P2X Receptor Inhibitor

PSFL2915 is a selective, orally active P2X receptor inhibitor with oral effectiveness, with an IC₅₀ of 0.319 μM for human P2X3, 0.261 μM for rat P2X2/3, and 13.3 μM for human P2X2. PSFL2915 exhibits ~42-fold selectivity over human P2X2. PSFL2915 can be used for the research of chronic cough.

AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.

Diadenosine pentaphosphate pentasodium is an agonist and negative modulator of the P2X1 receptor, an endogenous vasoactive purine dinucleotide that can be isolated from platelets. Diadenosine pentaphosphate pentasodium mediates negative regulation of dendrite growth and number by activating homologous and heterologous P2X1 receptors, which triggers a transient and moderate increase in intracellular calcium levels within dendritic growth cones. Diadenosine pentaphosphate pentasodium is widely present in secretory vesicles such as platelets, chromaffin cells and brain synaptosomes, and exhibits selective activity on dendrite growth of cultured hippocampal neurons, inhibiting only dendrite growth without affecting axon growth. Diadenosine pentaphosphate pentasodium has a weaker ability to compete with RcCHAD for binding to polyP than short-chain polyPs.

Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis.

Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression.

Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

Taspine is a natural product with anti-inflammatory activity. Taspine suppresses P2X4 receptor activity via PI3K inhibition. Taspine inhibits pro-inflammatory signalling via inhibition of P2X4 receptors in macrophage.

GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC₅₀ of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.

P2X3-IN-1 (example 7) is an inhibitor of P2X3 receptor. P2X3-IN-1 can be used for neurogenic diseases research.

7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders.

P2X7-IN-2 TFA (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 TFA inhibits IL-Iβ release with an IC₅₀ value of 0.01 nM. P2X7-IN-2 TFA can be used for the research of autoimmunity, inflammation and cardiovascular disease.

P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC₅₀ value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease.

P2X4 antagonist-3 (Compound 14c) is a P2X4 antagonist with an IC₅₀ value of 1.2 μM. P2X4 antagonist-3 is promising for research of neuroinflammation, chronic pain, and cancer progression.

Purotoxin 1 is a P2X3 receptor inhibitor. Purotoxin 1 shows antinociceptive properties in animal models of inflammatory pain. Purotoxin 1 can be isolated from the venom of the wolf spider Geolycosa sp.

NF864 is a selectivelyP2X1 receptorinhibitor in human platelets.

P2X4-IN-1 (Compound 1) is an orally active P2X4 inhibitor. P2X4-IN-1 can be used in the study of prophylaxis disease.

Z1456467176 is an allosteric inhibitor of P2X7R. Z1456467176 binds to P2X7R, prevents ATP-induced channel opening and receptor activation, and blocks ATP-induced activation of the NLRP3-caspase-1-IL-1β pathway. Z1456467176 inhibits ATP-induced P2X7R pore formation in macrophages, as well as IL-1β secretion induced by ATP or BzATP. Z1456467176 alleviates gouty joint inflammation in rats. Z1456467176 can be used for the research of gouty arthritis.

GSK1370319A is a human P2X7 receptor inhibitor with an IC₅₀ of 474 nM and a K_i of 176 nM. GSK1370319A inhibits the production of IL-1β, reduces the generation of reactive oxygen species (ROS), and increases the survival rate of macrophages. GSK1370319A can be used for the research of inflammatory bowel disease.

P2X receptor-1 is a potential inhibitor of P2X receptor for the research of pain and inflammation.

HW091077 is a highly selective P2X3 receptor antagonist with an IC₅₀ of 17 nM. HW091077 blocks ATP-induced calcium influx and cell depolarization to inhibit cough reflex pathways. HW091077 is promising for research of chronic cough.