p2x

P2X receptor-1 is a potential inhibitor of P2X receptor, used in the treatment of pain and inflammation.

P2X3-IN-1 (example 7) is a P2X3 receptor inhibitor suitable for neurogenic disease research [1].

Compound 38, also known as Compound 4, is a potent, orally active P2X3 antagonist that demonstrates inhibitory activity with IC50 values of 0.132 µM, 0.165 µM, and 0.421 µM against human (hP2X3), rat (rP2X3), and guinea pig (gpP2X3) P2X3 receptors, respectively [1].

P2X3 antagonist 34, a potent, selective, and orally active antagonist, targets the P2X3 homotrimeric receptor, exhibiting IC50s of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors respectively. It shows reduced activity against P2X2 3 heterotrimeric receptors across human, rat, and guinea pig models. Notably, this compound demonstrates a significant anti-tussive effect without altering taste[1].

P2X7 receptor antagonist-5 (compound 13a) is a potent, orally active, and long-lasting antagonist of the P2X7 receptor.

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

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

P2X7 receptor antagonist-2 is a highly potent inhibitor of the P2X7 receptor, with a pIC50 value range of 6.5-7.5 and demonstrated efficacy in combating neuroinflammation [1].

P2X7 receptor antagonist-1 is a purinergic P2X7 receptor antagonist with anti-neuroinflammatory effects.

P2X3 antagonist (36) is a compound that functions as a P2X3 antagonist.

P2X7 receptor antagonist-3 is a potent inhibitor of the P2X7 receptor, with IC50 values of 4.2 nM in humans and 6.8 nM in rats, demonstrating its high efficacy across species.

P2X7-IN-2, a P2X7 receptor inhibitor, effectively suppresses IL-Iβ release, demonstrating an inhibitory concentration (IC50) value of 0.01 nM. This compound is utilized in the study of autoimmunity, inflammation, and cardiovascular disease.

P2X2 3 Modulator-1 (Compound 46) serves as a modulator of P2X2 3 receptors and has applications in researching pain, central nervous system disorders, and inflammation [1].

P2X7-IN-2 TFA (compound 58) is a P2X7 receptor inhibitor with an IC50 value of 0.01 nM for inhibiting IL-Iβ release, used in research on autoimmunity, inflammation, and cardiovascular disease [1].

Compound 14a (P2X7 receptor antagonist-4) is a P2X7R antagonist with IC50 values of 64.7 nM in humans and 10.1 nM in mice. It inhibits the activation of the NLRP3 inflammasome, which subsequently reduces the expression of caspase-1, gasdermin D, IL-1β, and IL-18 in the kidneys of mice with sepsis-induced damage [1].

P2X4 antagonist-1 is a potent P2X4 receptor antagonist used in the study of neurological, cardiovascular, and immune system diseases.

P2X4 antagonist-2 is a specific antagonist for P2X4 with an IC50 of 24 nM [1].

P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC50 of 54.9 nM. It is utilized in the study of neuropathic pain models.

AZ10606120 dihydrochloride is a selectable, potent, high-affinity receptor antagonist with K D values of 1.4 and 19 nM at human and rat P2X 7 receptors, respectively. AZ10606120 dihydrochloride inhibits tumor growth and has anti-angiogenic activity. AZ 10606120 acts as a negative allosteric modulator when bound to a site coupled to the ATP binding site.

JNJ-54175446 (JNJ-5446) is a CNS-permeable and selective P2X7 receptor antagonist that attenuates the release of IL-1β IL-18 from microglia, and may be used in the study of depression.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.

JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively.

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+ H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.