Potent and selective TRPV4 antagonist (IC50
values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca2+
influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarction in vivo
models. Selective over a panel of ~200 human receptors, channels and enzymes. Orally active.
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An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Thorneloe et al.