Jules C. Hancox , Yibo Wang , Caroline S. Copeland , Henggui Zhang , Stephen C. Harmer , Graeme Henderson
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Nitazene opioids and the heart: Identification of a cardiac ion channel target for illicit nitazene opioids
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.