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Journal Article

Citation

Hancox JC, Copeland CS, Harmer SC, Henderson G. J. Mol. Cell. Cardiol. Plus 2023; 6: e100049.

Copyright

(Copyright © 2023, Elsevier Publishing)

DOI

10.1016/j.jmccpl.2023.100049

PMID

38143960

PMCID

PMC10739592

Abstract

Synthetic cannabinoid receptor agonists (SCRAs) have been associated with QT interval prolongation. Limited preclinical information on SCRA effects on cardiac electrogenesis results from the rapid emergence of new compounds and restricted research availability. We used two machine-learning-based tools to evaluate seven novel SCRAs' interaction potential with the hERG potassium channel, an important drug antitarget. Five SCRAs were predicted to have the ability to block the hERG channel by both prediction tools; ADB-FUBIATA was predicted to be a strong hERG blocker. ADB-5Br-INACA and ADB-4en-PINACA showed varied predictions. These findings highlight potentially proarrhythmic hERG block by novel SCRAs, necessitating detailed safety evaluations.


Language: en

Keywords

Cannabis; hERG; Long QT; Synthetic cannabinoid receptor agonists (SCRAs); Torsades de pointes

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