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Drofenine, was selective for TRPV3 in that activation of TRPA1, M8, V1, V2, and V4, which are known to be activated by the TRPV3 agonists 2-APB and/or carvacrol, was not observed at concentrations up to 1 mmol/L. A detectable change in TRPV3 activity was observed at concentrations as low as 30 μmol/L and increased in a concentration-dependent manner. At concentrations greater than 500 μmol/L, calcium flux exhibited some evidence of TRPV3 independence based on small and comparable responses in both native HEK-293 cells and other TRP channel overexpressing cell lines. The maximum change in cytosolic calcium (ΔF) for drofenine (EC50 = 207 μmol/L) was comparable to the known TRPV3 agonists 2-APB (EC50 = 78 μmol/L) and carvacrol (EC50 = 438 μmol/L).