Novel 3-cyanoisoquinoline Kv1.5 antagonists demonstrate excellent potency, selectivity, and oral bioavailability in preclinical models, suggesting potential for atrial fibrillation treatment.
Should not yet change AF practice; leaves open clinical translation of these Kv1.5 antagonists.
Novel 3-cyanoisoquinoline Kv1.5 antagonists have been prepared and evaluated in in vitro and in vivo assays for inhibition of the Kv1.5 potassium channel and its associated cardiac potassium current, IKur. Structural modifications of isoquinolinone lead 1 afforded compounds with excellent potency, selectivity, and oral bioavailability.
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Trotter et al. (2006) studied this question.
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