Tetrodotoxin
Chemical Name: (4R,4aR,5R,7S,9S,10S,10aR,11S,12S)-Octahydro-12-(hydroxymethyl)-2-imino-5,9:7,10a-dimethano-10aH-[1,3]dioxocino[6,5-d]pyrimidine-4,7,10,11,12-pentol
Purity: ≥98%
Biological Activity
Tetrodotoxin is a reversible, potent, selective and high affinity inhibitor of voltage gated sodium channels Nav 1.6, 1.1, 1.3, 1.4, 1.2 and 1.7 (IC50 values are 2.3 nM, 4.1 nM, 5.3 nM, 7.6 nM, 14 nM and 36 nM, respectively). Binding is reversible and high affinity (Kd = 1-10 nM). Tetrodotoxin shows antagonism of aconitine-induced cardiac toxicity, analgesic effects in mouse models of neuropathy and prolonged duration of local anesthesia in animals when combined with capsaicin. Tetrodotoxin also shows pH-dependent blockade of canine cardiac L-type Ca2+ (Cav1.x) channels, blocks primary reward in an animal study of drug-seeking lever pressing.Tetrodotoxin citrate (Cat. No. 1069) also available.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Citations for Tetrodotoxin
The citations listed below are publications that use Tocris products. Selected citations for Tetrodotoxin include:
338 Citations: Showing 1 - 10
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The orexigenic effect of ghrelin is mediated through central activation of the endogenous cannabinoid system.
Authors: Kola Et al.
Proc Natl Acad Sci U S A ;3:e1797
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Voltage-gated potassium channels ensure action potential shape fidelity in distal axons.
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J Neurosci 2021;41:5372
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Oxytocin Shapes Spontaneous Activity Patterns in the Developing Visual Cortex by Activating Somatostatin Interneurons.
Authors: Maldonado Et al.
Curr Biol 2021;31:322
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Axonal mechanisms mediating γ-aminobutyric acid receptor type A (GABA-A) inhibition of striatal dopamine release.
Authors: Kramer Et al.
ELIfe 2020;9
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TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations
Authors: O'Malley Et al.
J Neurosci 2020;40:4813
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Functional Dissection of Basal Ganglia Inhibitory Inputs onto Substantia Nigra Dopaminergic Neurons.
Authors: Evans Et al.
Cell Rep 2020;32
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Polysynaptic inhibition between striatal cholinergic interneurons shapes their network activity patterns in a dopamine-dependent manner.
Authors: Dorst Et al.
Nat Commun 2020;11:5113
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GABARAPs dysfunction by autophagy deficiency in adolescent brain impairs GABAA receptor trafficking and social behavior.
Authors: Hui Et al.
Sci Adv 2019;5:eaau8237
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Structures of human Nav1.7 channel in complex with auxiliary subunits and animal toxins.
Authors: Shen Et al.
Science 2019;363:1303
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Differences in glutamate uptake between cortical regions impact neuronal NMDA receptor activation.
Authors: Romanos Et al.
Commun Biol 2019;2:127
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NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
Authors: Chiu Et al.
Cell Rep 2019;28:332
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Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference.
Authors: Nam Et al.
Cell Rep 2019;28:1154
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Aquaporin-4 Surface Trafficking Regulates Astrocytic Process Motility and Synaptic Activity in Health and Autoimmune Disease.
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Cell Rep 2019;27:3860
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An Autaptic Culture System for Standardized Analyses of iPSC-Derived Human Neurons.
Authors: Rhee Et al.
Cell Rep 2019;27:2212
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Synergistic Nigral Output Pathways Shape Movement.
Authors: Rizzi and Tan
Cell Rep 2019;27:2184
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Homeostatic Intrinsic Plasticity Is Functionally Altered in Fmr1 KO Cortical Neurons.
Authors: Bülow Et al.
Cell Rep 2019;26:1378
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Sex-regulated gene dosage effect of PPARα on synaptic plasticity.
Authors: Pierrot Et al.
Life Sci Alliance 2019;2
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KA metabolite (2R,6R)-hydroxynorKA enhances aggression via periaqueductal gray glutamatergic transmission.
Authors: Ye Et al.
Neuropharmacology 2019;157
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HIV gp120 upregulates tonic inhibition through α5-containing GABAARs.
Authors: Green and Thayer Et al.
Neuropharmacology 2019;149:161
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Myosin XVI Regulates Actin Cytoskeleton Dynamics in Dendritic Spines of Purkinje Cells and Affects Presynaptic Organization.
Authors: Roesler Et al.
Front Cell Neurosci 2019;13:330
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Prenatal selective serotonin reuptake inhibitor (SSRI) exposure induces working memory and social recognition deficits by disrupting inhibitory synaptic networks in male mice.
Authors: Yu Et al.
Mol Brain 2019;12:29
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Class IIa HDACs regulate learning and memory through dynamic experience-dependent repression of transcription.
Authors: Zhu Et al.
Nat Commun 2019;10:3469
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Neural mechanisms of contextual modulation in the retinal direction selective circuit.
Authors: Huang Et al.
Nat Commun 2019;10:2431
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Evidence Supports Tradition: The in Vitro Effects of Roman Chamomile on Smooth Muscles.
Authors: Sándor Et al.
Front Pharmacol 2018;9:323
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The CaMKII/NMDA receptor complex controls hippocampal synaptic transmission by kinase-dependent and independent mechanisms.
Authors: Incontro
Nat Commun 2018;9:2069
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Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation.
Authors: Zhang Et al.
Neuron 2018;98:918
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Hypothalamic Circuits for Predation and Evasion.
Authors: Li Et al.
Neuron 2018;97:911
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The Microglial Innate Immune Receptor TREM2 Is Required for Synapse Elimination and Normal Brain Connectivity.
Authors: Filipello Et al.
Immunity 2018;48:979
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Role of Sympathetic Nerves and Adipocyte Catecholamine Uptake in the Vasorelaxant Function of Perivascular Adipose Tissue.
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Arterioscler Thromb Vasc Biol 2018;38:880
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Retinoic Acid Receptor RARα-Dependent Synaptic Signaling Mediates Homeostatic Synaptic Plasticity at the Inhibitory Synapses of Mouse Visual Cortex.
Authors: Zhong Et al.
J Neurosci 2018;38:10454
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AKAP150 Palmitoylation Regulates Synaptic Incorporation of Ca2+-Permeable AMPA Receptors to Control LTP.
Authors: Purkey Et al.
Cell Rep 2018;25:974
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Calcium Channel CaV2.3 Subunits Regulate Hepatic Glucose Production by Modulating Leptin-Induced Excitation of Arcuate Pro-opiomelanocortin Neurons.
Authors: Smith Et al.
Cell Rep 2018;25:278
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The locus coeruleus drives disinhibition in the midline thalamus via a dopaminergic mechanism.
Authors: Beas Et al.
Nat Neurosci 2018;21:963
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All-optical synaptic electrophysiology probes mechanism of KA-induced disinhibition.
Authors: Fan Et al.
Nat Methods 2018;15:823
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Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons.
Authors: Fernandez-Fernandez Et al.
PLoS One 2018;13:e0199282
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OXT Relieves Neuropathic Pain Through GABA Release and Presynaptic TRPV1 Inhibition in Spinal Cord.
Authors: Sun Et al.
Front Mol Neurosci 2018;11:248
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Heterophilic Type II Cadherins Are Required for High-Magnitude Synaptic Potentiation in the Hippocampus.
Authors: Basu Et al.
Neuron 2017;96:160
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LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance.
Authors: Hashimotodani Et al.
Neuron 2017;95:928
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Molecular Mechanisms of Synaptic Vesicle Priming by Munc13 and Munc18.
Authors: Lai Et al.
Neuron 2017;95:591
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A Central Catecholaminergic Circuit Controls Blood Glucose Levels during Stress.
Authors: Zhao Et al.
Neuron 2017;95:138
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IGF1-Dependent Synaptic Plasticity of Mitral Cells in Olfactory Memory during Social Learning.
Authors: Liu Et al.
Neuron 2017;95:106
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CaMKII Autophosphorylation Is Necessary for Optimal Integration of Ca2+ Signals during LTP Induction, but Not Maintenance.
Authors: Chang Et al.
Neuron 2017;94:800
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The Retromer Supports AMPA Receptor Trafficking During LTP.
Authors: Temkin Et al.
Neuron 2017;94:74
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Formation and Maintenance of Functional Spines in the Absence of Presynaptic Glutamate Release.
Authors: Sigler Et al.
Neuron 2017;94:304
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An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes.
Authors: McKeithan Et al.
Front Physiol 2017;8:766
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Distal axotomy enhances retrograde presynaptic excitability onto injured pyramidal neurons via trans-synaptic signaling.
Authors: Nagendran Et al.
Nat Commun 2017;8:625
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Inhibition of late sodium current suppresses calcium-related ventricular arrhythmias by reducing the phosphorylation of CaMK-II and sodium channel expressions.
Authors: Wei Et al.
Sci Rep 2017;7:981
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On-demand optogenetic activation of human stem-cell-derived neurons.
Authors: Klapper Et al.
Sci Rep 2017;7:14450
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A Co-culture Model for Determining the Target Specificity of the de novo Generated Retinal Ganglion Cells.
Authors: Teotia Et al.
Bio Protoc 2017;7
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Molecular basis of ancestral vertebrate electroreception.
Authors: Bellono
Nature 2017;543:391
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The RNA-Binding Protein hnRNP K Mediates the Effect of BDNF on Dendritic mRNA Metabolism and Regulates Synaptic NMDA Receptors in Hippocampal Neurons.
Authors: Leal Et al.
Eneuro 2017;4
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GluA1 subunit ubiquitination mediates amyloid-β-induced loss of surface α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors.
Authors: Guntupalli Et al.
J Biol Chem 2017;292:8186
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Synaptic Activity Drives a Genomic Program That Promotes a Neuronal Warburg Effect.
Authors: Bas-Orth Et al.
J Biol Chem 2017;292:5183
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Src homology 2 domain-containing phosphotyrosine phosphatase 2 (Shp2) controls surface GluA1 protein in synaptic homeostasis.
Authors: Zhang and Lu
J Biol Chem 2017;292:15481
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GLP-1 acts on habenular avoidance circuits to control nicotine intake.
Authors: Tuesta
Nat Neurosci 2017;20(5):708
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Posttranslational modification impact on the mechanism by which amyloid-β induces synaptic dysfunction.
Authors: Grochowska Et al.
EMBO Rep 2017;18:962
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Transcriptional Architecture of Synaptic Communication Delineates GABAergic Neuron Identity.
Authors: Paul Et al.
Cell 2017;171:522
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Ion channel expression patterns in glioblastoma stem cells with functional and therapeutic implications for malignancy.
Authors: Pollak Et al.
PLoS One 2017;12:e0172884
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Striatopallidal dysfunction underlies repetitive behavior in Shank3-deficient model of autism.
Authors: Wang Et al.
J Clin Invest 2017;127:1978
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Methylene blue inhibits GABAA receptors by interaction with GABA binding site.
Authors: Chen
Neuropharmacology 2017;119:100
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Targeted Intron Retention and Excision for Rapid Gene Regulation in Response to Neuronal Activity.
Authors: Mauger Et al.
Neuron 2016;92:1266
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Extra-coding RNAs regulate neuronal DNA methylation dynamics.
Authors: Savell Et al.
Nat Commun 2016;7:12091
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BK channel inactivation gates daytime excitability in the circadian clock.
Authors: Whitt Et al.
Nat Commun 2016;7:10837
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M1 ipRGCs Influence Visual Function through Retrograde Signaling in the Retina
Authors: Prigge Et al.
The Journal of Neuroscience 2016;6:7184
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High-throughput compound evaluation on 3D networks of neurons and glia in a microfluidic platform.
Authors: Wevers Et al.
Sci Rep 2016;6:38856
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The chemokine CXCL16 modulates neurotransmitter release in hippocampal CA1 area.
Authors: Di Castro Et al.
Scientific Reports 2016;6:34633
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Increased GABAB receptor signaling in a rat model for schizophrenia.
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Scientific Reports 2016;6:34240
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DArgic neurons differentiating from LRRK2 G2019S induced pluripotent stem cells show early neuritic branching defects.
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Scientific Reports 2016;6:33377
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Dopaminergic neurons differentiating from LRRK2 G2019S induced pluripotent stem cells show early neuritic branching defects
Authors: Borgs Et al.
Scientific Reports 2016;6:33377
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Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.
Authors: Colavita Et al.
Sci Rep 2016;6:28454
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Effects of ε-viniferin, a dehydrodimer of resveratrol, on transepithelial active ion transport and ion permeability in the rat small and large intestinal mucosa.
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Physiol Rep 2016;4
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Compartmentalized PDE4A5 Signaling Impairs Hippocampal Synaptic Plasticity and Long-Term Memory.
Authors: Havekes Et al.
J Neurosci 2016;36:8936
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The First Alcohol Drink Triggers mTORC1-Dependent Synaptic Plasticity in Nucleus Accumbens DA D1 Receptor Neurons.
Authors: Beckley Et al.
J Neurosci 2016;36:701
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17β-OE Acutely Potentiates Glutamatergic Synaptic Transmission in the Hippocampus through Distinct Mechanisms in Males and Females.
Authors: Oberlander
J Neurosci 2016;36:2677
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Tau-Driven Neuronal and Neurotrophic Dysfunction in a Mouse Model of Early Tauopathy.
Authors: Mazzaro Et al.
J Neurosci 2016;36:2086
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Cell-Autonomous Regulation of Dendritic Spine Density by PirB.
Authors: Vidal Et al.
Eneuro 2016;3
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Voltage Dependence of a Neuromodulator-Activated Ionic Current.
Authors: Gray and Golowasch
Eneuro 2016;3
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Increased Activity of Src Homology 2 Domain Containing Phosphotyrosine Phosphatase 2 (Shp2) Regulates Activity-dependent AMPA Receptor Trafficking.
Authors: Zhang Et al.
J Biol Chem 2016;291:18856
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Increasing the Receptor Tyrosine Kinase EphB2 Prevents Amyloid-β-induced Depletion of Cell Surface Glutamate Receptors by a Mechanism That Requires the PDZ-binding Motif of EphB2 and Neuronal Activity.
Authors: Miyamoto Et al.
PLoS Pathog 2016;291:1719
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Reduced Hyperpolarization-Activated Current Contributes to Enhanced Intrinsic Excitability in Cultured Hippocampal Neurons from PrP(-/-) Mice.
Authors: Fan Et al.
Front Cell Neurosci 2016;10:74
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Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells.
Authors: Elgueta Et al.
Physiol Rep 2015;9:6
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The Shaping of Two Distinct Dendritic Spikes by A-Type Voltage-Gated K(+) Channels.
Authors: Yang Et al.
Ann Clin Transl Neurol 2015;9:469
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NE Modulates Pyramidal Cell Synaptic Properties in the Anterior Piriform Cortex of Mice: Age-Dependent Effects of β-adrenoceptors.
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Cell Rep 2015;9:450
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Dendritic morphology, synaptic transmission, and activity of mature granule cells born following PilC-induced status epilepticus in the rat.
Authors: Gao Et al.
J Neurosci 2015;9:384
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Cell-type-specific tuning of Cav1.3 Ca(2+)-channels by a C-terminal automodulatory domain.
Authors: Scharinger Et al.
J Cell Biol 2015;9:309
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An excitatory GABA loop operating in vivo.
Authors: Astorga Et al.
Front Cell Neurosci 2015;9:275
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Inhibitory effects of endomorphin-2 on excitatory synaptic transmission and the neuronal excitability of sacral parasympathetic preganglionic neurons in young rats.
Authors: Chen Et al.
J Neurosci 2015;9:206
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Channel-mediated astrocytic glutamate modulates hippocampal synaptic plasticity by activating postsynaptic NMDA receptors.
Authors: Park Et al.
J Biomed Sci 2015;8:7
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Regulation of STEP61 and tyrosine-phosphorylation of NMDA and AMPA receptors during homeostatic synaptic plasticity.
Authors: Jang Et al.
Mol Brain 2015;8:55
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Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia.
Authors: Campbell Et al.
J Neurosci 2015;8:425
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N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity.
Authors: Lee Et al.
J Neurosci 2015;8:4
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Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity.
Authors: Pál Et al.
Front Cell Neurosci 2015;8:35
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Genetic targeting of NRXN2 in mice unveils role in excitatory cortical synapse function and social behaviors.
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Mol Brain 2015;7:3
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No evidence for a culturable bacterial tetrodotoxin producer in Pleurobranchaea maculata (Gastropoda: Pleurobranchidae) and Stylochoplana sp. (Platyhelminthes: Polycladida).
Authors: Salvitti Et al.
Toxins (Basel) 2015;7:255
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Novel RNA- and FMRP-binding protein TRF2-S regulates axonal mRNA transport and presynaptic plasticity.
Authors: Zhang Et al.
J Neurosci 2015;6:8888
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Optical control of NMDA receptors with a diffusible photoswitch.
Authors: Laprell Et al.
Sci Rep 2015;6:8076
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Synaptic GABA release prevents GABA transporter type-1 reversal during excessive network activity.
Authors: Savtchenko Et al.
PLoS One 2015;6:6597
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Subventricular zone neural progenitors reverse TNF-α effects in cortical neurons.
Authors: Morini Et al.
Front Cell Neurosci 2015;6:166
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MicroRNA miR124 is required for the expression of homeostatic synaptic plasticity.
Authors: Hou Et al.
Nat Commun 2015;6:10045
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Synaptic structure and function are altered by the neddylation inhibitor MLN4924.
Authors: Scudder and Patrick
Mol Cell Neurosci 2015;65:52
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Optogenetic induction of contractile ability in immature C2C12 myotubes.
Authors: Asano Et al.
Curr Mol Med 2015;5:8317
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Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranol.
Authors: Virsolvy Et al.
Nat Commun 2015;5:17969
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Modulation of AMPA receptor mediated current by nicotinic acetylcholine receptor in layer I neurons of rat prefrontal cortex.
Authors: Tang Et al.
Stem Cells 2015;5:14099
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Spexin Enhances Bowel Movement through Activating L-type Voltage-dependent Calcium Channel via Galanin Receptor 2 in Mice.
Authors: Lin Et al.
Sci Rep 2015;5:12095
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Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
Authors: Saunders Et al.
Sci Rep 2015;4
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Autism-Associated Insertion Mutation (InsG) of Shank3 Exon 21 Causes Impaired Synaptic Transmission and Behavioral Deficits.
Authors: Speed Et al.
J Neurosci 2015;35:9648
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Disruption of Fgf13 causes synaptic excitatory-inhibitory imbalance and genetic epilepsy and febrile seizures plus.
Authors: Puranam Et al.
Mol Brain 2015;35:8866
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Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo.
Authors: Sivakumaran Et al.
Nat Commun 2015;35:8291
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Inhibitory Interneurons That Express GFP in the PrP-GFP Mouse Spinal Cord Are Morphologically Heterogeneous, Innervated by Several Classes of Primary Afferent and Include Lamina I Projection Neurons among Their Postsynaptic Targets.
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Front Synaptic Neurosci 2015;35:7626
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Cholinergic control of γ power in the midbrain spatial attention network.
Authors: Bryant Et al.
Mol Brain 2015;35:761
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Single-Molecule Imaging of PSD-95 mRNA Translation in Dendrites and Its Dysregulation in a Mouse Model of Fragile X Syndrome.
Authors: Ifrim Et al.
Nat Neurosci 2015;35:7116
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Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse.
Authors: Cramer Et al.
Mol Cell Biol 2015;35:5664
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BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain DA neurons.
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J Neurosci 2015;35:4469
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Dual-channel circuit mapping reveals sensorimotor convergence in the primary motor cortex.
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Front Cell Neurosci 2015;35:4418
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Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP.
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J Neurosci 2015;35:3016
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Modulation of microglial process convergence toward neuronal dendrites by extracellular calcium.
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J Neurosci 2015;35:2417
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Protein kinase C-dependent growth-associated protein 43 phosphorylation regulates gephyrin aggregation at developing GABAergic synapses.
Authors: Wang Et al.
PLoS One 2015;35:1712
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Miro1 Regulates Activity-Driven Positioning of Mitochondria within Astrocytic Processes Apposed to Synapses to Regulate Intracellular Calcium Signaling.
Authors: Stephen Et al.
Nat Commun 2015;35:15996
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Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro.
Authors: Sobieski Et al.
J Neurosci 2015;35:11105
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Combination of miRNA499 and miRNA133 exerts a synergic effect on cardiac differentiation.
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Biomed Res Int 2015;33:1187
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Neural control of submucosal gland and apical membrane secretions in airways.
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Oncotarget 2015;3
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D.pam effect during early neonatal development correlates with neuronal Cl(.).
Authors: Glykys and Staley
J Cell Sci 2015;2:1055
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Soluble epoxide hydrolase inhibitor enhances synaptic neurotransmission and plasticity in mouse prefrontal cortex.
Authors: Wu Et al.
Front Cell Neurosci 2015;22:94
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Tau reduction prevents Aβ-induced axonal transport deficits by blocking activation of GSK3β.
Authors: Vossel Et al.
Elife 2015;209:419
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Biological Activities of Tetrodotoxin-Producing Enterococcus faecium AD1 Isolated from Puffer Fishes.
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Front Cell Neurosci 2015;2015:973235
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Early depolarizing GABA controls critical-period plasticity in the rat visual cortex.
Authors: Deidda Et al.
J Neurosci 2015;18:87
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Clinical utility of neuronal cells directly converted from fibroblasts of patients for neuropsychiatric disorders: studies of lysosomal storage diseases and channelopathy.
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