Overview
- Honore, P. et al. (2006) J. Pharmacol. Exp. Ther. 319, 1376.
- Donnelly-Roberts, D.L. et al. (2009) Br. J. Pharmacol. 157, 1203.
Alomone Labs A-740003 inhibits human P2X7 receptors expressed in HEK-293 cells.Dose-response curve of hP2X7 inhibition by A-740003 (#A-420). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of A-740003, and stimulated with 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 72 nM.
A-740003 is a potent, selective, and competitive antagonist of the P2X7 receptor, with IC50 values of 18 nM and 44 nM for rat and human P2RX7, respectively1. The compound shows weak or no activity on other P2 receptors.
A-740003 has the ability to reduce neuropathic pain and tumor growth in vivo. Systemic administration of A-740003 in rat produces dose-dependent antinociception in a spinal nerve ligation model1,2.
The P2X receptor family includes seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. They are highly expressed on immune cells including glial cells, macrophages and other antigen-presenting cells1,2.
