Background:

SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nMtarget: VR1/TRPV1IC 50: 5.7±1.2 nM [1] SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis indicated a competitive mechanism of action with a pA2 of 7.71.[1] SB-366791 showed a concentration-dependent potentiation of pH 5-induced 45Ca2+uptake in CHO cells expressing rat TRPV1 but not in untransfected cells[2]

参考文献:
[1]. M.J. Gunthorpe et al. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology, 2004 Jan, 46(1):133-49.
[2]. Gavva NR et al. Proton Activation Does Not Alter Antagonist Interaction with the Capsaicin-Binding Pocket of TRPV1. Mol Pharmacol, 2005 Dec, 68(6), 1524-33.