SB-366791 is a structurally novel and potent TRPV1 antagonist which is capable of inhibiting the capsaicin-, acid- and heat-mediated activation of the receptor but produces little or no effect on a wide range of enzymes, ion channels, GPCRs and other proteins. SB-366791 may prove to be a better tool for unambiguously defining the (patho)physiological role of TRPV1.
In vivo
the TRPV1 antagonist SB366791 reduces the number of flinches but did not improve ambulation and weight-bearing. A sub-analgesic dose of SB366791 potentiates the effects of morphine at doses of
3.0 and 10.0 mg/kg on flinches and weight-bearing but not ambulation. The combination of morphine and SB366791 has potent analgesic effects on bone cancer pain.