Key result
Verapamil accesses delayed rectifier K channel binding sites from the cytoplasm in its uncharged form.
Population
Chick dorsal root ganglion (DRG) neurons
Design
Preclinical
Authors
Loading...
Provides no immediate clinical implications for arrhythmia management; extends mechanistic understanding of verapamil on K channels in preclinical models.
Verapamil blocks delayed rectifier K channels by accessing its binding domain from the cytoplasm in an uncharged form, which can then be protonated.
Catacuzzeno et al. (1999) studied this question. Verapamil and D890 was evaluated on Voltage dependence and mechanism of delayed rectifier K channel block. Verapamil reaches its binding site on delayed rectifier K channels in the uncharged form from the cytoplasm, with unbinding kinetics consistent with rapid protonation equilibrium of the bound drug.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: