biological activity | AF-353 (Ro-4), selective and orally bioavailable antagonists of P2X3 receptor and P2X2/3 receptor have pIC50 values of 8.06, 8.05 and 7.41 for human P2X3, rat P2X3 and human P2X2/3, respectively. |
Target | TargetValue hP2X3 (Cell-free assay) 8.06(pIC50) rP2X3 (Cell-free assay) 8.05(pIC50) hP2X2/3 (Cell-free assay) 7.41(pIC50) |
Target | Value |
hP2X3
(Cell-free assay)
| 8.06(pIC50) |
rP2X3
(Cell-free assay)
| 8.05(pIC50) |
hP2X2/3
(Cell-free assay)
| 7.41(pIC50) |
Use | a p2x3 receptor antagonist. AF353 is a P2X3 receptor antagonist. Antagonism of the P2X3 receptor is one of the potential therapeutic strategies for the management of neuropathic pain because P2X3 receptors are predominantly localized on small to medium diameter C- and Aδ-fiber primary afferent neurons, which are related to the pain-sensing system. |