- Gever, J.R. et al. (2010) Br. J. Pharmacol. 160, 1387.
- Alomone Labs AF-353 inhibits P2X3 receptors expressed in HEK-293 cells.Dose-response curve of P2X3 inhibition by AF-353 (#A-375). Cells were loaded with Calcium-6 dye, incubated for 5 min with increasing concentrations of AF-353, and stimulated by 3 µM α,β-MeATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was determined as 9.84 nM.
AF-353 is a highly potent and selective antagonist of P2X3 and P2X2/3 purinergic receptors. The compound is orally bioavailable and is being used as an in vivo tool for studying the role of P2X channels in animal pain models.
P2X receptors are a family of ion channels that are gated by ATP. They are expressed in cell types of almost every origin, including neuronal, muscular, epithelial and immune and have been shown to play a pivotal role in models of various pain conditions1.
Antagonism of P2X3 receptors can reduce arterial pressure and basal sympathetic activity and normalizes carotid body hyper-reflexia in rats with hypertension2.
AF-353 (#A-375) is a highly pure, synthetic, and biologically active compound.