Overview
- Gunthorpe, M.J. et al. (2004) Neuropharmacology 46, 133.
Alomone Labs SB-366791 inhibits TRPV1 channels expressed in C6 cells.mTRPV1-C6 cells were loaded with Fluo-3 AM. Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following agonist application. 10 minutes pre-incubation with 5 and 50 µM SB-366791 (#S-180) inhibited 10 µM Capsaicin (#C-125)-evoked rise in intracellular Ca2+. Normalized fluorescence before and after application (arrow) of 10 µM Capsaicin in cells pre-incubated with 0 nM (DMSO equivalent control, black), 5 µM (gray) or 50 µM SB-366791 (dotted line).
SB-366791 is a potent and selective TRPV1 channel antagonist1. Novel strategies for the treatment of bone cancer pain have shown that morphine in combination with SB-366791 has potent analgesic effects on bone cancer pain2.
TRPV1 (Vanilloid receptor-1) is a member of a distinct subgroup of transient receptor potential (TRP) family. These channels are highly expressed on primary nociceptors. TRPV1 can be activated by several different stimuli such as heat, acid, certain arachidonic acid derivatives and direct phosphorylation via PKC. TRPV1 may serve a central role in inflammatory nociception3.
Studies have shown that local intradermal treatment with SB-366791 compound has the ability to reduce thermal hyperalgesia and mechanical allodynia without affecting mechanical hyperalgesia4.
