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Submit ReviewTetrodotoxin
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% (HPLC)
Biological Activity for Tetrodotoxin
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 for Tetrodotoxin
| M. Wt | 319.27 |
| Formula | C11H17N3O8 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 4368-28-9 |
| PubChem ID | 16759596 |
| InChI Key | CFMYXEVWODSLAX-CKYAAQHSSA-N |
| 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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| acidic buffer (pH 4.8) | 0.96 | 3 |
Preparing Stock Solutions for Tetrodotoxin
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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.03 mM | 104.4 mL | 522.02 mL | 1044.05 mL |
| 0.15 mM | 20.88 mL | 104.4 mL | 208.81 mL |
| 0.3 mM | 10.44 mL | 52.2 mL | 104.4 mL |
| 1.5 mM | 2.09 mL | 10.44 mL | 20.88 mL |
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Product Datasheets for Tetrodotoxin
References for Tetrodotoxin
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
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
Ono et al (2013) Antagonistic effects of tetrodotoxin on aconitine-induced cardiac toxicity. J.Nippon Med.Sch. 80 350 PMID: 24189353
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
Grimm and See (2000) Dissociation of primary and secondary reward-relevant limbic nuclei in an animal model of relapse. Neuropsychopharmacology 22 473 PMID: 10731622
Shomorony 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, please let us know.
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Keywords: Tetrodotoxin, Tetrodotoxin supplier, Na+, channel, blockers, Sodium, NaV, Channels, voltage-gated, voltage-dependent, TTx, Voltage-gated, 1078, Tocris Bioscience
337 Citations for Tetrodotoxin
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Volgin and Kubin (2007) Regionally selective effects of GABA on hypothalamic GABAA receptor mRNA in vitro. Proc Natl Acad Sci U S A 353 726 PMID: 17188647
Milenković et al (2007) Development of chloride-mediated inhibition in neurons of the anteroventral cochlear nucleus of gerbil (Meriones unguiculatus). J Neurophysiol 98 1634 PMID: 17596413
Woo et al (2007) Neuregulin-1 enhances depolarization-induced GABA release. Neuron 54 599 PMID: 17521572
Nakamoto et al (2007) Fragile X mental retardation protein deficiency leads to excessive mGluR5-dependent internalization of AMPA receptors. Proc Natl Acad Sci U S A 104 15537 PMID: 17881561
Baldelli et al (2007) Lack of synapsin I reduces the readily releasable pool of synaptic vesicles at central inhibitory synapses. J Neurosci 27 13520 PMID: 18057210
Do you know of a great paper that uses Tetrodotoxin from Tocris? Please let us know.
Reviews for Tetrodotoxin
Average Rating: 4.8 (Based on 5 Reviews.)
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Totally blocked action potential.
By
Yuyang Sun on 05/30/2022
Assay Type: In Vitro
Species: Mouse
Works great. Totally blocked the action potential in mouse brain slice.
Validation.
By
Anonymous on 04/04/2020
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Sprague-Dawley rats primary neuronal
10 μM for 30min
The pharmacological inhibitors for electrophysiology assay.
By
Anonymous on 02/28/2020
Assay Type: In Vitro
Species: Other
The following concentrations we were used:1 μM Bay K, 10 μM nifedipine, 10 μM nimodipine, 300 nM omega -agatoxin, 1 μM omega -conotoxin, 5 μM mibefradil, 1 μM tetrodotoxin, 1 μM charybdotoxin, 100 nM iberiotoxin, 10 μM NS11021.
TTX blocks action potential propagation.
By
Anonymous on 08/31/2019
Assay Type: Ex Vivo
Species: Rat
Cell Line/Tissue: Hippocampus
Tetrodotoxin (TTX) was used to block action potential propagation in response to lasting current injection into living neuron. This illustrated a critical role of voltage-gated sodium channels in inter-neuronal crosstalk. 1 microM of TTX developed 100% effect (see Figure). Figure: action potential generation by isolated neuron under control and after TTX was added to perfusion solution.
Compound should be sonicated when dissolved.
good drug for neuronal activity inhibition.
By
Lihua Wang on 01/24/2018
Assay Type: In Vitro
Species: Mouse
We use this to block cell activity of the brain slices, in order to keep the cells more healthy after they are dissociated. It works great and helps a lot for our purpose; but the only little problem is that it's very hard to dissolve in the water.