SB-366791 is a potent and selective TRPV1 antagonist. SB-366791 inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. SB-366791 decreased capsaicin-induced Ca2+ influx in cultured trigeminal ganglion cells in a concentration-dependent manner (0.5-10 microM) with an IC50 of 651.9 nM. SB366791 is a more selective and in vivo also a more potent TRPV1 receptor antagonist than capsazepine in the rat therefore, it may promote the assessment of the therapeutic utility of TRPV1 channel blockers.