Tetrodotoxin Citrate Liquid

Biological Activity for Tetrodotoxin citrate

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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.