P2X4 Receptor Antagonist

5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC₅₀ of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).

BAY-1797, a chemical probe, is a potent, orally active, and selective P2X4 antagonist, with an IC₅₀ of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects.

BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC₅₀ of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.

NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC₅₀ of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis).

PSB-12054 is a P2X4 receptor antagonist with IC₅₀ values of 0.19 μM, 2.10 μM and 1.77 μM against human, rat and mouse receptors, respectively, and exhibits selectivity over other human P2X receptor subtypes. PSB-12054 inhibits ATP-induced calcium influx, suppresses shear stress-induced transverse Ca²⁺ wave generation, and elevates basal Ca²⁺ levels in rat atrial myocytes. PSB-12054 binds to the 5-HT2B receptor. PSB-12054 can be used in research related to neuropathic pain, traumatic brain injury, cerebral ischemia and spinal cord injury.

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

NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC₅₀ value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection.

P2X4 antagonist-1 is a P2X4 receptor antagonist with an IC₅₀ of 15 nM. P2X4 antagonist-1 inhibits ATP (HY-B2176)-induced calcium influx. P2X4 antagonist-1 can be used for the research of pain syndromes, endometriosis, cancer.

P2X4 antagonist-4 (compound 64) is a potent P2X4R antagonist with an IC₅₀ value of 8 µM. P2X4 antagonist-4 blocks the ATP-induced NLRP3 inflammasome activation and release of IL-1β.

P2X4 antagonist-2 is an antagonist for P2X4 with an IC₅₀ of 24 nM.