Potent reversible and selective TRPV4 antagonist. Active at mouse, human and rat TRPV4, IC50 = 17, 48 and 133 nM respectively. Also inhibits the endogenous TRPV4-mediated response to 4alpha-PDH (IC50 = 22 nM). Selective for TRPV4 over TRPV1, TRPV2, TRPV3 and TRPM8 channels1. Increases functional bladder capacity and reduces micturition frequency in mice and rats with cystitis1. Inhibits brain edema in middle cerebral artery occlusion mice2. Induces an increase in core body temperature accompanied by increased oxygen consumption in Wistar rats3. Active in vivo.
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