Popis: |
CPUY11018 has anti-atrial fibrillation (AF) effects in rats. The effects of CPUY11018 on the transient outward K+ current (Ito) and ultra-rapid delayed rectifier K+ current (IKur) were studied using whole-cell patch clamp techniques and an acetylcholine (ACh)-CaCl2 induced AF model. CPUY11018 inhibited Ito and IKur in a concentration-dependent manner with IC50 values of 18.5 and 1.7 µM, respectively. Inhibition was independent of the depolarizing voltage. In the AF ACh-CaCl2 model, AF duration was effectively shortened after treatment with 5 mg/kg CPUY11018 for 4 days. These results indicate that CPUY11018 is effective in treating AF partly by blocking Ito and IKur. Drug Dev Res 71, 2010. © 2010 Wiley-Liss, Inc. |