Overview
- Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
Alomone Labs Capsazepine inhibits TRPV1 channels expressed in C6 cells.mTRPV1-C6 cells were loaded with Fluo-3AM. Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following agonist application. 5 minutes pre-incubation with 10 µM Capsazepine (#C-120) 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 without (black) or with 10 µM Capsazepine (gray).
Capsazepine is a synthetic, competitive and selective antagonist of TRPV1 (transient receptor potential vanilloid 1)1 and an activator of amiloride-sensitive epithelial Na+ channel gamma (ENaCγ). It also inhibits K+-dependent ATP hydrolysis with no effect on Na+-ATPase2,3.
Capsazepine is being used in in vitro and in vivo pharmacological studies as a standard TRPV1 competitive antagonist.
Capsazepine exhibits potent inhibition of expression of the iNOS gene in LPS-stimulated murine macrophages through inactivation of NF-κB4.
The amiloride-sensitive epithelial Na+ channel (ENaC) regulates Na+ homeostasis into cells and across epithelia5.
TRPV1 is a member of a distinct subgroup of transient receptor potential (TRP) ion channels. These channels are highly expressed on primary nociceptors and can be activated by several different stimuli such as heat, acid, certain arachidonic acid derivatives and direct phosphorylation via PKC6.
