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RN-1747 is an agonist of transient receptor potential vanilloid 4 (TRPV4).1 It selectively induces calcium influx in HEK293 cells expressing human, rat, or mouse TRPV4 (EC50s = 0.77, 4.1, and 4 µM, respectively) over HEK293 cells expressing human TRPV1, TRPV3, or transient receptor potential melastatin 8 (TRPM8; EC50s = >100, >30, and >30 µM, respectively). RN-1747 (10 µM) induces inward current in Xenopus oocytes expressing human TRPV4. Topical, but not intravenous, administration of RN-1747 induces hypothermia in rats.2
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1. Identification and characterization of novel TRPV4 modulators. Biochem. Biophys. Res. Commun. 389(3), 490-494 (2009).
2. TRPV4 activates autonomic and behavioural warmth-