RN 1747 is a selective TRPV4 agonist (EC50 values are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively). Shown to display selectivity over other TRP channels (EC50 values are 0.77, >30, >30 and >100 μM for TRPV4, TRPM8, TRPV3 and TRPV1 receptors respectively). Also has been shown to antagonize TRPM8 at relevant concentrations (IC50 = 4 μM).
Vincent et al (2009) Identification and characterization of novel TRPV4 modulators. Biochem.Biophys.Res.Comms. 389 490.
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