A-317491 

A-317491 is a potent, selective and non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors, with K_is of 22, 22, 9, and 92 nM for hP2X₃, rP2X₃, hP2X_2/3, and rP2X_2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X₃ and P2X_2/3 receptor-mediated calcium flux^[1][2].

A-317491 potently blocks recombinant human and rat P2X₃ and P2X_2/3 receptor-mediated calcium flux (K_i=22-92 nM) ^[1].
A-317491 (1 nM-10 μM) produces a concentration-dependent block of dorsal root ganglion (DRG) currents with an IC₅₀ of 15 nM^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

A-317491 (0.1-30 mg/kg; a single s.c.) dose-dependently reverses inflammatory mechanical hyperalgesia in rats^[2].
A-317491 (3-30 mg/kg; a single .v.) exhibits the plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

565.57

Solid

C₃₃H₂₇NO₈

475205-49-3

O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[[email protected]]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O

Room temperature in continental US; may vary elsewhere.

• [1]. Jarvis MF, et, al. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84.  [Content Brief]

  [2]. Wu G, et, al. A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53.  [Content Brief]