Active Ingredient: AMOXAPINE
Amoxapine exhibits a 'triple threat' mechanism of hERG liability, significantly increasing the risk of QT prolongation and sudden death : - Direct Blockade: It potently inhibits hERG potassium currents by binding inside the channel pore (IC50=5.1μM). - Trafficking Disruption: It chronically reduces the transport of hERG proteins to the cell surface membrane (IC50=15.3μM). - Pro-apoptotic Effect: It has been shown to trigger apoptosis (programmed cell death) in hERG-expressing cells. This multi-level interference with cardiac repolarization makes it a high-risk antidepressant regarding cardiotoxicity.
https://doi.org/10.1007/s00210-010-0496-7