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https://www.readbyqxmd.com/read/29738885/regulation-of-seizure-induced-mecp2-ser421-phosphorylation-in-the-developing-brain
#1
Evan C Rosenberg, Jocelyn J Lippman-Bell, Marcus Handy, Samantha S Soldan, Sanjay Rakhade, Cristina Hilario-Gomez, Kaitlyn Folweiler, Leah Jacobs, Frances E Jensen
Neonatal seizures disrupt normal synaptic maturation and often lead to later-life epilepsy and cognitive deficits. During early life, the brain exhibits heightened synaptic plasticity, in part due to a developmental overabundance of CaV 1.2 L-type voltage gated calcium (Ca2+ ) channels (LT-VGCCs) and Ca2+ -permeable AMPARs (CP-AMPARs) lacking GluA2 subunits. We hypothesized that early-life seizures overactivate these channels, in turn dysregulating Ca2+ -dependent signaling pathways including that of methyl-CPG-binding protein 2 (MeCP2), a transcription factor implicated in the autism spectrum disorder (ASD) Rett Syndrome...
May 5, 2018: Neurobiology of Disease
https://www.readbyqxmd.com/read/29713521/new-experimental-models-of-retinal-degeneration-for-screening-molecular-photochromic-ion-channel-blockers
#2
A Yu Rotov, L A Astakhova, V S Sitnikova, A A Evdokimov, V M Boitsov, M V Dubina, M N Ryazantsev, M L Firsov
Application of molecular photochromic ion channel blockers to recover the visual function of a degenerated retina is one of the promising trends in photopharmacology. To this day, several photochromic azobenzene-based compounds have been proposed and their functionality has been demonstrated on cell lines and knockout mouse models. Further advance necessitates testing of the physiological activity of a great number of new compounds. The goal of this study is to propose animal models of photoreceptor degeneration that are easier to obtain than knockout mouse models but include the main features required for testing the physiological activity of molecular photoswitches...
January 2018: Acta Naturae
https://www.readbyqxmd.com/read/29686743/antinociceptive-activity-of-methanolic-extract-of-clinacanthus-nutans-leaves-possible-mechanisms-of-action-involved
#3
Zainul Amiruddin Zakaria, Mohammad Hafiz Abdul Rahim, Rushduddin Al Jufri Roosli, Mohd Hijaz Mohd Sani, Maizatul Hasyima Omar, Siti Farah Mohd Tohid, Fezah Othman, Siew Mooi Ching, Arifah Abdul Kadir
Methanolic extract of Clinacanthus nutans Lindau leaves (MECN) has been proven to possess antinociceptive activity that works via the opioid and NO-dependent/cGMP-independent pathways. In the present study, we aimed to further determine the possible mechanisms of antinociception of MECN using various nociceptive assays. The antinociceptive activity of MECN was (i) tested against capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged against selective antagonist of opioid receptor subtypes ( β -funaltrexamine, naltrindole, and nor-binaltorphimine); (iii) prechallenged against antagonist of nonopioid systems, namely, α 2 -noradrenergic (yohimbine), β -adrenergic (pindolol), adenosinergic (caffeine), dopaminergic (haloperidol), and cholinergic (atropine) receptors; (iv) prechallenged with inhibitors of various potassium channels (glibenclamide, apamin, charybdotoxin, and tetraethylammonium chloride)...
2018: Pain Research & Management: the Journal of the Canadian Pain Society
https://www.readbyqxmd.com/read/29580953/effects-of-drugs-of-abuse-on-channelrhodopsin-2-kinetics
#4
Dominic Gioia, Minfu Xu, Wesley Wayman, John Woodward
Channelrhodopsins are light activated ion channels used extensively over the past decade to probe the function of genetically defined neuronal populations and distinct neural circuits with high temporal and spatial precision. The widely used Channelrhodopsin-2 variant (ChR2) is an excitatory opsin that undergoes conformational changes in response to blue light, allowing non-selective passage of protons and cations across the plasma membrane thus leading to depolarization. In the addiction neuroscience field, opsins such as ChR2 provide a means to disambiguate the overlapping circuitry involved in mediating the reinforcing and aversive effects of drugs of abuse as well as to determine the plasticity that can occur in these circuits during the development of dependence...
March 23, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29569041/non-invasive-multimodality-imaging-directly-shows-trpm4-inhibition-ameliorates-stroke-reperfusion-injury
#5
Bo Chen, Gandi Ng, Yahui Gao, See Wee Low, Edwin Sandanaraj, Boominathan Ramasamy, Sakthivel Sekar, Kishore Bhakoo, Tuck Wah Soong, Bernd Nilius, Carol Tang, Edward G Robins, Julian Goggi, Ping Liao
The transient receptor potential melastatin 4 (TRPM4) channel has been suggested to play a key role in the treatment of ischemic stroke. However, in vivo evaluation of TRPM4 channel, in particular by direct channel suppression, is lacking. In this study, we used multimodal imaging to assess edema formation and quantify the amount of metabolically functional brain salvaged after a rat model of stroke reperfusion. TRPM4 upregulation in endothelium emerges as early as 2 h post-stroke induction. Expression of TRPM4 channel was suppressed directly in vivo by treatment with siRNA; scrambled siRNA was used as a control...
March 22, 2018: Translational Stroke Research
https://www.readbyqxmd.com/read/29509582/ketamine-action-in-the-in-vitro-cortical-slice-is-mitigated-by-potassium-channel-blockade
#6
Logan J Voss, Sebastian Karalus, Vilhelm Englund, James W Sleigh
BACKGROUND: Ketamine is a general anesthetic thought to act by antagonizing N-methyl-D-aspartate receptors. However, ketamine acts on multiple channels, many of which are potential targets-including hyperpolarization-activated cyclic nucleotide-gated and potassium channels. In this study we tested the hypothesis that potassium leak channels contribute to the anesthetic action of ketamine. METHODS: Adult mouse cortical slices (400 µm) were exposed to no-magnesium artificial cerebrospinal fluid to generate seizure-like event activity...
June 2018: Anesthesiology
https://www.readbyqxmd.com/read/29500929/mapping-ligand-binding-pockets-in-chloride-clc-1-channels-through-an-integrated-in-silico-and-experimental-approach-using-anthracene-9-carboxylic-acid-and-niflumic-acid
#7
C Altamura, G F Mangiatordi, O Nicolotti, D Sahbani, A Farinato, F Leonetti, M R Carratù, D Conte, J-F Desaphy, P Imbrici
BACKGROUND AND PURPOSE: Although chloride channels are involved in several physiological processes and acquired diseases, the availability of compounds selectively targeting CLC proteins is limited. ClC-1 channels are responsible for sarcolemma repolarization after an action potential in skeletal muscle and have been associated with myotonia congenita and myotonic dystrophy as well as with other muscular physiopathological conditions. To date only a few ClC-1 blockers have been discovered, such as anthracene-9-carboxylic acid (9-AC) and niflumic acid (NFA), whereas no activator exists...
May 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29475947/functional-organization-of-cytoplasmic-portals-controlling-access-to-the-cystic-fibrosis-transmembrane-conductance-regulator-cftr-chloride-channel-pore
#8
Man-Song Li, Elizabeth A Cowley, Yassine El Hiani, Paul Linsdell
The cystic fibrosis transmembrane conductance regulator (CFTR) is a Cl- channel that apparently has evolved from an ancestral active transporter. Key to the CFTR's switch from pump to channel function may have been the appearance of one or more "lateral portals." Such portals connect the cytoplasm to the transmembrane channel pore, allowing a continuous pathway for the electrodiffusional movement of Cl- ions. However, these portals remain the least well-characterized part of the Cl- transport pathway; even the number of functional portals is uncertain, and if multiple portals do exist, their relative functional contributions are unknown...
April 13, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29449621/polygonum-aviculare-l-extract-and-quercetin-attenuate-contraction-in-airway-smooth-muscle
#9
Xi Luo, Lu Xue, Hao Xu, Qing-Yang Zhao, Qian Wang, Yu-Shan She, Dun-An Zang, Jinhua Shen, Yong-Bo Peng, Ping Zhao, Meng-Fei Yu, Weiwei Chen, Li-Qun Ma, Shu Chen, Shanshan Chen, Xiangning Fu, Sheng Hu, Xiaowei Nie, Chenyou Shen, Chunbin Zou, Gangjian Qin, Jiapei Dai, Guangju Ji, Yunchao Su, Shen Hu, Jingyu Chen, Qing-Hua Liu
Because of the serious side effects of the currently used bronchodilators, new compounds with similar functions must be developed. We screened several herbs and found that Polygonum aviculare L. contains ingredients that inhibit the precontraction of mouse and human airway smooth muscle (ASM). High K+ -induced precontraction in ASM was completely inhibited by nifedipine, a selective blocker of L-type voltage-dependent Ca2+ channels (LVDCCs). However, nifedipine only partially reduced the precontraction induced by acetylcholine chloride (ACH)...
February 15, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29444316/glucose-triggers-stomatal-closure-mediated-by-basal-signaling-through-hxk1-and-pyr-rcar-receptors-in-arabidopsis
#10
Yan Li, Shanshan Xu, Zhiwei Wang, Lingchao He, Kang Xu, Genxuan Wang
Sugars play important roles in regulating plant growth, development, and stomatal movement. Here, we found that glucose triggered stomatal closure in a dose- and time-dependent manner in Arabidopsis. Pharmacological data showed that glucose-induced stomatal closure was greatly inhibited by catalase [CAT; a reactive oxygen species (ROS) scavenger], diphenyleneiodonium chloride (DPI; an NADPH oxidase inhibitor), lanthanum chloride (LaCl3; a Ca2+ channel blocker), EGTA (a Ca2+ chelator), and two nitrate reductase (NR) inhibitors, tungstate and sodium azide (NaN3), while it was not affected by salicylhydroxamic acid (SHAM; a peroxidase inhibitor)...
March 24, 2018: Journal of Experimental Botany
https://www.readbyqxmd.com/read/29430647/the-cells-and-conductance-mediating-cholinergic-neurotransmission-in-the-murine-proximal-stomach
#11
Tae Sik Sung, Sung Jin Hwang, Sang Don Koh, Yulia Bayguinov, Lauen E Peri, Peter J Blair, Timothy I Webb, David M Pardo, Jason R Rock, Kenton M Sanders, Sean M Ward
KEY POINTS: Enteric neurotransmission is essential for gastrointestinal (GI) motility, although the cells and conductances responsible for post-junctional responses are controversial. The calcium-activated chloride conductance (CaCC), anoctamin-1 (Ano1), was expressed by intramuscular interstitial cells of Cajal (ICC-IM) in proximal stomach and not resolved in smooth muscle cells (SMCs). Cholinergic nerve fibres were closely apposed to ICC-IM. Conductances activated by cholinergic stimulation in isolated ICC-IM and SMCs were determined...
May 1, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29427588/hyperpolarization-by-n-3-oxododecanoyl-l-homoserine-lactone-a-quorum-sensing-molecule-in-rat-thymic-lymphocytes
#12
Yumiko Nishimura-Danjobara, Keisuke Oyama, Kumio Yokoigawa, Yasuo Oyama
To study the adverse effects of N-(3-oxododecanoyl)-l-homoserine-lactone (ODHL), a quorum sensing molecule, on mammalian host cells, its effect on membrane potential was examined in rat thymic lymphocytes using flow cytometric techniques with a voltage-sensitive fluorescent probe. As 3-300 μM ODHL elicited hyperpolarization, it is likely that it increases membrane K+ permeability because hyperpolarization is directly linked to changing K+ gradient across membranes, but not Na+ and Cl- gradients. ODHL did not increase intracellular Ca2+ concentration...
March 1, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29421809/a-potassium-selective-current-affected-by-micromolar-concentrations-of-anion-transport-inhibitors
#13
Roberta Costa, Davide Antonio Civello, Emanuele Bernardinelli, Simone Vanoni, Michaela Zopf, Giada Scantamburlo, Charity Nofziger, Wolfgang Patsch, Markus Paulmichl, Silvia Dossena
BACKGROUND/AIMS: In the human genome, more than 400 genes encode ion channels, which are ubiquitously expressed and often coexist and participate in almost all physiological processes. Therefore, ion channel blockers represent fundamental tools in discriminating the contribution of individual channel types to a physiological phenomenon. However, unspecific effects of these compounds may represent a confounding factor. Three commonly used chloride channel inhibitors, i.e. 4,4'-diisothiocyano-2,2'-stilbene-disulfonic acid (DIDS), 5-nitro-2-[(3-phenylpropyl) amino]benzoic acid (NPPB) and the anti-inflammatory drug niflumic acid were tested to identify the lowest concentration effective on Cl- channels and ineffective on K+ channels...
2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29415993/evaluation-of-autophagy-inducers-in-epithelial-cells-carrying-the-%C3%AE-f508-mutation-of-the-cystic-fibrosis-transmembrane-conductance-regulator-cftr
#14
Shaoyi Zhang, Gautier Stoll, José Manuel Bravo San Pedro, Valentina Sica, Allan Sauvat, Florine Obrist, Oliver Kepp, Yousheng Li, Luigi Maiuri, Naoufal Zamzami, Guido Kroemer
Cystic Fibrosis (CF) due to the ΔF508 mutation of cystic fibrosis transmembrane conductance regulator (CFTR) can be treated with a combination of cysteamine and Epigallocatechin gallate (EGCG). Since ECGC is not a clinically approved drug, we attempted to identify other compounds that might favourably interact with cysteamine to induce autophagy and thus rescuing the function of ΔF508 CFTR as a chloride channel in the plasma membrane. For this, we screened a compound library composed by chemically diverse autophagy inducers for their ability to enhance autophagic flux in the presence of cysteamine...
February 7, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29411605/investigation-of-agonist-recognition-and-channel-properties-in-a-flatworm-glutamate-gated-chloride-channel
#15
Daniel Callau-Vázquez, Stephan A Pless, Timothy Lynagh
Glutamate-gated chloride channels (GluCls) are neurotransmitter receptors that mediate crucial inhibitory signaling in invertebrate neuromuscular systems. Their role in invertebrate physiology and their absence from vertebrates make GluCls a prime target for antiparasitic drugs. GluCls from flatworm parasites are substantially different from and are much less understood than those from roundworm and insect parasites, hindering the development of potential therapeutics targeting GluCls in flatworm-related diseases such as schistosomiasis...
February 27, 2018: Biochemistry
https://www.readbyqxmd.com/read/29356280/potential-role-of-potassium-and-chloride-channels-in-regulation-of-silymarin-induced-apoptosis-in-candida-albicans
#16
Wonjong Lee, Dong Gun Lee
Silymarin, which is derived from the seeds of Silybum marianum, has been widely used to prevent and treat liver diseases. In our previous study, we reported that at concentrations above the minimal inhibitory concentration (MIC), silymarin exhibited antifungal activity against Candida albicans by targeting its plasma membrane. However, the antifungal mechanism at concentration below the MIC remains unknown. Therefore, we aimed to determine the underlying mechanism of antifungal effects of silymarin at concentration below the MIC...
March 2018: IUBMB Life
https://www.readbyqxmd.com/read/29344669/clc-2-is-a-positive-modulator-of-oligodendrocyte-precursor-cell-differentiation-and-myelination
#17
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
#18
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...
March 2018: 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
#19
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...
April 2018: 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
#20
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...
June 2018: Journal of Cellular Physiology
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