V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin ( CAP )- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC 50 =423.2 nM for CAP ; IC 50 =180.3 nM for acid). V116517 can be used for the research of pain.