472981-92-3

SB-366791 (472981-92-3) is a potent (IC50 = 0.7 μM) and selective TRPV1 blocker.1,2 Selective for TRPV1 in a panel of 47 different binding assays.

A potent and selective vanilloid receptor (TRPV1) antagonist. An effective antagonist of hTRPV1 when stimulated by capsaicin, acid, or noxious heat.

ChEBI: 3-(4-chlorophenyl)-N-(3-methoxyphenyl)-2-propenamide is a member of cinnamamides and a secondary carboxamide.

Potent, selective and competitive vanilloid TRPV1 (VR1) receptor antagonist (pA 2 = 7.71 at hVR1); antagonizes hTRPV1 receptors activated by agonists, noxious heat, but not protons. Displays selectivity over a wide range of receptors and systems including CB 1 and CB 2 receptors, voltage-gated Ca 2+ channels and the hyperpolarization-activated current (I h ). Also available as part of the Vanilloid TRPV1 Receptor Tocriset™ .

SB-366791 might exhibit analgesic properties on bone cancer-related pain behavior.

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1) Gunthorpe, et al., (2004) Identification and characterization of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist; Neuropharmacology 46 133 2) Varga et al. (2005) Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat; Neurosci. Lett.. 385 137