P2X Receptor

A 740003 is a novel competitive antagonist of P2X7 receptors (IC50 values = 40 nM for human and 18 nM for rat).

NF279 is a suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC50/KB ~ 1 μM in smooth muscle).

A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.

A-438079 HCl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 >> 10 uM).

AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).

A 438079 Hcl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).

A-804598 is a P2X7 selective, competitive antagonist with the IC50s value for human, rat and mouse channels of 11, 10 and 9 nM, respectively.

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.

Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.

AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10?nM.

A 839977 is a P2X7 selective antagonist.

CE-224535 is a selective P2X7 receptor antagonist.

Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.

NSC 102533 is a potent antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel involved in inflammation and immune regulation. It effectively inhibits ATP-induced dye uptake in HEK293 cells expressing human P2X7 receptors with an IC₅₀ of 22.4 nM. NSC 102533 also suppresses ATP-induced IL-1β secretion in human THP-1 monocytes and primary mouse peritoneal macrophages, with IC₅₀ values of 9.8 nM and 11.2 nM, respectively, demonstrating strong anti-inflammatory activity.

In addition to its immunomodulatory effects, NSC 102533 exhibits antivenom potential by inhibiting Bothrops atrox venom proteolysis in a concentration-dependent manner. In in vivo studies, intradermal administration of NSC 102533 (3 mg/kg) significantly reduces skin hemorrhage induced by B. atrox and B. jararaca venom and attenuates carrageenan-induced paw edema in mice at doses between 0.01 and 1 mg/kg. These properties highlight NSC 102533 as a valuable pharmacological tool for studying P2X7 receptor–mediated inflammatory responses and venom-induced pathology.