p2x receptor

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

BzATP triethylammonium salt is a P2X7 receptor agonist.

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.

(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM, suitable for respiratory diseases research.

Ivermectin (MK-933) is an activator of glutamate-gated chloride channels (GluCls) with antiparasitic activity.

ATP disodium salt (Adenosine-Triphosphate) is a P2 purinoceptor agonist.

Lappaconitine ((+)-Lappaconitine), isolated from Aconitum sinomontanum Nakai, was characterized as an analgesic.

Gefapixant citrate (AF-219 citrate) is an orally available, highly potent P2X3 receptor antagonist with antitussive properties that inhibits hP2X2/3. It can be used to study chronic cough.

Sodium metatungstate (Sodium polyoxotungstate) is a potent inhibitor of ecto-nucleoside triphosphate diphosphohydrolase (NTPDase), with Ki values of 2.58 μM for NTPDase 1, 3.26 μM for NTPDase 3, and 28.8 μM for NTPDase 2.

Minodronic acid monohydrate is an farnesyl diphosphate synthase inhibitor that acts as a bone resorption inhibitor.

NP-1815-PX is a selective P2X4 receptor antagonist with anti-inflammatory and analgesic properties. It inhibits guinea pig tracheal/bronchial smooth muscle contraction and can be used to study chronic pain.

AF-353 (Ro-4), an effective and orally bioavailable antagonist of the P2X3/P2X2/3 receptor, inhibits human and rat P2X3 (pIC50= 8.0).

AZ 11645373 (3-[1-[[(3'-NITRO[1,1'-BIPHENYL]-4-YL)OXY]METHYL]-3-(4-PYRIDINYL)PROPYL]-2,4-THIAZOLIDINEDIONE) is a highly selective and potent human P2X7 receptor antagonist that has no effect on mouse/rat P2X7 receptor.

Indophagolin is a potent, indoline-containing autophagy inhibitor with an IC50 of 140 nM, and it antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40, and 3.49 μM, respectively.

A 438079 is a potent and selective antagonist of the P2X7 receptor (pIC50: 6.9).

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

PSB-12062 (N-(p-Methylphenylsulfonyl)phenoxazine) is a potent and selective antagonist of P2X4(IC50 of 1.38 μM for human P2X4).

α,β-Methylene ATP trisodium, a phosphonate analog of ATP, is a selective P2X agonist that induces enhanced contraction of UBSM. α,β-Methylene ATP trisodium inhibits P2X1 and P2X3, but is inactive against P2X2, 4 and 7.

A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.