Dimebolin

溶解度:Soluble to 25 mM in water and to 50 mM in DMSO

储存条件:Desiccate at +4°C

生物活性

Orally active atypical voltage-gated sodium channel blocker. Inhibits sustained sodium currents (INaL) and prevents diastolic contracture in isolated atria in vitro (IC50 values are 9.6 and 0.55 - 0.79 μM respectively). Displays anti-ischemic, bradycardic and cardioprotective activity in vivo

参考文献

Decking et al (1998) Cardioprotective actions of KC 12291. Naunyn-Schmied.Arch.Pharmacol. 358 547. Tamareille et al (2002) Anti-ischemic compound KC 12291 prevents diastolic contracture in isolated atria by blockade of voltage-gated sodium channels. J.Cardiovasc.Pharmacol. 40 346. PMID: 12198320. John et al (2004) KC 12291: an atypical sodium channel blocker with myocardial antiischemic properties. Cardiovasc.Drug Rev. 22 17. PMID: 14978516.