IndraLab

Statements

Tetrodotoxin inhibits SCN5A. 8 / 9
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"This residue was also shown to dictate the intermediate TTX resistance of Nav1.5 [24,25], and Nav1.5 is the only subunit with a cysteine at this position [1]."
38928302
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"C, TTX 1 muM alone had only an insignificant effect on bradykinin-inducedAP discharge in jugular C-fibres (n = 9); however, the response to bradykinin was by 50% inhibited by NaV1.8 blocker PF-01247324 10 muM (n = 11) (* P < 0.05, paired t test) and> 80% inhibited by combination of PF-01247324 10 muM and TTX 1 muM (n = 7) (* P < 0.05, paired t test)."
29435993
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"Inhibition of NaV1.5 by TTX prevented phagocytosis, sodium efflux and endosomal acidification [28] ."
25922224
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"TTX shows little selectivity for TTX-S channels in the nM range but have up to100-fold reduced affinity to cardiac Nav1.5 channels.58 Despite lack of selectivity, a phase III trial although underpowered, indicates that subcutaneous TTX (TEC-006) may provide clinically meaningful analgesia for persistent refractory cancer pain.130 Although selectivity and systemic toxicity of toxins constrains clinical use, they are promising scaffolds for more specific inhibitors.Peptide -conotoxins of marine cone snails, GIIIA and GIIB, block the rat skeletal muscle Nav1.4 by binding neurotoxin site 1."
31564962
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"Moreover, ropivacaine, lidocaine, TTX, and a siRNA specifically targeting Nav1.5 could inhibit Nav1.5 channel function and invasion of metastatic colon cancer SW620 cells, and the Nav1.5 channel activator veratridine promoted SW620 cell invasion (9,18)."
35116732
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"The voltage gated sodium channel family is comprised of ten members : SCN1A (Nav1.1), SCN2A (Nav1.2; SCN2A1 in mouse), SCN3A (Nav1.3), SCN4A (Nav1.4), SCN8A (Nav1.6), and SCN9A (Nav1.7) are blocked by tetrodotoxin, whereas SCN5A (Nav1.5), SCN7A (Nax), SCN10A (Nav1.8), and SCN11A (Nav1.9) are not blocked by tetrodotoxin [XREF_BIBR, XREF_BIBR, XREF_BIBR]."
19284629
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"Further, we note the difference between sodium currents in hCICs and cardiomyocytes—I in hCIC is mainly encoded by Nav1.3 and Nav1.6, and is very sensitive to inhibition by TTX in the nanomolar range, whereas human cardiac myocyte I (Nav1.5) is usually blocked by TTX in the micromolar range (Zhang et al., 2014)."
35046835
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"The characteristic low affinity for block of NaV1.5 by TTX is a hallmark of sodium channel pharmacology ."
31866066