://www.readbyqxmd.com/read/28943490/the-curcumin-induced-vasorelaxation-in-rat-superior-mesenteric-arteries
#5
Han Zhang, Huanhuan Liu, Yulong Chen, Yan Zhang
BACKGROUND: Curcumin (Cur) is a natural lipophilic polyphenol compound extracted from the rhizome of turmeric. Recently, protective effect of Cur on cardiovascular system is paid close attention. Some researches demonstrated that Cur could induce vascular relaxation in many arterial beds. However, relaxant effect of Cur on rat superior mesenteric artery is not clear. This present study will investigate the vasorelaxant effect of Cur on rat superior mesenteric arteries and the mechanisms involved...
September 22, 2017: Annals of Vascular Surgery
https://www.readbyqxmd.com/read/28920462/involvement-of-atrial-natriuretic-peptide-in-abrogated-cardioprotective-effect-of-ischemic-preconditioning-in-ovariectomized-rat-heart
#6
V K Vishwakarma, A Goyal, J K Gupta, P K Upadhyay, H N Yadav
BACKGROUND: Nitric oxide (NO) is an effective mediator of ischemic preconditioning (IPC)-induced cardioprotection. Atrial natriuretic peptide (ANP) is downregulated after ovariectomy, which results in reduction in the level of NO. The present study deals with the investigation of the role of ANP in abrogated cardioprotective effect of IPC in the ovariectomized rat heart. METHODS: Heart was isolated from ovariectomized rat and mounted on Langendorff's apparatus, subjected to 30 min of ischemia and 120 min of reperfusion...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/28819106/identification-and-characterization-of-a-bacterial-homolog-of-chloride-intracellular-channel-clic-protein
#7
Shubha Gururaja Rao, Devasena Ponnalagu, Sowmya Sukur, Harkewal Singh, Shridhar Sanghvi, Yixiao Mei, Ding J Jin, Harpreet Singh
Chloride intracellular channels (CLIC) are non-classical ion channels lacking a signal sequence for membrane targeting. In eukaryotes, they are implicated in cell volume regulation, acidification, and cell cycle. CLICs resemble the omega class of Glutathione S-transferases (GST), yet differ from them in their ability to form ion channels. They are ubiquitously found in eukaryotes but no prokaryotic homolog has been characterized. We found that indanyloxyacetic acid-94 (IAA-94), a blocker of CLICs, delays the growth of Escherichia coli...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28727479/extracellular-chloride-is-required-for-efficient-platelet-aggregation
#8
Kirk A Taylor, Darren G S Wilson, Matthew T Harper, Nicholas Pugh
Anion channels perform a diverse range of functions and have been implicated in ATP release, volume regulation, and phosphatidylserine exposure. Platelets have been shown to express several anion channels but their function is incompletely understood. Due to a paucity of specific pharmacological blockers, we investigated the effect of extracellular chloride substitution on platelet activation using aggregometry and flow cytometry. In the absence of extracellular chloride, we observed a modest reduction of the maximum aggregation response to thrombin or collagen-related peptide...
July 20, 2017: Platelets
https://www.readbyqxmd.com/read/28642338/cellular-distribution-and-function-of-ion-channels-involved-in-transport-processes-in-rat-tracheal-epithelium
#9
Anne Hahn, Johannes Faulhaber, Lalita Srisawang, Andreas Stortz, Johanna J Salomon, Marcus A Mall, Stephan Frings, Frank Möhrlen
Transport of water and electrolytes in airway epithelia involves chloride-selective ion channels, which are controlled either by cytosolic Ca(2+) or by cAMP The contributions of the two pathways to chloride transport differ among vertebrate species. Because rats are becoming more important as animal model for cystic fibrosis, we have examined how Ca(2+)- dependent and cAMP- dependent Cl(-) secretion is organized in the rat tracheal epithelium. We examined the expression of the Ca(2+)-gated Cl(-) channel anoctamin 1 (ANO1), the cystic fibrosis transmembrane conductance regulator (CFTR) Cl(-) channel, the epithelial Na(+) channel ENaC, and the water channel aquaporin 5 (AQP5) in rat tracheal epithelium...
June 2017: Physiological Reports
https://www.readbyqxmd.com/read/28633068/multi-electrode-system-for-measurement-of-transmembrane-ion-fluxes-through-living-epithelial-cells
#10
Mirosław Zając, Andrzej Lewenstam, Krzysztof Dolowy
Cystic Fibrosis (CF) is the most common fatal human genetic disease. It is caused by the defect in a single anion channel protein which affects ion and water transport across the epithelial tissue. A flat multi-electrode platform of diameter 12mm, allowing for measurement of four ions: sodium, potassium, hydrogen and chloride by exchangeable/replaceable ion-selective electrodes is described. The measurement is possible owing to the architecture of the platform which accommodates all the electrodes and inlets/outlets...
October 2017: Bioelectrochemistry
https://www.readbyqxmd.com/read/28559795/voltage-dependent-inhibition-of-glycine-receptor-channels-by-niflumic-acid
#11
Galyna Maleeva, Franck Peiretti, Boris S Zhorov, Piotr Bregestovski
Niflumic acid (NFA) is a member of the fenamate class of nonsteroidal anti-inflammatory drugs. This compound and its derivatives are used worldwide clinically for the relief of chronic and acute pain. NFA is also a commonly used blocker of voltage-gated chloride channels. Here we present evidence that NFA is an efficient blocker of chloride-permeable glycine receptors (GlyRs) with subunit heterogeneity of action. Using the whole-cell configuration of patch-clamp recordings and molecular modeling, we analyzed the action of NFA on homomeric α1ΔIns, α2B, α3L, and heteromeric α1β and α2β GlyRs expressed in CHO cells...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28468943/estradiol-activates-chloride-channels-via-estrogen-receptor-%C3%AE-in-the-cell-membranes-of-osteoblasts
#12
Zhiqin Deng, Shuang Peng, Yanfang Zheng, Xiaoya Yang, Haifeng Zhang, Qiuchan Tan, Xiechou Liang, Hong Gao, Yuan Li, Yanqing Huang, Linyan Zhu, Tim J C Jacob, Lixin Chen, Liwei Wang
Estrogen plays important roles in regulation of bone formation. Cl(-) channels in the ClC family are expressed in osteoblasts and are associated with bone physiology and pathology, but the relationship between Cl(-) channels and estrogen is not clear. In this study the action of estrogen on Cl(-) channels was investigated in the MC3T3-E1 osteoblast cell line. Our results show that 17β-estradiol could activate a current that reversed at a potential close to the Cl(-) equilibrium potential, with a sequence of anion selectivity of I(-) > Br(-) > Cl(-) > gluconate, and was inhibited by the Cl(-) channel blockers 5-nitro-2-(3-phenylpropylamino)-benzoate and 4,4'-diisothiocyano-2,2'-stilbene disulfonic acid...
August 1, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28446427/airway-epithelial-anion-secretion-and-barrier-function-following-exposure-to-fungal-aeroallergens-role-of-oxidative-stress
#13
Nathan A Zaidman, Kelly E O'Grady, Nandadevi Patil, Francesca Milavetz, Peter J Maniak, Hirohito Kita, Scott M O'Grady
Aeroallergens produced by Alternaria alternata can elicit life-threatening exacerbations of asthma in patients sensitized to this fungus. In this study, the effect of Alternaria on ion transport mechanisms underlying mucociliary clearance and airway epithelial barrier function was investigated in human airway epithelial cells. Apical exposure to Alternaria induced an increase in anion secretion that was inhibited by blockers of CFTR and Ca(2+)-activated Cl(-) channels. Stimulation of anion secretion was dependent on Ca(2+) uptake from the apical solution...
July 1, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28435971/-mechanisms-underlying-rat-coronary-arterial-vasoconstriction-induced-by-blockade-of-inward-rectifier-potassium-channels-with-bacl2
#14
Fang-Wen Fan, Ze-Fang He, Meng Shi, Rong Yang, Xiao-Min Hou, Yu Liu, Ming-Sheng Zhang
In order to explore the mechanisms underlying the vasoconstriction induced by blockade of inward rectifier K(+) channels (Kir) with BaCl2, myogenic tone of isolated rat coronary artery (RCA) was recorded with wire myograph. The dependence of BaCl2- induced contraction on intracellular Ca(2+) ([Ca(2+)]i) release and extracellular Ca(2+) ([Ca(2+)]o) influx was studied by Ca(2+) deprivation and restoration. The mechanisms underlying BaCl2-induced RCA contraction were investigated with specific inhibitors. BaCl2 (0...
April 25, 2017: Sheng Li Xue Bao: [Acta Physiologica Sinica]
https://www.readbyqxmd.com/read/28419445/activation-of-clc-3-chloride-channel-by-17%C3%AE-estradiol-relies-on-the-estrogen-receptor-%C3%AE-expression-in-breast-cancer
#15
Haifeng Yang, Lianshun Ma, Yawei Wang, Wanhong Zuo, Bingxue Li, Yaping Yang, Yehui Chen, Lixin Chen, Liwei Wang, Linyan Zhu
Although extensively studied, the mechanisms by which estrogen promotes breast cancer growth remain to be fully elucidated. Tamoxifen, an antiestrogen agent to treat ERα+ breast cancer, is also a high-affinity blocker of the chloride channels. In this study, we explored the involvement of the chloride channels in the action of estrogen in breast cancer. We found that 17β-estradiol (17β-E2) concentration-dependently activated the chloride currents in ERα+ breast cancer MCF-7 cells. Extracellular hypertonic challenge and chloride channel blockers, NPPB and DIDS inhibited the 17β-E2-activated chloride currents...
April 17, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28416372/effects-of-bilobalide-ginkgolide-b-and-picrotoxinin-on-gabaa-receptor-modulation-by-structurally-diverse-positive-modulators
#16
Chiu Chin Ng, Rujee K Duke, Tina Hinton, Graham A R Johnston
Anxiolytics and anticonvulsants generally positively modulate the action of GABA, whereas many convulsants (including the chloride channel blocker picrotoxinin) negatively modulate the action of GABA on GABAA receptors. Like picrotoxinin, bilobalide and ginkgolide B, active constituents of Ginkgo biloba, have been shown to negatively modulate the action of GABA at α1β2γ2L GABAA receptors. However, unlike picrotoxinin, bilobalide and ginkgolide B are not known to cause convulsions. We have assessed the action of bilobalide, ginkgolide B and picrotoxinin on a range of GABAA modulators (etomidate, loreclezole, propofol, thiopentone sodium, diazepam, and allopregnanolone), using two-electrode voltage clamp electrophysiology at recombinant α1β2γ2L GABAA receptors expressed in Xenopus oocytes...
April 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28411554/emodin-suppresses-the-nasopharyngeal-carcinoma-cells-by-targeting-the-chloride-channels
#17
Lianshun Ma, Yaping Yang, Zizhang Yin, Mei Liu, Liwei Wang, Lixin Chen, Linyan Zhu, Haifeng Yang
Emodin is a natural anthraquinone derivative isolated from the Rheum palmatum. Recent studies demonstrated that emodin has anti-cancer activity in different kinds of human cancer cell lines. However, the underlying mechanism has not been very well studied. Our previous studies showed chloride channels is an important target of anti-cancer drugs. Therefore, the purpose of this research was aimed to explore the role of chloride channels involving in the anti-cancer activity of emodin. The proliferation, cell cycle arrest and apoptosis of poorly differentiated human nasopharyngeal carcinoma cells (CNE-2Z) and normal nasopharyngeal epithelial cells (NP69-SV40T) were detected by 3-(4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide(MTT)and flow cytometry...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28334417/pharmacovigilance-database-search-discloses-clc-k-channels-as-a-novel-target-of-the-at1-receptor-blockers-valsartan-and-olmesartan
#18
Paola Imbrici, Domenico Tricarico, Giuseppe Felice Mangiatordi, Orazio Nicolotti, Marcello Diego Lograno, Diana Conte, Antonella Liantonio
BACKGROUND AND PURPOSE: Human ClC-K chloride channels are highly attractive targets for drug discovery as they have a variety of important physiological functions and are associated with genetic disorders. These channels are crucial in the kidney as they control chloride reabsorption and water diuresis. In addition, loss-of-function mutations of CLCNKB and BSND genes cause Bartter's syndrome (BS), whereas CLCNKA and CLCNKB gain-of-function polymorphisms predispose to a rare form of salt sensitive hypertension...
July 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28300155/volume-sensitive-outwardly-rectifying-chloride-channel-blockers-protect-against-high-glucose-induced-apoptosis-of-cardiomyocytes-via-autophagy-activation
#19
Lin Wang, Mingzhi Shen, Xiaowang Guo, Bo Wang, Yuesheng Xia, Ning Wang, Qian Zhang, Lintao Jia, Xiaoming Wang
Hyperglycemia is a well-characterized contributing factor for cardiac dysfunction and heart failure among diabetic patients. Apoptosis of cardiomyocytes plays a major role during the onset and pathogenesis of diabetic cardiomyopathy (DCM). Nonetheless, the molecular machinery underlying hyperglycemia-induced cardiac damage and cell death remains elusive. In the present study, we found that chloride channel blockers, 4,4'-diisothiocya-natostilbene-2,2'- disulfonic acid (DIDS) and 4-(2-butyl-6,7-dichlor-2-cyclopentyl-indan-1-on-5-yl) oxybutyric acid (DCPIB), inhibited high glucose-activated volume-sensitive outwardly rectifying (VSOR) Cl(-) channel and improved the viability of cardiomyocytes...
March 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28280458/jmv5656-a-novel-derivative-of-tlqp-21-triggers-the-activation-of-a-calcium-dependent-potassium-outward-current-in-microglial-cells
#20
Ilaria Rivolta, Anna Binda, Laura Molteni, Laura Rizzi, Elena Bresciani, Roberta Possenti, Jean-Alain Fehrentz, Pascal Verdié, Jean Martinez, Robert J Omeljaniuk, Vittorio Locatelli, Antonio Torsello
TLQP-21 (TLQPPASSRRRHFHHALPPAR) is a multifunctional peptide that is involved in the control of physiological functions, including feeding, reproduction, stress responsiveness, and general homeostasis. Despite the huge interest in TLQP-21 biological activity, very little is known about its intracellular mechanisms of action. In microglial cells, TLQP-21 stimulates increases of intracellular Ca(2+) that may activate functions, including proliferation, migration, phagocytosis and production of inflammatory molecules...
2017: Frontiers in Cellular Neuroscience
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