A 317491 sodium salt

Biological Activity

A 317491 sodium salt is a selective, high affinity non-nucleotide P2X₃ and P2X_2/3 receptor antagonist (K_i values are 9, 22, 22 and 92 nM at human P2X_2/3, rat P2X₃, human P2X₃ and rat P2X_2/3, respectively); blocks recombinant human and rat P2X₃ and P2X_2/3 receptor-mediated calcium flux (K_i = 22 - 92 nM). Exhibits selectivity over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes (IC₅₀ > 5 μM). Reduces mechanical allodynia and thermal hyperalgesia in the CCI in vivo models. Antinociceptive.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Endogenous opioid mechanisms partially mediate P2X3/P2X2/3-related antinociception in rat models of inflammatory and chemogenic pain but not neuropathic pain.
   McGaraughty et al.
   Br.J.Pharmacol., 2005;146:180
2. X-ray structures define human P2X₃ receptor gating cycle and antagonist action.
   Mansoor et al.
   Nature, 2016;538:66
3. A-317491, a novel potent and selective non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat.
   Jarvis et al.
   Proc.Nat.Acad.Sci.USA, 2002;99:17179
4. 2', 3'-O-(2,4,6,trinitrophenyl)-ATP and A-317491 are competitive antagonists at a slowly desensitizing chimeric human P2X₃ receptor.
   Neelands et al.
   Br.J.Pharmacol., 2003;140:202
5. Effects of A-317491, a novel and selective P2X₃/P2X_2/3 receptor antagonist, on neuropathic, inflammatory and chemogenic nociception following intrathecal and intraplantar administration.
   McGaraughty et al.
   Br.J.Pharmacol., 2003;140:1381

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