Key result
NE-10064 (azimilide) selectively blocked IKr (IC50 0.4 microM) over IKs (IC50 3 microM) and inhibited ICa in a use-dependent manner in animal cardiac tissues.
Population
Ferret papillary muscles and guinea pig ventricular myocytes
Design
Preclinical
Authors
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Azimilide's ion-channel profile merits human testing; leaves open translation to clinical arrhythmia management.
NE-10064 (azimilide) acts as a relatively selective blocker of IKr over IKs and inhibits ICa in a use-dependent manner, explaining its effects on cardiac repolarization.
Fermini et al. (1995) studied this question. NE-10064 (azimilide) was evaluated on Cardiac repolarization (effective refractory period, action potential duration, and ion currents). NE-10064 (azimilide) selectively blocked IKr (IC50 0.4 microM) over IKs (IC50 3 microM) and inhibited ICa in a use-dependent manner in animal cardiac tissues.
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