P2X Receptor

BzATP triethylammonium salt is a P2X7 receptor agonist.

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

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

Brilliant blue G-250 (Acid blue 90, Coomassie Brilliant Blue G) is an antagonist of the P2X7 purinergic receptor.

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

CTP disodium dihydrate is an agonist of P2X4 purinergic receptor

CI 75300 targets the P2X purinoceptor 7 (human).

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.

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.

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

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

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 μみゅーM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μみゅーM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μみゅーM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

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

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.

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.

A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).

KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μみゅーM.

Bongkrekic acid (Bongkrekic Acid (ammonium salt)) is a mitochondrial toxin secreted by Burkholderia gladioli that inhibits adenine nucleotide translocase (ANT).Bongkrekic acid Bongkrekic acid Bongkrekic acid induces extracellular traps in neutrophils through signaling mediated by p38, ERK, PAD4, and P2X1.

Sivopixant (S-600918) (S-600918) is a potent and selective antagonist of P2X3 receptor (P2X3 IC 50 =4.2 nM; P2X2 3 IC 50 =1100 nM). Sivopixant shows strong analgesic effect .

A-740003 (A 740003) is an effective and specific P2X7 receptor antagonist (IC50: 18 40 nM, for rat human). It can reduce nociception in animal models of persistent neuropathic and inflammatory pain, and also reduce neuroblastoma tumor growth in mice.

A 438079 hydrochloride (A-438079 HCl) is a potent and selective P2X7 receptor antagonist with pIC50 of 6.9.

JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively).

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

1. Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects, may be used for the treatment of neurodegenerative diseases such as arthritis.

Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.

AZD9056 hydrochloride is a P2X7 inhibitor，Which plays a significant role in pain-causing diseases and inflammation.

RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2/3 receptor

GW791343 dihydrochloride (GW791343 (HCl)) is a P2X7 allosteric modulator.

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

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 μみゅーM, respectively.

Eliapixant (BAY 1817080) (BAY 1817080) is a potent and selective P2X3 receptor antagonist, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough.

A-317491 (ABT 202) is a non-nucleotide P2X3 ( Ki: 22 nM) and P2X2/3 receptor (Ki: 9 nM) antagonist, which inhibits calcium flux mediated by the receptors.

Opiranserin (VVZ-149) hydrochloride is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μみゅーM, respectively. It shows antagonistic activity on rP2X3 (IC50=0.87 μみゅーM). It is development as an injectable agent for the treatment of postoperative pain.

5-BDBD is a potent and selective P2X4 receptor antagonist. 5-BDBD inhibits rP2X4R-mediated currents with an IC50 of 0.75 μみゅーM. 5-BDBD completely blocked the basal and acute hyperalgesia induced by NTG.

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2 3 heterotrimeric receptors.

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

Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μみゅーM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μみゅーM).

NP-1815-PX is a selective P2X4R antagonist with demonstrated anti-inflammatory effects and the capability to alleviate pain in chronic pain models. Additionally, it impedes contractions of guinea pig tracheal and bronchial smooth muscle (TSM and BSM)[1][2][3].

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.

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