Ontology highlight
ABSTRACT:
SUBMITTER: Smith CD
PROVIDER: S-EPMC3896386 | biostudies-literature | 2013 Nov
REPOSITORIES: biostudies-literature
Smith Chris D CD Wang Aixia A Vembaiyan Kannan K Zhang Jingqun J Xie Cuihong C Zhou Qiang Q Wu Guogen G Chen S R Wayne SR Back Thomas G TG
Journal of medicinal chemistry 20131105 21
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 was employed on the basis of the RyR2-R4496C mutant ...[more]