p2x1

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.

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.

BzATP triethylammonium salt is a P2X7 receptor agonist.

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.

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.

PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na Ca²⁺ exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.

P2X1 receptor potentiator

P2X1 receptor antagonist

P2X1 purinergic receptor antagonist

NF864, a suramin analog, is a P2X1 receptor inhibitor.

MRS2220 is a selective enhancer of the ATP effects at fast desensitizing P2X (P2X1 and P2X3) receptors.

α,β-Methylene ATP dilithium, a phosphonic analog of ATP, serves as a ligand for P2X3 and P2X7 receptors. It is a potent agonist specifically targeting P2X1 and P2X3 receptors while exerting negligible activity on P2X2, P2X4, P2X5, P2X6, and P2X7 receptors.

Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist and exhibits non-selective antagonism at both recombinant and human platelet P2X1 receptors.

Adenosine 5'-diphosphate sodium salt (ADP sodium salt) is an adenine nucleotide that is phosphorylated into ATP by ATPase. This phosphorylation is a key part of cellular homeostatis as it allows for energy storage and is involved in nucleic acid metabolism. ADP affects platelet activation through its interaction with ADP receptors P2Y1, P2Y12 and P2X1. Upon its conversion to adenosine by ecto-ADPases, platelet activation is inhibited via adenosine receptors.

MRS2179 tetrasodium hydrate, a competitive antagonist of the P2Y1 receptor, acts on the turkey P2Y1 receptor (Kb: 102 nM, pA2: 6.99) and exhibits an inhibitory effect on platelet aggregation. IC50: 1.15 μM), P2X3 (IC50: 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors.

NF 023 is a potent, selective P2X1 purinoceptor antagonist.

α,β-Methylene ATP, a phosphonic analog of ATP, functions as a ligand for P2X3 and P2X7 receptors, and acts primarily as a selective agonist for P2X1 and P2X3 receptors, exhibiting minimal to no activity on P2X2, P2X4 through P2X7 receptors.

Blue FPG-A trisodium, a structural isomer of Reactive Blue 2 (RB2) components [1], serves as a selective antagonist for both P2X1 and P2Y1 receptors, boasting IC50 values of 35.5 μM and 2.6 μM, respectively.

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.

PPADS is a P2 receptor antagonist with IC50 values of 68 nM (P2X1) and 214 nM (P2X3). This compound functions as an ATP (nucleotide) analog, competing for binding sites on the P2 receptors with ATP. Additionally, PPADS acts as a reversible competitive antagonist of the NAADP receptor. It is capable of reversing hyperalgesia, and it diminishes the enhanced NO NOS signaling and IL-1β production in both peripheral and central steps of the nervous system.

Uridine adenosine tetraphosphate (UP4A) acts primarily as an endothelium-derived vasoconstrictor, exerting its effects mainly through the P2X1 receptor, and potentially through the P2Y2 and P2Y4 receptors as well. It is utilized in research related to cardiovascular diseases.

NF023 hexasodium is a selective and competitive P2X1 receptor antagonist with IC50 values of 0.21 μM, 28.9 μM, > 50 μM, and > 100 μM for human [P2X1], [P2X3], [P2X2], and [P2X4]-mediated responses, respectively.

P2X1 antagonist