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September 5, 2026EP EuropaceOpen Access

AaH-II activates tetrodotoxin-sensitive sodium channels to drive arrhythmogenesis and QT prolongation independently of Nav1.5.

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Why the study?

Whether tetrodotoxin-sensitive sodium channel isoforms directly contribute to pathological late sodium current and arrhythmogenesis was unresolved due to a lack of isoform-selective pharmacological tools.

Does selective activation of TTX-S sodium channels by AaH-II drive arrhythmogenic late Na+ current in the heart?

Population

Human iPS-derived cardiomyocytes, adult ventricular cardiomyocytes, isolated hearts, and in vivo models

Comparison

AaH-II vs reference inducer ATX-II or nanomolar tetrodotoxin

Design

Preclinical experimental study

Key result

AaH-II selectively activates tetrodotoxin-sensitive sodium channels to generate arrhythmogenic late Na+ current, causing conduction abnormalities and QT prolongation independently of Nav1.5.

Authors

HMHugo MilletMCMaureen Choteau‐BodorTSThomas Stervinou

Discussion

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Member takes

Overview

Challenges Nav1.5-centric arrhythmia models; hypothesis-generating for TTX-S targeting but requires human validation before any therapeutic consideration.

Key Points

  • To determine whether tetrodotoxin-sensitive (TTX-S) sodium channels contribute directly to pathological cardiac late sodium current and arrhythmogenesis using selective pharmacological tools.
  • Characterized the isoform selectivity of reference inducer ATX-II and scorpion toxin AaH-II using automated patch-clamp and human Nav isoform profiling.
  • Assessed electrophysiological and arrhythmogenic effects in human induced pluripotent stem cell-derived cardiomyocytes, adult ventricular cardiomyocytes, isolated hearts, and in vivo models.
  • AaH-II selectively and potently enhanced late sodium current through TTX-S Nav isoforms, whereas ATX-II predominantly targeted Nav1.5 and lacked isoform selectivity at high concentrations.
  • Selective TTX-S activation triggered action potential prolongation, abnormal calcium handling, QT interval prolongation, and ventricular arrhythmias, all of which were prevented by low-dose tetrodotoxin.

Structured PICO

Does selective activation of TTX-S sodium channels by AaH-II drive arrhythmogenic late Na+ current in the heart?

P
Population
Human iPS-derived cardiomyocytes, adult ventricular cardiomyocytes, isolated hearts, and in vivo models
I
Intervention
AaH-II (a peptide from Androctonus australis hector scorpion venom) to selectively activate TTX-S Nav channels
C
Comparator
ATX-II (reference INaL inducer) and nanomolar tetrodotoxin (TTX) concentrations
O
Outcome
Arrhythmogenic late Na+ current (INaL), action potential prolongation, abnormal Ca2+ handling, conduction abnormalities, QT prolongation, and ventricular proarrhythmic eventssurrogate

Selective activation of TTX-S sodium channels is sufficient to generate arrhythmogenic late Na+ current independently of Nav1.5, suggesting a novel target for antiarrhythmic therapy.

Cite This Study

Millet et al. (2026) studied Cardiac arrhythmias. AaH-II vs. ATX-II was evaluated on Late sodium current (INaL) activation and arrhythmogenesis. AaH-II selectively activates tetrodotoxin-sensitive sodium channels to generate arrhythmogenic late Na+ current, causing conduction abnormalities and QT prolongation independently of Nav1.5.

synapsesocial.com/papers/6a9bd4216b95aff0620eb958https://doi.org/10.1093/europace/euag249
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