Journal of Molecular and Cellular Cardiology Plus (Dec 2024)

Nitazene opioids and the heart: Identification of a cardiac ion channel target for illicit nitazene opioids

  • Jules C. Hancox,
  • Yibo Wang,
  • Caroline S. Copeland,
  • Henggui Zhang,
  • Stephen C. Harmer,
  • Graeme Henderson

Journal volume & issue
Vol. 10
p. 100118

Abstract

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The growing use of nitazene synthetic opioids heralds a new phase of the opioid crisis. However, limited information exists on the toxic effects of these drugs, aside from a propensity for respiratory depression. With restricted research availability of nitazenes, we used machine-learning-based tools to evaluate five nitazene compounds' interaction potential with the hERG potassium channel, a key drug antitarget in the heart. All nitazenes were predicted to inhibit hERG with low μM IC50 values. These findings indicate a potential for proarrhythmic hERG block by nitazene opioids, warranting detailed cardiac safety evaluations of these drugs.

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