Population
Mutant HERG (D540K) channels and wild-type HERG channels expressed in Xenopus oocytes
Comparison
2 microM MK-499 and membrane hyperpolarization vs Wild-type HERG channels
Design
Preclinical
Authors
Loading...
Confirms activation-gate trapping in HERG block by methanesulfonanilides; hypothesis-generating for human cardiac safety.
Provides direct evidence that slow recovery from HERG channel block by methanesulfonanilides is due to trapping of the compound in the inner vestibule by closure of the activation gate.
Mitcheson et al. (2000) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: