Tetrodotoxin citrate

Product Description

Tetrodotoxin citrate, the water-soluble citrate salt of tetrodotoxin, is a reversible, potent, selective and high affinity inhibitor of voltage gated sodium channels Na_v 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 (K_d = 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⁺ (Ca_v1.x) channels, blocks primary reward in an animal study of drug-seeking lever pressing.

Tetrodotoxin (Cat. No. 1078) also available.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	31.32 mL	156.61 mL	313.21 mL
0.5 mM	6.26 mL	31.32 mL	62.64 mL
1 mM	3.13 mL	15.66 mL	31.32 mL
5 mM	0.63 mL	3.13 mL	6.26 mL

Calculators

Background References

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

• Shoromony Prolonged duration local anesthesia by combined delivery of capsaicin- and tetrodotoxin-loaded liposomes. Anesth.Analg. 2019 PMID: 31425210
• Ono Antagonistic effects of tetrodotoxin on aconitine-induced cardiac toxicity. J.Nippon Med.Sch. 2013 PMID: 24189353
• Tsukamoto Differential binding of tetrodotoxin and its derivatives to voltage-sensitive sodium channel subtypes (Nav1.1 to Nav1.7). Br.J.Pharmacol. 2017 PMID: 28832970
• Hegyi Tetrodotoxin blockade on canine cardiac L-type Ca²⁺ channels depends on pH and redox potential. Mar.Drugs 2013 PMID: 23771047
• Grimm and See Dissociation of primary and secondary reward-relevant limbic nuclei in an animal model of relapse. Neuropsychopharmacology 2000 PMID: 10731622
• Kao Structure-activity relations of tetrodotoxin, saxitoxin, and analogues. Ann.N.Y.Acad.Sci. 1986 PMID: 2434008
• Kao Pharmacology of tetrodotoxin and saxitoxin. Fed.Proc. 1972 PMID: 5032475
• Gleitz The protective action of tetrodotoxin and (±)-kavain on anaerobic glycolysis, ATP content and intracellular Na⁺ and Ca²⁺ of anoxic brain vesicles. Neuropharmacology 1996 PMID: 9076753