Uses
PPADS is a P2 receptor antagonist, with IC50s of 68 nM (P2X1) and 214 nM (P2X3). PPADS acts as an ATP (nucleotide) mimetic and competes with ATP for its binding site on P2 receptors. PPADS is also a reversible competitive antagonist of the NAADP receptor. PPADS reverses nociceptive hypersensitivity and reduces the increased NO/NOS system and IL-1β in both peripheral and central steps of nervous system[1][2][3].
Definition
ChEBI: An arenesulfonic acid that is pyridoxal 5'-phosphate carrying an additional 2,4-disulfophenylazo substituent at position 6.
Biological Activity
A non-selective P2 purinergic antagonist. Blocks recombinant P2X 1 , P2X 2 , P2X 3 , P2X 5 (IC 50 = 1 - 2.6 μ M), native P2Y 2 -like (IC 50 ~ 0.9 mM), and recombinant P2Y 4 (IC 50 ~ 15 mM) receptors.
IC 50
p2x1 Receptor: 68 nM (IC
50); P2X2 Receptor: 214 nM (IC
50)
References
[1] Billington RA, et al. PPADS is a reversible competitive antagonist of the NAADP receptor. Cell Calcium. 2007 Jun;41(6):505-11. DOI:
10.1016/j.ceca.2006.10.002[2] Brown SG, et al. Actions of a Series of PPADS Analogs at P2X1 and P2X3 Receptors. Drug Dev Res. 2001 Aug;53(4):281-291. DOI:
10.1002/ddr.1197[3] Martucci C, et al. The purinergic antagonist PPADS reduces pain related behaviours and interleukin-1 beta, interleukin-6, iNOS and nNOS overproduction in central and peripheral nervous system after peripheral neuropathy in mice. Pain. 2008 Jul;137(1):81-95. DOI:
10.1016/j.pain.2007.08.017
