Tetrodotoxin citrate

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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% (HPLC)
Citations (74)
Reviews (3)

Biological Activity for Tetrodotoxin citrate

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 for Tetrodotoxin citrate

M. Wt 319.27
Formula C11H17N3O8
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 18660-81-6
PubChem ID 16759596
Smiles OC1(CO)[C@H](O4)C(O)[C@@]2([C@@H]([C@@H](O)N3)C1O[C@](O)4[C@H]2O)NC3=N

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.

Solubility Data for Tetrodotoxin citrate

Solvent Max Conc. mg/mL Max Conc. mM
water 31.93 100

Preparing Stock Solutions for Tetrodotoxin citrate

The following data is based on the product molecular weight 319.27. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.13 mL 15.66 mL 31.32 mL
5 mM 0.63 mL 3.13 mL 6.26 mL
10 mM 0.31 mL 1.57 mL 3.13 mL
50 mM 0.06 mL 0.31 mL 0.63 mL

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Product Datasheets for Tetrodotoxin citrate

Certificate of Analysis / Product Datasheet
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References for Tetrodotoxin citrate

References are publications that support the biological activity of the product.

Gleitz et al (1996) The protective action of tetrodotoxin and (±)-kavain on anaerobic glycolysis, ATP content and intracellular Na+ and Ca2+ of anoxic brain vesicles. Neuropharmacology 35 1743 PMID: 9076753

Kao (1972) Pharmacology of tetrodotoxin and saxitoxin. Fed.Proc. 31 1117 PMID: 5032475

Kao (1986) Structure-activity relations of tetrodotoxin, saxitoxin, and analogues. Ann.N.Y.Acad.Sci. 479 52 PMID: 2434008

Merck Index 12 9382

Grimm and See (2000) Dissociation of primary and secondary reward-relevant limbic nuclei in an animal model of relapse. Neuropsychopharmacology 22 473 PMID: 10731622

Hegyi et al (2013) Tetrodotoxin blockade on canine cardiac L-type Ca2+ channels depends on pH and redox potential. Mar.Drugs 11 2140 PMID: 23771047

Ono et al (2013) Antagonistic effects of tetrodotoxin on aconitine-induced cardiac toxicity. J.Nippon Med.Sch. 80 350 PMID: 24189353

Tsukamoto et al (2017) Differential binding of tetrodotoxin and its derivatives to voltage-sensitive sodium channel subtypes (Nav1.1 to Nav1.7). Br.J.Pharmacol. 174 3881 PMID: 28832970

Shoromony et al (2019) Prolonged duration local anesthesia by combined delivery of capsaicin- and tetrodotoxin-loaded liposomes. Anesth.Analg. 129 709 PMID: 31425210

If you know of a relevant reference for Tetrodotoxin citrate, please let us know.

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Keywords: Tetrodotoxin citrate, Tetrodotoxin citrate supplier, Citrate, salt, Sodium, NaV, Channels, voltage-gated, voltage-dependent, Na+, TTx, citrate, Voltage-gated, 1069, Tocris Bioscience

74 Citations for Tetrodotoxin citrate

Citations are publications that use Tocris products. Selected citations for Tetrodotoxin citrate include:

Kiritoshi and Neugebauer (2018) Pathway-specific alterations of cortico-amygdala transmission in an arthritis pain model. ACS Chem Neurosci 9 2252 PMID: 29630339

Chou et al (2018) (2R,6R)-hydroxynorKA rescues chronic stress-induced depression-like behavior through its actions in the midbrain periaqueductal gray. Neuropharmacology 139 1 PMID: 29953886

Dover et al (2016) FHF-independent conduction of action potentials along the leak-resistant cerebellar granule cell axon. Nat Commun 7 12895 PMID: 27666389

Liu et al (2016) Cortico-fugal output from visual cortex promotes plasticity of innate motor behaviour. Nature 538 383 PMID: 27732573

Riquelme et al (2018) Subcellular Localization and Activity of TRPM4 in Medial Prefrontal Cortex Layer 2/3. Front Cell Neurosci 12 12 PMID: 29440991

Donlea et al (2018) Recurrent Circuitry for Balancing Sleep Need and Sleep. Neuron 97 378 PMID: 29307711

Whitt et al (2018) Differential contribution of Ca2+ sources to day and night BK current activation in the circadian clock. J Gen Physiol 150 259 PMID: 29237755

Wall et al (2018) The Temporal Dynamics of Arc Expression Regulate Cognitive Flexibility. Neuron 98 1124 PMID: 29861284

Groschner et al (2018) Dendritic Integration of Sensory Evidence in Perceptual Decision-Making. Cell 173 894 PMID: 29706545

Zhang et al (2018) Heparan Sulfate Organizes Neuronal Synapses through Neurexin Partnerships. Cell 174 1450 PMID: 30100184

Khodai et al (2018) PACAP Neurons in the Ventromedial Hypothalamic Nucleus Are Glucose Inhibited and Their Selective Activation Induces Hyperglycaemia. Front Endocrinol (Lausanne) 9 632 PMID: 30425681

McKay et al (2018) The Developmental Shift of NMDA Receptor Composition Proceeds Independently of GluN2 Subunit-Specific GluN2 C-Terminal Sequences. Cell Rep 25 841 PMID: 30355491

Thomsen et al (2016) Fixed single-cell transcriptomic characterization of human radial glial diversity. Proc Natl Acad Sci U S A 13 87 PMID: 26524239

Cichon and Gan (2015) Branch-specific dendritic Ca(2+) spikes cause persistent synaptic plasticity. Nature 520 180 PMID: 25822789

Dieck et al (2015) Direct visualization of newly synthesized target proteins in situ. Nat Methods 12 411 PMID: 25775042

Ouwenga and Dougherty (2015) Fmrp targets or not: long, highly brain-expressed genes tend to be implicated in autism and brain disorders. Mol Autism 6 16 PMID: 25789151

Bijland et al (2019) An in vitro model for studying CNS white matter: functional properties and experimental approaches. F1000Res 8 117 PMID: 31069065

Pagani et al (2019) How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch. Neuron PMID: 31103358

Ackman et al (2012) Retinal waves coordinate patterned activity throughout the developing visual system. Nature 490 219 PMID: 23060192

Lee et al (2013) 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. J Neurosci 33 1157 PMID: 23325252

Battefeld et al (2019) High-Frequency Microdomain Ca2+ Transients and Waves during Early Myelin Internode Remodeling. Cell Rep 26 182 PMID: 30605675

Spoljaric et al (2019) KCC2-Mediated Cl- Extrusion Modulates Spontaneous Hippocampal Network Events in Perinatal Rats and Mice. Cell Rep 26 1073 PMID: 30699338

Chen et al (2019) Enhancer Histone Acetylation Modulates Transcriptional Bursting Dynamics of Neuronal Activity-Inducible Genes. Cell Rep 26 1174 PMID: 30699347

Zhong et al (2019) Soluble TREM2 ameliorates pathological phenotypes by modulating microglial functions in an Alzheimer's disease model. Nat Commun 10 1365 PMID: 30911003

Woo et al (2019) Pharmacological Dissection of Intrinsic Optical Signal Reveals a Functional Coupling between Synaptic Activity and Astrocytic Volume Transient. Exp Neurobiol 28 30 PMID: 30853822

Ouwenga et al (2017) Transcriptomic Analysis of Ribosome-Bound mRNA in Cortical Neurites In Vivo. J Neurosci 37 8688 PMID: 28821669

Cichon et al (2017) Activation of cortical somatostatin interneurons prevents the development of neuropathic pain. Nat Neurosci 20 1122 PMID: 28671692

Fontenot et al (2017) A Model-Based Approach for Separating the Cochlear Microphonic from the Auditory Nerve Neurophonic in the Ongoing Response Using Electrocochleography. Front Neurosci 11 592 PMID: 29123468

Sigler et al (2017) Formation and Maintenance of Functional Spines in the Absence of Presynaptic Glutamate Release. Neuron 94 304 PMID: 28426965

Ferrai et al (2017) RNA polymerase II primes Polycomb-repressed developmental genes throughout terminal neuronal differentiation. Mol Syst Biol 13 946 PMID: 29038337

Fox and Hentges (2017) Differential Desensitization Observed at Multiple Effectors of Somatic μ-Opioid Receptors Underlies Sustained Agonist-Mediated Inhibition of Proopiomelanocortin Neuron Activity. J Neurosci 37 8667 PMID: 28821664

Yusta et al (2017) GLP-2 promotes gallbladder refilling via a TGR5-independent, GLP-2R-dependent pathway. Mol Metab 6 503 PMID: 28580281

Williams et al (2014) Excitatory drive onto DArgic neurons in the rostral linear nucleus is enhanced by NE in an α1 adrenergic receptor-dependent manner. Neuropharmacology 86 116 PMID: 25018040

Carneiro et al (2014) Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium. Br J Pharmacol 171 3404 PMID: 24697602

Tozzi et al (2012) A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation. PLoS One 7 e38312 PMID: 22715379

Jurgens et al (2012) Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus. PLoS One 7 e45717 PMID: 23029198

Janssen et al (2012) Neuregulin directly decreases voltage-gated sodium current in hippocampal ErbB4-expressing interneurons. J Neurosci 32 13889 PMID: 23035098

Weiner et al (2019) Cholinergic neural activity directs retinal layer-specific angiogenesis and blood retinal barrier formation. Nat Commun 10 2477 PMID: 31171770

Li et al (2015) The Cancer Chemotherapeutic PacT. Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4. J Neurosci 35 13487 PMID: 26424893

Brown and Wonnacott (2015) Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors. Gastroenterology 40 2047 PMID: 24728867

Slowik and Henderson (2015) Benchmarking the stability of human detergent-solubilised voltage-gated sodium channels for structural studies using eel as a reference. J Neurosci 1848 1545 PMID: 25838126

Dagostin et al (2012) Increased bursting glutamatergic neurotransmission in an auditory forebrain area of the zebra finch (Taenopygia guttata) induced by auditory stimulation. J Biol Chem 198 705 PMID: 22752655

Austgen et al (2012) 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii. PLoS One 108 2292 PMID: 22855775

Watmuff et al (2012) In vitro maturation of DArgic neurons derived from mouse embryonic stem cells: implications for transplantation. J Neurosci 7 e31999 PMID: 22384125

Austgen et al (2011) Hydrogen sulfide augments synaptic neurotransmission in the nucleus of the solitary tract. Mol Brain 106 1822 PMID: 21734104

Park et al (2017) Optogenetic Modulation of Urinary Bladder Contraction for Lower Urinary Tract Dysfunction. Sci Rep 7 40872 PMID: 28098199

Reutsky-Gefen et al (2013) Holographic optogenetic stimulation of patterned neuronal activity for vision restoration. Nat Methods 4 1509 PMID: 23443537

Mameza et al (2013) SHANK3 gene mutations associated with autism facilitate ligand binding to the Shank3 ankyrin repeat region. Biochim Biophys Acta 288 26697 PMID: 23897824

Specht et al (2011) Regulation of glycine receptor diffusion properties and gephyrin interactions by protein kinase C. EMBO J 30 3842 PMID: 21829170

Stacpoole et al (2011) Efficient derivation of NPCs, spinal motor neurons and midbrain DArgic neurons from hESCs at 3% oxygen. Nat Protoc 6 1229 PMID: 21799491

Zemkova et al (2011) NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+. Endocrinology 152 3842 PMID: 21828176

Calloe et al (2011) Multiple arrhythmic syndromes in a newborn, owing to a novel mutation in SCN5A. Can J Physiol Pharmacol 89 723 PMID: 21895525

Vornanen et al (2011) Tetrodotoxin sensitivity of the vertebrate cardiac Na+ current. Mar Drugs 9 2409 PMID: 22163193

Yang et al (2016) Transcriptomes of lineage-specific Drosophila neuroblasts profiled by genetic targeting and robotic sorting. Development 143 411 PMID: 26700685

Liu et al (2015) Muscarinic receptors modulate dendrodendritic inhibitory synapses to sculpt glomerular output. J Neurophysiol 35 5680 PMID: 25855181

Tseng et al (2015) Giant ankyrin-G stabilizes somatodendritic GABAergic synapses through opposing endocytosis of GABAA receptors. Front Cell Neurosci 112 1214 PMID: 25552561

Angelantonio et al (2015) Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R. PLoS One 9 409 PMID: 26528137

Jonas et al (2015) Assessment of TTX-s and TTX-r Action Potential Conduction along Neurites of NGF and GDNF Cultured Porcine DRG Somata. Neurochem Res 10 e0139107 PMID: 26407014

Halff et al (2014) A novel mechanism for nicotinic potentiation of glutamatergic synapses. J Neurosci 34 2051 PMID: 24501347

Yuan et al (2018) A role for proteolytic regulation of δ-catenin in remodeling a subpopulation of dendritic spines in the rodent brain. J Biol Chem 293 11625 PMID: 29875160

Collins et al (2018) Reciprocal Circuits Linking the Prefrontal Cortex with Dorsal and Ventral Thalamic Nuclei. Neuron 98 366 PMID: 29628187

Song et al (2018) Selective Role of RGS9-2 in Regulating Retrograde Synaptic Signaling of Indirect Pathway Medium Spiny Neurons in Dorsal Striatum. J Neurosci 38 7120 PMID: 30006367

Di Castro et al (2016) The chemokine CXCL16 modulates neurotransmitter release in hippocampal CA1 area Scientific Reports 6 34633 PMID: 27721466

Evans et al (2013) Dynamic interactions mediated by nonredundant signaling mechanisms couple circadian clock neurons. Neuron 80 973 PMID: 24267653

Montgomery et al (2013) Mis-expression of the BK K(+) channel disrupts suprachiasmatic nucleus circuit rhythmicity and alters clock-controlled behavior. Am J Physiol Cell Physiol 304 C299 PMID: 23174562

Ren et al (2013) Direct retino-raphe projection alters serotonergic tone and affective behavior. Neuropsychopharmacology 38 1163 PMID: 23370156

Bloodgood et al (2013) The activity-dependent transcription factor NPAS4 regulates domain-specific inhibition. Nature 503 121 PMID: 24201284

Wang et al (2011) Characteristics of 5-hydroxytryptamine receptors involved in contraction of feline ileal longitudinal smooth muscle. Korean J Physiol Pharmacol 15 267 PMID: 22128258

Han et al (2007) DArgic modulation of spinal neuronal excitability. J Neurophysiol 27 13192 PMID: 18045913

Kato et al (2007) New transmembrane AMPA receptor regulatory protein isoform, γ-7, differentially regulates AMPA receptors. J Comp Physiol A Neuroethol Sens Neural Behav Phys 27 4969 PMID: 17475805

Schicho et al (2006) Hydrogen sulfide is a novel prosecretory neuromodulator in the Guinea-pig and human colon. J Neurosci 131 1542 PMID: 17101327

Khan et al (2006) Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br J Pharmacol 147 607 PMID: 16432510

Lee and Tepper (2007) A calcium-activated nonselective cation conductance underlies the plateau potential in rat substantia nigra GABAergic neurons. J Neurosci 27 6531 PMID: 17567814

Pinaud et al (2008) Inhibitory network interactions shape the auditory processing of natural communication signals in the songbird auditory forebrain. J Neurophysiol 100 441 PMID: 18480371

Do you know of a great paper that uses Tetrodotoxin citrate from Tocris? Please let us know.

Reviews for Tetrodotoxin citrate

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homeostatic plasticity.
By Vineet Arora on 11/19/2020
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: Organotypic cultures

For studying homeostatic plasticity

Antidepressantsby Cholecystokinin Neurons of the Dentate Gyrus.
By Anonymous on 02/03/2020
Assay Type: In Vivo
Species: Mouse

10uM TTX

PMID: 28735749
review image

blocks calcium oscillations well.
By Karthik krishnamurthy on 11/08/2018
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: hippocampal neurons

used to block calcium oscillations in neurons

20 nM was used

review image