A-784168 is a transient receptor potential vanilloid 1 (TRPV1) competitive antagonist. It inhibits capsaicin-induced activation of TRPV1 in 1321N1 cells expressing TRPV1 (IC = 25 nM for the human receptor). A-784168 is selective for TRPV1 over a panel of 74 neurotransmitter receptors, ion channels, and other TRP channels at 50 μM but does act as an antagonist at TRP melastatin 8 (TRPM8; IC = 20.8 μM). It also inhibits TRPV1 activation induced by mildly acidic conditions, N-arachidonoyl dopamine (NADA; ), or anandamide in HEK293 cells (ICs = 14, 33.7, and 35.1 nM, respectively). It inhibits capsaicin-induced currents in primary rat dorsal root ganglion neurons (IC = 10 nM). A-784168 (200 μmol/kg) inhibits thermal hypersensitivity and mechanical hypersensitivity induced by NGF in rats.