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Submit ReviewTetrodotoxin citrate
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)
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 |
| 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 citrate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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:
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Reviews for Tetrodotoxin citrate
Average Rating: 4.3 (Based on 3 Reviews.)
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Filter by:
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
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
