Novel carvedilol analogues that suppress store-overload-induced Ca2+ release
CD Smith, A Wang, K Vembaiyan, J Zhang…
Index: Smith, Chris D.; Wang, Aixia; Vembaiyan, Kannan; Zhang, Jingqun; Xie, Cuihong; Zhou, Qiang; Wu, Guogen; Chen, S. R. Wayne; Back, Thomas G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 21 p. 8626 - 8655
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Citation Number: 9
Abstract
Carvedilol is a uniquely effective drug for the treatment of cardiac arrhythmias in patients with heart failure. This activity is in part because of its ability to inhibit store-overload-induced calcium release (SOICR) through the RyR2 channel. We describe the synthesis, characterization, and bioassay of ca. 100 compounds based on the carvedilol motif to identify features that correlate with and optimize SOICR inhibition. A single-cell bioassay ...
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