Overview
- Michel, A.D. et al. (2008) Br. J. Pharmacol. 153, 737.
- Michel, A.D. et al. (2008) Br. J. Pharmacol. 155, 738.
Alomone Labs GW 791343 hydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.Dose response curve of hP2X7 inhibition by GW 791343 hydrochloride (# G-115). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of GW 791343 hydrochloride, and stimulated by 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated as 0.4 µM.
GW 791343 hydrochloride is a species-specific allosteric modulator of purinergic P2X7 receptor. The compound acts as a negative modulator of human P2X7 receptors and as a positive modulator of rat P2X71. GW 791343 displays pIC50 values between 6.9 - 7.2 on human P2X7 receptors1,2.
P2X receptors are a family of ligand-gated cation channels activated by extracellular ATP, a ligand that mediates numerous cellular and biological functions. Seven members of P2X receptors are identified and shown to function either in homomeric or heteromeric combinations. The P2X receptors are widely localized in cell types of almost every origin, including neuronal, muscular, epithelial and immune and play a pivotal role in models of various pain conditions. P2X7 receptors are responsible for mediating the release of proinflammatory cytokines in inflammatory/immune conditions and pain1,3,4.
