Key result
GPR4 antagonist 3b demonstrates effectiveness in a mouse model of MI.
Compound 3b is a novel, potent, and selective GPR4 antagonist that shows preclinical effectiveness as a potential drug lead for treating myocardial infarction.
GPR4, a pH-sensing G protein-coupled receptor, is highly expressed in endothelial cells and may be activated in myocardial infarction due the decreased tissue pH. We are interested in GPR4 antagonists as potential effective pharmacologic tools and/or drug leads for the treatment of myocardial infarction. We investigated the structure-activity relationship of a known GPR4 antagonist 1 as a lead compound to identify 3b as the first potent and selective GPR4 antagonist, whose effectiveness was demonstrated in a mouse myocardial infarction model.
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Fukuda et al. (2016) studied Myocardial infarction. GPR4 antagonist 3b was evaluated on Effectiveness in a mouse myocardial infarction model. The potent and selective GPR4 antagonist 3b demonstrated effectiveness as a potential drug lead in a mouse model of myocardial infarction.
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