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Cardioselective KATP channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas

…, U Gerlach, H Goegelein, J Hartung…

文献索引:Englert; Gerlach; Goegelein; Hartung; Heitsch; Mania; Scheidler Journal of Medicinal Chemistry, 2001 ,  vol. 44,  # 7  p. 1085 - 1098

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被引用次数: 44

摘要

Sulfonylthioureas exhibiting cardioselective blockade of ATP-sensitive potassium channels (KATP channels) were discovered by stepwise structural variations of the antidiabetic sulfonylurea glibenclamide. As screening assays, reversal of rilmakalim-induced shortening of the cardiac action potential in guinea pig papillary muscles was used to probe for activity on cardiac KATP channels as the target, and membrane depolarization in CHO cells ...