V116517 is a potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM.
V116517 shows high selectivity for TRPV1 over TRPV3 and TRPV4 (>10 uM) in a panel of 66 ion channels, receptors, transporters.
V116517 dose-dependently reverses thermal hyperalgesia with ED50 of 2 mg/kg (p.o.) in acute inflammatory CFA model; shows excellent aqueous solubility, metabolic stability, oral bioavailability in multiple species, and excellent efficacy in a variety of animal pain models.
