Orally active atypical voltage-gated sodium channel blocker. Inhibits sustained sodium currents (INaL
) and prevents diastolic contracture in isolated atria in vitro
values are 9.6 and 0.55 - 0.79 μ
M respectively). Displays anti-ischemic, bradycardic and cardioprotective activity in vivo
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Anti-ischemic compound KC 12291 prevents diastolic contracture in isolated atria by blockade of voltage-gated sodium channels.
Tamareille et al.
KC 12291: an atypical sodium channel blocker with myocardial antiischemic properties.
John et al.
Cardiovasc.Drug Rev., 2004;22:17
Pharmacological characterisation of sodium channels in sinoatrial node pacemaking in the rat heart.
Letienne et al.
Cardioprotective actions of KC 12291.
Decking et al.