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

…, U Gerlach, H Goegelein, J Hartung…

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

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Citation Number: 44

Abstract

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 ...