Tetrodotoxin

Catalog # Availability Size / Price Qty
1078/1
Tetrodotoxin | CAS No. 4368-28-9 | Voltage-gated Sodium Channel Blockers
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Description: Na+ channel blocker
Alternative Names: TTx

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%

Product Details
Citations (338)
Supplemental Products
Reviews

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

M.Wt:
319.27
Formula:
C11H17N3O8
Solubility:
Soluble to 3 mM in acidic buffer (pH 4.8)
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
4368-28-9

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.

Background References

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    Tan YW, Zhang SJ, Hoffmann T, Bading H
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  19. Blockade of Na+ channels in pancreatic alpha-cells has antidiabetic effects.
    Dhalla A, Yang M, Ning Y, Kahlig K, Krause M, Rajamani S, Belardinelli L
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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

  1. 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
  2. Voltage-gated potassium channels ensure action potential shape fidelity in distal axons.
    Authors: Sabater Et al.
    J Neurosci  2021;41:5372
  3. Oxytocin Shapes Spontaneous Activity Patterns in the Developing Visual Cortex by Activating Somatostatin Interneurons.
    Authors: Maldonado Et al.
    Curr Biol  2021;31:322
  4. Axonal mechanisms mediating γ-aminobutyric acid receptor type A (GABA-A) inhibition of striatal dopamine release.
    Authors: Kramer Et al.
    ELIfe  2020;9
  5. TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations
    Authors: O'Malley Et al.
    J Neurosci  2020;40:4813
  6. Functional Dissection of Basal Ganglia Inhibitory Inputs onto Substantia Nigra Dopaminergic Neurons.
    Authors: Evans Et al.
    Cell Rep  2020;32
  7. 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
  8. GABARAPs dysfunction by autophagy deficiency in adolescent brain impairs GABAA receptor trafficking and social behavior.
    Authors: Hui Et al.
    Sci Adv  2019;5:eaau8237
  9. Structures of human Nav1.7 channel in complex with auxiliary subunits and animal toxins.
    Authors: Shen Et al.
    Science  2019;363:1303
  10. Differences in glutamate uptake between cortical regions impact neuronal NMDA receptor activation.
    Authors: Romanos Et al.
    Commun Biol  2019;2:127
  11. NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
    Authors: Chiu Et al.
    Cell Rep  2019;28:332
  12. Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference.
    Authors: Nam Et al.
    Cell Rep  2019;28:1154
  13. Aquaporin-4 Surface Trafficking Regulates Astrocytic Process Motility and Synaptic Activity in Health and Autoimmune Disease.
    Authors: Ciappelloni Et al.
    Cell Rep  2019;27:3860
  14. An Autaptic Culture System for Standardized Analyses of iPSC-Derived Human Neurons.
    Authors: Rhee Et al.
    Cell Rep  2019;27:2212
  15. Synergistic Nigral Output Pathways Shape Movement.
    Authors: Rizzi and Tan
    Cell Rep  2019;27:2184
  16. Homeostatic Intrinsic Plasticity Is Functionally Altered in Fmr1 KO Cortical Neurons.
    Authors: Bülow Et al.
    Cell Rep  2019;26:1378
  17. Sex-regulated gene dosage effect of PPARα on synaptic plasticity.
    Authors: Pierrot Et al.
    Life Sci Alliance  2019;2
  18. KA metabolite (2R,6R)-hydroxynorKA enhances aggression via periaqueductal gray glutamatergic transmission.
    Authors: Ye Et al.
    Neuropharmacology  2019;157
  19. HIV gp120 upregulates tonic inhibition through α5-containing GABAARs.
    Authors: Green and Thayer Et al.
    Neuropharmacology  2019;149:161
  20. 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
  21. 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
  22. Class IIa HDACs regulate learning and memory through dynamic experience-dependent repression of transcription.
    Authors: Zhu Et al.
    Nat Commun  2019;10:3469
  23. Neural mechanisms of contextual modulation in the retinal direction selective circuit.
    Authors: Huang Et al.
    Nat Commun  2019;10:2431
  24. Evidence Supports Tradition: The in Vitro Effects of Roman Chamomile on Smooth Muscles.
    Authors: Sándor Et al.
    Front Pharmacol  2018;9:323
  25. The CaMKII/NMDA receptor complex controls hippocampal synaptic transmission by kinase-dependent and independent mechanisms.
    Authors: Incontro
    Nat Commun  2018;9:2069
  26. Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation.
    Authors: Zhang Et al.
    Neuron  2018;98:918
  27. Hypothalamic Circuits for Predation and Evasion.
    Authors: Li Et al.
    Neuron  2018;97:911
  28. The Microglial Innate Immune Receptor TREM2 Is Required for Synapse Elimination and Normal Brain Connectivity.
    Authors: Filipello Et al.
    Immunity  2018;48:979
  29. Role of Sympathetic Nerves and Adipocyte Catecholamine Uptake in the Vasorelaxant Function of Perivascular Adipose Tissue.
    Authors: Saxton Et al.
    Arterioscler Thromb Vasc Biol  2018;38:880
  30. 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
  31. AKAP150 Palmitoylation Regulates Synaptic Incorporation of Ca2+-Permeable AMPA Receptors to Control LTP.
    Authors: Purkey Et al.
    Cell Rep  2018;25:974
  32. 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
  33. The locus coeruleus drives disinhibition in the midline thalamus via a dopaminergic mechanism.
    Authors: Beas Et al.
    Nat Neurosci  2018;21:963
  34. All-optical synaptic electrophysiology probes mechanism of KA-induced disinhibition.
    Authors: Fan Et al.
    Nat Methods  2018;15:823
  35. 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
  36. OXT Relieves Neuropathic Pain Through GABA Release and Presynaptic TRPV1 Inhibition in Spinal Cord.
    Authors: Sun Et al.
    Front Mol Neurosci  2018;11:248
  37. Heterophilic Type II Cadherins Are Required for High-Magnitude Synaptic Potentiation in the Hippocampus.
    Authors: Basu Et al.
    Neuron  2017;96:160
  38. 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
  39. Molecular Mechanisms of Synaptic Vesicle Priming by Munc13 and Munc18.
    Authors: Lai Et al.
    Neuron  2017;95:591
  40. A Central Catecholaminergic Circuit Controls Blood Glucose Levels during Stress.
    Authors: Zhao Et al.
    Neuron  2017;95:138
  41. IGF1-Dependent Synaptic Plasticity of Mitral Cells in Olfactory Memory during Social Learning.
    Authors: Liu Et al.
    Neuron  2017;95:106
  42. CaMKII Autophosphorylation Is Necessary for Optimal Integration of Ca2+ Signals during LTP Induction, but Not Maintenance.
    Authors: Chang Et al.
    Neuron  2017;94:800
  43. The Retromer Supports AMPA Receptor Trafficking During LTP.
    Authors: Temkin Et al.
    Neuron  2017;94:74
  44. Formation and Maintenance of Functional Spines in the Absence of Presynaptic Glutamate Release.
    Authors: Sigler Et al.
    Neuron  2017;94:304
  45. An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes.
    Authors: McKeithan Et al.
    Front Physiol  2017;8:766
  46. Distal axotomy enhances retrograde presynaptic excitability onto injured pyramidal neurons via trans-synaptic signaling.
    Authors: Nagendran Et al.
    Nat Commun  2017;8:625
  47. 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
  48. On-demand optogenetic activation of human stem-cell-derived neurons.
    Authors: Klapper Et al.
    Sci Rep  2017;7:14450
  49. 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
  50. Molecular basis of ancestral vertebrate electroreception.
    Authors: Bellono
    Nature  2017;543:391
  51. 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
  52. 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
  53. Synaptic Activity Drives a Genomic Program That Promotes a Neuronal Warburg Effect.
    Authors: Bas-Orth Et al.
    J Biol Chem  2017;292:5183
  54. 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
  55. GLP-1 acts on habenular avoidance circuits to control nicotine intake.
    Authors: Tuesta
    Nat Neurosci  2017;20(5):708
  56. Posttranslational modification impact on the mechanism by which amyloid-β induces synaptic dysfunction.
    Authors: Grochowska Et al.
    EMBO Rep  2017;18:962
  57. Transcriptional Architecture of Synaptic Communication Delineates GABAergic Neuron Identity.
    Authors: Paul Et al.
    Cell  2017;171:522
  58. Ion channel expression patterns in glioblastoma stem cells with functional and therapeutic implications for malignancy.
    Authors: Pollak Et al.
    PLoS One  2017;12:e0172884
  59. Striatopallidal dysfunction underlies repetitive behavior in Shank3-deficient model of autism.
    Authors: Wang Et al.
    J Clin Invest  2017;127:1978
  60. Methylene blue inhibits GABAA receptors by interaction with GABA binding site.
    Authors: Chen
    Neuropharmacology  2017;119:100
  61. Targeted Intron Retention and Excision for Rapid Gene Regulation in Response to Neuronal Activity.
    Authors: Mauger Et al.
    Neuron  2016;92:1266
  62. Extra-coding RNAs regulate neuronal DNA methylation dynamics.
    Authors: Savell Et al.
    Nat Commun  2016;7:12091
  63. BK channel inactivation gates daytime excitability in the circadian clock.
    Authors: Whitt Et al.
    Nat Commun  2016;7:10837
  64. M1 ipRGCs Influence Visual Function through Retrograde Signaling in the Retina
    Authors: Prigge Et al.
    The Journal of Neuroscience  2016;6:7184
  65. High-throughput compound evaluation on 3D networks of neurons and glia in a microfluidic platform.
    Authors: Wevers Et al.
    Sci Rep  2016;6:38856
  66. The chemokine CXCL16 modulates neurotransmitter release in hippocampal CA1 area.
    Authors: Di Castro Et al.
    Scientific Reports  2016;6:34633
  67. Increased GABAB receptor signaling in a rat model for schizophrenia.
    Authors: Selten Et al.
    Scientific Reports  2016;6:34240
  68. DArgic neurons differentiating from LRRK2 G2019S induced pluripotent stem cells show early neuritic branching defects.
    Authors: Borgs Et al.
    Scientific Reports  2016;6:33377
  69. Dopaminergic neurons differentiating from LRRK2 G2019S induced pluripotent stem cells show early neuritic branching defects
    Authors: Borgs Et al.
    Scientific Reports  2016;6:33377
  70. Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.
    Authors: Colavita Et al.
    Sci Rep  2016;6:28454
  71. Effects of ε-viniferin, a dehydrodimer of resveratrol, on transepithelial active ion transport and ion permeability in the rat small and large intestinal mucosa.
    Authors: Karaki Et al.
    Physiol Rep  2016;4
  72. Compartmentalized PDE4A5 Signaling Impairs Hippocampal Synaptic Plasticity and Long-Term Memory.
    Authors: Havekes Et al.
    J Neurosci  2016;36:8936
  73. 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
  74. 17β-OE Acutely Potentiates Glutamatergic Synaptic Transmission in the Hippocampus through Distinct Mechanisms in Males and Females.
    Authors: Oberlander
    J Neurosci  2016;36:2677
  75. Tau-Driven Neuronal and Neurotrophic Dysfunction in a Mouse Model of Early Tauopathy.
    Authors: Mazzaro Et al.
    J Neurosci  2016;36:2086
  76. Cell-Autonomous Regulation of Dendritic Spine Density by PirB.
    Authors: Vidal Et al.
    Eneuro  2016;3
  77. Voltage Dependence of a Neuromodulator-Activated Ionic Current.
    Authors: Gray and Golowasch
    Eneuro  2016;3
  78. 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
  79. 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
  80. 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
  81. 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
  82. 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
  83. NE Modulates Pyramidal Cell Synaptic Properties in the Anterior Piriform Cortex of Mice: Age-Dependent Effects of β-adrenoceptors.
    Authors: Ghosh Et al.
    Cell Rep  2015;9:450
  84. 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
  85. 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
  86. An excitatory GABA loop operating in vivo.
    Authors: Astorga Et al.
    Front Cell Neurosci  2015;9:275
  87. 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
  88. Channel-mediated astrocytic glutamate modulates hippocampal synaptic plasticity by activating postsynaptic NMDA receptors.
    Authors: Park Et al.
    J Biomed Sci  2015;8:7
  89. Regulation of STEP61 and tyrosine-phosphorylation of NMDA and AMPA receptors during homeostatic synaptic plasticity.
    Authors: Jang Et al.
    Mol Brain  2015;8:55
  90. 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
  91. 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
  92. Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity.
    Authors: Pál Et al.
    Front Cell Neurosci  2015;8:35
  93. Genetic targeting of NRXN2 in mice unveils role in excitatory cortical synapse function and social behaviors.
    Authors: Born Et al.
    Mol Brain  2015;7:3
  94. 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
  95. Novel RNA- and FMRP-binding protein TRF2-S regulates axonal mRNA transport and presynaptic plasticity.
    Authors: Zhang Et al.
    J Neurosci  2015;6:8888
  96. Optical control of NMDA receptors with a diffusible photoswitch.
    Authors: Laprell Et al.
    Sci Rep  2015;6:8076
  97. Synaptic GABA release prevents GABA transporter type-1 reversal during excessive network activity.
    Authors: Savtchenko Et al.
    PLoS One  2015;6:6597
  98. Subventricular zone neural progenitors reverse TNF-α effects in cortical neurons.
    Authors: Morini Et al.
    Front Cell Neurosci  2015;6:166
  99. MicroRNA miR124 is required for the expression of homeostatic synaptic plasticity.
    Authors: Hou Et al.
    Nat Commun  2015;6:10045
  100. Synaptic structure and function are altered by the neddylation inhibitor MLN4924.
    Authors: Scudder and Patrick
    Mol Cell Neurosci  2015;65:52
  101. Optogenetic induction of contractile ability in immature C2C12 myotubes.
    Authors: Asano Et al.
    Curr Mol Med  2015;5:8317
  102. 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
  103. 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
  104. 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
  105. Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
    Authors: Saunders Et al.
    Sci Rep  2015;4
  106. 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
  107. Disruption of Fgf13 causes synaptic excitatory-inhibitory imbalance and genetic epilepsy and febrile seizures plus.
    Authors: Puranam Et al.
    Mol Brain  2015;35:8866
  108. 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
  109. 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.
    Authors: Ganley Et al.
    Front Synaptic Neurosci  2015;35:7626
  110. Cholinergic control of γ power in the midbrain spatial attention network.
    Authors: Bryant Et al.
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