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chloride channel blockers

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https://www.readbyqxmd.com/read/29344669/clc-2-is-a-positive-modulator-of-oligodendrocyte-precursor-cell-differentiation-and-myelination
#1
Xiaolin Hou, Rui Zhang, Junyan Wang, Yunhong Li, Fan Li, Yan Zhang, Xiaomin Zheng, Ying Shen, Yin Wang, Liang Zhou
Oligodendrocytes (OLs) are myelin-forming cells that are present within the central nervous system. Impaired oligodendrocyte precursor cell (OPC) differentiation into mature OLs is a major cause of demyelination diseases. Therefore, identifying the underlying molecular mechanisms of OPC differentiation is crucial to understand the processes of myelination and demyelination. It has been acknowledged that various extrinsic and intrinsic factors are involved in the control of OPC differentiation; however, the function of ion channels, particularly the voltage‑gated chloride channel (CLC), in OPC differentiation and myelination are not fully understood...
January 17, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29286070/nppb-modulates-apoptosis-proliferation-migration-and-extracellular-matrix-synthesis-of-conjunctival-fibroblasts-by-inhibiting-pi3k-akt-signaling
#2
Lixia Sun, Yaru Dong, Jing Zhao, Yuan Yin, Bainan Tong, Yajuan Zheng, Hua Xin
When treating glaucoma, excessive scar tissue reactions reduce the postoperative survival rate of the filtering bleb. Accumulating evidence has demonstrated that the proliferation, migration and extracellular matrix (ECM) synthesis of fibroblasts are important molecular mechanisms underlying scar formation. Recent evidence has demonstrated that chloride channels play an important role in controlling cell proliferation, apoptosis, migration and the cell cycle process in several cell types, but the effects of chloride channels on conjunctival fibroblasts have not be studied...
December 15, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29283974/the-role-of-distal-tubule-and-collecting-duct-sodium-reabsorption-in-sunitinib-induced-hypertension
#3
Jeannine Witte, Josephine Lampe, Anna Koenen, Ines Urbaneck, Antje Steinbach, Rainer Rettig, Olaf Grisk
OBJECTIVE: Antiangiogenic receptor tyrosine kinase inhibitors (RTKI) induce arterial hypertension which may limit their use. Renal fractional sodium excretion (FENa) is reduced in early RTKI-induced hypertension, whereas fractional lithium excretion is unaltered. Therefore, we tested the hypothesis that activated distal tubule and collecting duct sodium reabsorption contributes to RTKI-induced hypertension. METHODS: Amiloride-sensitive and hydrochlorothiazide (HCTZ)-sensitive fractional sodium reabsorption (FRNa) and renal epithelial sodium channel (ENaC) as well as sodium chloride cotransporter (NCC) abundances were determined in sunitinib-treated and control rats...
December 27, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/29231977/dids-inhibits-overexpression-bak1-induced-mitochondrial-apoptosis-through-gsk3%C3%AE-%C3%AE-catenin-signaling-pathway
#4
Xiayun Yang, Shusheng Tang, Daowen Li, Xiaohong Yu, Fuyun Wang, Xilong Xiao
Bcl-2 homologous antagonist/killer (BAK1) is a critical regulator of mitochondrial apoptosis. Although upregulation of BAK1 induces apoptosis has been established, the underlying molecular mechanism is far from clear. 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS), an organic anion used as a blocker of anion exchangers and chloride channels, has been proved to rescue cell apoptosis both in vitro and in vivo. However, whether DIDS can inhibit BAK1-induced mitochondrial apoptosis remains undefined. Thus, this study aimed to explore whether DIDS could protect BAK1-induced apoptosis through GSK3β/β-catenin signaling pathway...
December 12, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29185178/vasorelaxant-activities-and-the-underlying-pharmacological-mechanisms-of-gynura-procumbens-merr-leaf-extracts-on-rat-thoracic-aorta
#5
Zafar Iqbal, Idris Bello, Mohd Zaini Asmawi, Majed Ahmed Al-Mansoub, Ashfaq Ahmad, Qaiser Jabeen, Yam Mun Fei
Previous studies have investigated the cardiovascular activity of Gynura procumbens Merr. single-solvent extracts. The objective of this study was to evaluate the in vitro vasorelaxant properties and the underlying pharmacological mechanisms of serial extracts and fractions of Gynura procumbens (GP). The leaves of GP were serially extracted with petroleum ether, chloroform, methanol and water using the maceration method. Suspended aortic ring preparations were pre-contracted with phenylephrine (PE 1 µM), followed by cumulative addition of GP extracts (0...
November 28, 2017: Inflammopharmacology
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
#6
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
#7
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
#8
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
#9
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. Ca2+-activated Cl- channels mediate physiological functions independently of cystic fibrosis transmembrane conductance regulator. Anoctamin 1 (ANO1/TMEM16A) was identified as the major Ca2+-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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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