p2xrs

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.

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

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.

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

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).

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

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.

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 .

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.

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

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

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 μM. BX430 has species specificity.

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

PSB-12062 (N-(p-Methylphenylsulfonyl)phenoxazine) is a potent and selective antagonist of P2X4(IC50 of 1.38 μM 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 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).

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.

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.

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 μM, respectively. It shows antagonistic activity on rP2X3 (IC50=0.87 μM). It is development as an injectable agent for the treatment of postoperative pain.

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

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

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