Overview
- Ford, A. et al. (2006) Br. J. Pharmacol. 147, S132.
Alomone Labs RO-3 inhibits P2X3 channels expressed in HEK-293 cells.Dose-response curve of P2X3 inhibition by RO-3 (#R-190). hP2X3/HEK-293 cells were loaded with Calcium-6 dye, incubated for 5 min with rising concentrations of RO-3, 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 1.11 µM.
RO-3 is a potent inhibitor of human homomultimeric P2X3 receptor and heteromultimeric P2X2/3 receptor and demonstrates pIC50 value of 7.0 and pIC50=5.9 respectively1.
The compound shows to have to high metabolic stability in rat and human hepatocytes and liver microsomes. It's highly permeable, orally bioavailable, and has a good in vivo plasma half-life in rats. RO-3 is also widely distributed to tissues after administration, with low plasma protein binding and good CNS penetration1.
The P2X receptors are a family of ion channels that are gated by ATP. P2X receptors are widely localized 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 conditions2.
