Tetrodotoxin citrate

Catalog # Availability Size / Price Qty
Tetrodotoxin citrate | CAS No. 18660-81-6 | Voltage-gated Sodium Channel Blockers
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Description: Na+ channel blocker; citrate salt of tetrodotoxin (Cat. No. 1078)
Alternative Names: TTx 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%

Product Details
Citations (74)
Supplemental Products

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

Soluble to 100 mM in water
Store at -20°C

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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Additional Information

Other Product-Specific Information:
Each vial contains 1mg of tetrodotoxin and 5mg of lyophilized citrate buffer, pH 4.8.

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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

  1. An in vitro model for studying CNS white matter: functional properties and experimental approaches.
    Authors: Bijland Et al.
    F1000Res  2019;8:117
  2. Pharmacological Dissection of Intrinsic Optical Signal Reveals a Functional Coupling between Synaptic Activity and Astrocytic Volume Transient.
    Authors: Woo Et al.
    Exp Neurobiol  2019;28:30
  3. High-Frequency Microdomain Ca2+ Transients and Waves during Early Myelin Internode Remodeling.
    Authors: Battefeld Et al.
    Cell Rep  2019;26:182
  4. Enhancer Histone Acetylation Modulates Transcriptional Bursting Dynamics of Neuronal Activity-Inducible Genes.
    Authors: Chen Et al.
    Cell Rep  2019;26:1174
  5. KCC2-Mediated Cl- Extrusion Modulates Spontaneous Hippocampal Network Events in Perinatal Rats and Mice.
    Authors: Spoljaric Et al.
    Cell Rep  2019;26:1073
  6. Cholinergic neural activity directs retinal layer-specific angiogenesis and blood retinal barrier formation.
    Authors: Weiner Et al.
    Nat Commun  2019;10:2477
  7. Soluble TREM2 ameliorates pathological phenotypes by modulating microglial functions in an Alzheimer's disease model.
    Authors: Zhong Et al.
    Nat Commun  2019;10:1365
  8. How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch.
    Authors: Pagani Et al.
    Neuron  2019;
  9. PACAP Neurons in the Ventromedial Hypothalamic Nucleus Are Glucose Inhibited and Their Selective Activation Induces Hyperglycaemia.
    Authors: Khodai Et al.
    Front Endocrinol (Lausanne)  2018;9:632
  10. Pathway-specific alterations of cortico-amygdala transmission in an arthritis pain model.
    Authors: Kiritoshi and Neugebauer
    ACS Chem Neurosci  2018;9:2252
  11. Reciprocal Circuits Linking the Prefrontal Cortex with Dorsal and Ventral Thalamic Nuclei.
    Authors: Collins Et al.
    Neuron  2018;98:366
  12. The Temporal Dynamics of Arc Expression Regulate Cognitive Flexibility.
    Authors: Wall Et al.
    Neuron  2018;98:1124
  13. Recurrent Circuitry for Balancing Sleep Need and Sleep.
    Authors: Donlea Et al.
    Neuron  2018;97:378
  14. Selective Role of RGS9-2 in Regulating Retrograde Synaptic Signaling of Indirect Pathway Medium Spiny Neurons in Dorsal Striatum.
    Authors: Song Et al.
    J Neurosci  2018;38:7120
  15. 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
  16. The Developmental Shift of NMDA Receptor Composition Proceeds Independently of GluN2 Subunit-Specific GluN2 C-Terminal Sequences.
    Authors: McKay Et al.
    Cell Rep  2018;25:841
  17. Heparan Sulfate Organizes Neuronal Synapses through Neurexin Partnerships.
    Authors: Zhang Et al.
    Cell  2018;174:1450
  18. Dendritic Integration of Sensory Evidence in Perceptual Decision-Making.
    Authors: Groschner Et al.
    Cell  2018;173:894
  19. Differential contribution of Ca2+ sources to day and night BK current activation in the circadian clock.
    Authors: Whitt Et al.
    J Gen Physiol  2018;150:259
  20. (2R,6R)-hydroxynorKA rescues chronic stress-induced depression-like behavior through its actions in the midbrain periaqueductal gray.
    Authors: Chou Et al.
    Neuropharmacology  2018;139:1
  21. Subcellular Localization and Activity of TRPM4 in Medial Prefrontal Cortex Layer 2/3.
    Authors: Riquelme Et al.
    Front Cell Neurosci  2018;12:12
  22. Formation and Maintenance of Functional Spines in the Absence of Presynaptic Glutamate Release.
    Authors: Sigler Et al.
    Neuron  2017;94:304
  23. Optogenetic Modulation of Urinary Bladder Contraction for Lower Urinary Tract Dysfunction.
    Authors: Park Et al.
    Sci Rep  2017;7:40872
  24. GLP-2 promotes gallbladder refilling via a TGR5-independent, GLP-2R-dependent pathway.
    Authors: Yusta Et al.
    Mol Metab  2017;6:503
  25. Transcriptomic Analysis of Ribosome-Bound mRNA in Cortical Neurites In Vivo.
    Authors: Ouwenga Et al.
    J Neurosci  2017;37:8688
  26. 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
  27. Activation of cortical somatostatin interneurons prevents the development of neuropathic pain.
    Authors: Cichon Et al.
    Nat Neurosci  2017;20:1122
  28. RNA polymerase II primes Polycomb-repressed developmental genes throughout terminal neuronal differentiation.
    Authors: Ferrai Et al.
    Mol Syst Biol  2017;13:946
  29. A Model-Based Approach for Separating the Cochlear Microphonic from the Auditory Nerve Neurophonic in the Ongoing Response Using Electrocochleography.
    Authors: Fontenot Et al.
    Front Neurosci  2017;11:592
  30. FHF-independent conduction of action potentials along the leak-resistant cerebellar granule cell axon.
    Authors: Dover Et al.
    Nat Commun  2016;7:12895
  31. The chemokine CXCL16 modulates neurotransmitter release in hippocampal CA1 area
    Authors: Di Castro Et al.
    Scientific Reports  2016;6:34633
  32. Cortico-fugal output from visual cortex promotes plasticity of innate motor behaviour.
    Authors: Liu Et al.
    Nature  2016;538:383
  33. Transcriptomes of lineage-specific Drosophila neuroblasts profiled by genetic targeting and robotic sorting.
    Authors: Yang Et al.
    Development  2016;143:411
  34. Fixed single-cell transcriptomic characterization of human radial glial diversity.
    Authors: Thomsen Et al.
    Proc Natl Acad Sci U S A  2016;13:87
  35. Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R.
    Authors: Angelantonio Et al.
    PLoS One  2015;9:409
  36. Fmrp targets or not: long, highly brain-expressed genes tend to be implicated in autism and brain disorders.
    Authors: Ouwenga and Dougherty
    Mol Autism  2015;6:16
  37. Branch-specific dendritic Ca(2+) spikes cause persistent synaptic plasticity.
    Authors: Cichon and Gan
    Nature  2015;520:180
  38. Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
    Authors: Brown and Wonnacott
    Gastroenterology  2015;40:2047
  39. Muscarinic receptors modulate dendrodendritic inhibitory synapses to sculpt glomerular output.
    Authors: Liu Et al.
    J Neurophysiol  2015;35:5680
  40. The Cancer Chemotherapeutic PacT. Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4.
    Authors: Li Et al.
    J Neurosci  2015;35:13487
  41. Benchmarking the stability of human detergent-solubilised voltage-gated sodium channels for structural studies using eel as a reference.
    Authors: Slowik and Henderson
    J Neurosci  2015;1848:1545
  42. Direct visualization of newly synthesized target proteins in situ.
    Authors: Dieck Et al.
    Nat Methods  2015;12:411
  43. Giant ankyrin-G stabilizes somatodendritic GABAergic synapses through opposing endocytosis of GABAA receptors.
    Authors: Tseng Et al.
    Front Cell Neurosci  2015;112:1214
  44. Assessment of TTX-s and TTX-r Action Potential Conduction along Neurites of NGF and GDNF Cultured Porcine DRG Somata.
    Authors: Jonas Et al.
    Neurochem Res  2015;10:e0139107
  45. Excitatory drive onto DArgic neurons in the rostral linear nucleus is enhanced by NE in an α1 adrenergic receptor-dependent manner.
    Authors: Williams Et al.
    Neuropharmacology  2014;86:116
  46. A novel mechanism for nicotinic potentiation of glutamatergic synapses.
    Authors: Halff Et al.
    J Neurosci  2014;34:2051
  47. Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium.
    Authors: Carneiro Et al.
    Br J Pharmacol  2014;171:3404
  48. Dynamic interactions mediated by nonredundant signaling mechanisms couple circadian clock neurons.
    Authors: Evans Et al.
    Neuron  2013;80:973
  49. The activity-dependent transcription factor NPAS4 regulates domain-specific inhibition.
    Authors: Bloodgood Et al.
    Nature  2013;503:121
  50. Holographic optogenetic stimulation of patterned neuronal activity for vision restoration.
    Authors: Reutsky-Gefen Et al.
    Nat Methods  2013;4:1509
  51. Direct retino-raphe projection alters serotonergic tone and affective behavior.
    Authors: Ren Et al.
    Neuropsychopharmacology  2013;38:1163
  52. 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
  53. 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
  54. SHANK3 gene mutations associated with autism facilitate ligand binding to the Shank3 ankyrin repeat region.
    Authors: Mameza Et al.
    Biochim Biophys Acta  2013;288:26697
  55. Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus.
    Authors: Jurgens Et al.
    PLoS One  2012;7:e45717
  56. A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation.
    Authors: Tozzi Et al.
    PLoS One  2012;7:e38312
  57. In vitro maturation of DArgic neurons derived from mouse embryonic stem cells: implications for transplantation.
    Authors: Watmuff Et al.
    J Neurosci  2012;7:e31999
  58. Retinal waves coordinate patterned activity throughout the developing visual system.
    Authors: Ackman Et al.
    Nature  2012;490:219
  59. Neuregulin directly decreases voltage-gated sodium current in hippocampal ErbB4-expressing interneurons.
    Authors: Janssen Et al.
    J Neurosci  2012;32:13889
  60. 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
  61. 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii.
    Authors: Austgen Et al.
    PLoS One  2012;108:2292
  62. Tetrodotoxin sensitivity of the vertebrate cardiac Na+ current.
    Authors: Vornanen Et al.
    Mar Drugs  2011;9:2409
  63. Multiple arrhythmic syndromes in a newborn, owing to a novel mutation in SCN5A.
    Authors: Calloe Et al.
    Can J Physiol Pharmacol  2011;89:723
  64. 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
  65. Regulation of glycine receptor diffusion properties and gephyrin interactions by protein kinase C.
    Authors: Specht Et al.
    EMBO J  2011;30:3842
  66. 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
  67. 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
  68. Hydrogen sulfide augments synaptic neurotransmission in the nucleus of the solitary tract.
    Authors: Austgen Et al.
    Mol Brain  2011;106:1822
  69. 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
  70. 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
  71. 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
  72. DArgic modulation of spinal neuronal excitability.
    Authors: Han Et al.
    J Neurophysiol  2007;27:13192
  73. 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
  74. 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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