af-353

AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).IC50 value: pIC50 = 8.0 (pIC50, for P2X3)Target: P2X3/P2X2/3 receptorin vitro: AF-353 is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1]in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2]

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

Research Areas >> Cancer

[1]. Gever JR, et al. AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br J Pharmacol. 2010 Jul;160(6):1387-1398.

[2]. Munoz A, et al. Modulation of bladder afferent signals in normal and spinal cord-injured rats by purinergic P2X3 and P2X2/3receptors. BJU Int. 2012 Oct;110(8 Pt B):E409-414.

Adenosine 5'-triphosphate disodium salt | KN-62 | A-740003 | A 438079 | AZD9056 hydrochloride | PSB-12062 | A-317491 | A 804598 | A 839977 | Gefapixant | GW791343 | Lappaconitine | CE-224535 | JNJ-54175446