Tetrodotoxin citrate
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 citrate
Purity: ≥98%
Biological Activity
Tetrodotoxin citrate, the water-soluble citrate salt of 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 (Cat. No. 1078) 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.
Additional Information
Background References
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Citations for Tetrodotoxin citrate
The citations listed below are publications that use Tocris products. Selected citations for Tetrodotoxin citrate include:
74 Citations: Showing 1 - 10
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An in vitro model for studying CNS white matter: functional properties and experimental approaches.
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F1000Res 2019;8:117
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Pharmacological Dissection of Intrinsic Optical Signal Reveals a Functional Coupling between Synaptic Activity and Astrocytic Volume Transient.
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Enhancer Histone Acetylation Modulates Transcriptional Bursting Dynamics of Neuronal Activity-Inducible Genes.
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Cell Rep 2019;26:1174
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KCC2-Mediated Cl- Extrusion Modulates Spontaneous Hippocampal Network Events in Perinatal Rats and Mice.
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Cell Rep 2019;26:1073
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Cholinergic neural activity directs retinal layer-specific angiogenesis and blood retinal barrier formation.
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Nat Commun 2019;10:2477
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Soluble TREM2 ameliorates pathological phenotypes by modulating microglial functions in an Alzheimer's disease model.
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Nat Commun 2019;10:1365
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Neuron 2019;
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PACAP Neurons in the Ventromedial Hypothalamic Nucleus Are Glucose Inhibited and Their Selective Activation Induces Hyperglycaemia.
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Front Endocrinol (Lausanne) 2018;9:632
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Pathway-specific alterations of cortico-amygdala transmission in an arthritis pain model.
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Reciprocal Circuits Linking the Prefrontal Cortex with Dorsal and Ventral Thalamic Nuclei.
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Neuron 2018;98:366
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The Temporal Dynamics of Arc Expression Regulate Cognitive Flexibility.
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Neuron 2018;98:1124
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Recurrent Circuitry for Balancing Sleep Need and Sleep.
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Neuron 2018;97:378
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Selective Role of RGS9-2 in Regulating Retrograde Synaptic Signaling of Indirect Pathway Medium Spiny Neurons in Dorsal Striatum.
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J Neurosci 2018;38:7120
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A role for proteolytic regulation of δ-catenin in remodeling a subpopulation of dendritic spines in the rodent brain.
Authors: Yuan Et al.
J Biol Chem 2018;293:11625
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The Developmental Shift of NMDA Receptor Composition Proceeds Independently of GluN2 Subunit-Specific GluN2 C-Terminal Sequences.
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Cell Rep 2018;25:841
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Heparan Sulfate Organizes Neuronal Synapses through Neurexin Partnerships.
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Cell 2018;174:1450
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Dendritic Integration of Sensory Evidence in Perceptual Decision-Making.
Authors: Groschner Et al.
Cell 2018;173:894
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Differential contribution of Ca2+ sources to day and night BK current activation in the circadian clock.
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J Gen Physiol 2018;150:259
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(2R,6R)-hydroxynorKA rescues chronic stress-induced depression-like behavior through its actions in the midbrain periaqueductal gray.
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Neuropharmacology 2018;139:1
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Subcellular Localization and Activity of TRPM4 in Medial Prefrontal Cortex Layer 2/3.
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Front Cell Neurosci 2018;12:12
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Formation and Maintenance of Functional Spines in the Absence of Presynaptic Glutamate Release.
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Neuron 2017;94:304
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Optogenetic Modulation of Urinary Bladder Contraction for Lower Urinary Tract Dysfunction.
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Sci Rep 2017;7:40872
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GLP-2 promotes gallbladder refilling via a TGR5-independent, GLP-2R-dependent pathway.
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Mol Metab 2017;6:503
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J Neurosci 2017;37:8688
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Differential Desensitization Observed at Multiple Effectors of Somatic μ-Opioid Receptors Underlies Sustained Agonist-Mediated Inhibition of Proopiomelanocortin Neuron Activity.
Authors: Fox and Hentges
J Neurosci 2017;37:8667
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Activation of cortical somatostatin interneurons prevents the development of neuropathic pain.
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Nat Neurosci 2017;20:1122
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RNA polymerase II primes Polycomb-repressed developmental genes throughout terminal neuronal differentiation.
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Mol Syst Biol 2017;13:946
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A Model-Based Approach for Separating the Cochlear Microphonic from the Auditory Nerve Neurophonic in the Ongoing Response Using Electrocochleography.
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Front Neurosci 2017;11:592
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FHF-independent conduction of action potentials along the leak-resistant cerebellar granule cell axon.
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Nat Commun 2016;7:12895
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Scientific Reports 2016;6:34633
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Cortico-fugal output from visual cortex promotes plasticity of innate motor behaviour.
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PLoS One 2015;9:409
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Fmrp targets or not: long, highly brain-expressed genes tend to be implicated in autism and brain disorders.
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Mol Autism 2015;6:16
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Branch-specific dendritic Ca(2+) spikes cause persistent synaptic plasticity.
Authors: Cichon and Gan
Nature 2015;520:180
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Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
Authors: Brown and Wonnacott
Gastroenterology 2015;40:2047
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Muscarinic receptors modulate dendrodendritic inhibitory synapses to sculpt glomerular output.
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J Neurophysiol 2015;35:5680
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The Cancer Chemotherapeutic PacT. Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4.
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J Neurosci 2015;35:13487
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Benchmarking the stability of human detergent-solubilised voltage-gated sodium channels for structural studies using eel as a reference.
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J Neurosci 2015;1848:1545
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Nat Methods 2015;12:411
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Giant ankyrin-G stabilizes somatodendritic GABAergic synapses through opposing endocytosis of GABAA receptors.
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Front Cell Neurosci 2015;112:1214
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Assessment of TTX-s and TTX-r Action Potential Conduction along Neurites of NGF and GDNF Cultured Porcine DRG Somata.
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Neurochem Res 2015;10:e0139107
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Neuropharmacology 2014;86:116
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J Neurosci 2014;34:2051
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Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium.
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Br J Pharmacol 2014;171:3404
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Dynamic interactions mediated by nonredundant signaling mechanisms couple circadian clock neurons.
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Neuron 2013;80:973
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The activity-dependent transcription factor NPAS4 regulates domain-specific inhibition.
Authors: Bloodgood Et al.
Nature 2013;503:121
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Holographic optogenetic stimulation of patterned neuronal activity for vision restoration.
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Nat Methods 2013;4:1509
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Direct retino-raphe projection alters serotonergic tone and affective behavior.
Authors: Ren Et al.
Neuropsychopharmacology 2013;38:1163
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TRPM2 channels are required for NMDA-induced burst firing and contribute to H(2)O(2)-dependent modulation in substantia nigra pars reticulata GABAergic neurons.
Authors: Lee Et al.
J Neurosci 2013;33:1157
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Mis-expression of the BK K(+) channel disrupts suprachiasmatic nucleus circuit rhythmicity and alters clock-controlled behavior.
Authors: Montgomery Et al.
Am J Physiol Cell Physiol 2013;304:C299
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SHANK3 gene mutations associated with autism facilitate ligand binding to the Shank3 ankyrin repeat region.
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Biochim Biophys Acta 2013;288:26697
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Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus.
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PLoS One 2012;7:e45717
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A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation.
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PLoS One 2012;7:e38312
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In vitro maturation of DArgic neurons derived from mouse embryonic stem cells: implications for transplantation.
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J Neurosci 2012;7:e31999
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Retinal waves coordinate patterned activity throughout the developing visual system.
Authors: Ackman Et al.
Nature 2012;490:219
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Neuregulin directly decreases voltage-gated sodium current in hippocampal ErbB4-expressing interneurons.
Authors: Janssen Et al.
J Neurosci 2012;32:13889
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Increased bursting glutamatergic neurotransmission in an auditory forebrain area of the zebra finch (Taenopygia guttata) induced by auditory stimulation.
Authors: Dagostin Et al.
J Biol Chem 2012;198:705
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5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii.
Authors: Austgen Et al.
PLoS One 2012;108:2292
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Tetrodotoxin sensitivity of the vertebrate cardiac Na+ current.
Authors: Vornanen Et al.
Mar Drugs 2011;9:2409
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Multiple arrhythmic syndromes in a newborn, owing to a novel mutation in SCN5A.
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Can J Physiol Pharmacol 2011;89:723
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Efficient derivation of NPCs, spinal motor neurons and midbrain DArgic neurons from hESCs at 3% oxygen.
Authors: Stacpoole Et al.
Nat Protoc 2011;6:1229
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Regulation of glycine receptor diffusion properties and gephyrin interactions by protein kinase C.
Authors: Specht Et al.
EMBO J 2011;30:3842
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Characteristics of 5-hydroxytryptamine receptors involved in contraction of feline ileal longitudinal smooth muscle.
Authors: Wang Et al.
Korean J Physiol Pharmacol 2011;15:267
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NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+.
Authors: Zemkova Et al.
Endocrinology 2011;152:3842
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Hydrogen sulfide augments synaptic neurotransmission in the nucleus of the solitary tract.
Authors: Austgen Et al.
Mol Brain 2011;106:1822
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Inhibitory network interactions shape the auditory processing of natural communication signals in the songbird auditory forebrain.
Authors: Pinaud Et al.
J Neurophysiol 2008;100:441
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A calcium-activated nonselective cation conductance underlies the plateau potential in rat substantia nigra GABAergic neurons.
Authors: Lee and Tepper
J Neurosci 2007;27:6531
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New transmembrane AMPA receptor regulatory protein isoform, γ-7, differentially regulates AMPA receptors.
Authors: Kato Et al.
J Comp Physiol A Neuroethol Sens Neural Behav Phys 2007;27:4969
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DArgic modulation of spinal neuronal excitability.
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J Neurophysiol 2007;27:13192
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Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon.
Authors: Khan Et al.
Br J Pharmacol 2006;147:607
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Hydrogen sulfide is a novel prosecretory neuromodulator in the Guinea-pig and human colon.
Authors: Schicho Et al.
J Neurosci 2006;131:1542
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