p2x4

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

CTP disodium dihydrate is an agonist of P2X4 purinergic 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.

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

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.

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.

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.

P2X4-IN-1 is an orally bioavailable P2X4 receptor antagonist. P2X4-IN-1 has potential application value in disease intervention research.

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].

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.

BzATP triethylammonium salt is a P2X7 receptor agonist.

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.

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.

MSK-9 is an allosteric modulator of the P2X4 receptor, exhibiting dual actions of enhancing ion conductivity and delaying receptor desensitization. By stabilizing the receptor's open state, MSK-9 utilizes rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 is applicable in research related to multiple sclerosis (MS).

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.

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.

PSB-12054 is a potent P2X4 receptor inhibitor. PSB-12054 has IC(50) of 0.189 μM and good selectivity versus the other human P2X receptor subtypes.

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.

MRS4596, a potent and selective antagonist of the P2X4 receptor, exhibits an IC50 of 1.38 μM for the human P2X4 receptor. This compound demonstrates both neuroprotective and neuro-rehabilitative effects in ischemic stroke models, making it valuable for research purposes in the context of ischemic stroke.

MRS4719, a potent P2X4 receptor antagonist, exhibits a half-maximal inhibitory concentration (IC50) of 0.503 μM for the human P2X4 receptor. Demonstrating both neuroprotective and neuro-rehabilitative effects, it can decrease infarct volume and brain atrophy in an ischemic stroke model. Additionally, MRS4719 mitigates ATP-induced calcium influx in primary human monocyte-derived macrophages, making it a valuable tool for researching ischemic stroke.

TNP-ATP, a derivative of ATP, acts as an antagonist to the purinergic P2Y1, P2X3, and P2X2/3 receptors, demonstrating selectivity by showing lower inhibitory concentrations (IC50 = 6, 0.9, 7 nM, respectively) compared to the P2X2, P2X4, and P2X7 receptors (IC50 = 2, 15.2, >30 µM, respectively) in HEK293 cells expressing these human receptors. It effectively diminishes acetic acid-induced calcium influx in 1321N1 cells targeting P2X3 and P2X2/3 receptors (IC50 = 100 and 62 nM, respectively) and alleviates pain in a mouse model of visceral pain (ED50 = 6.35 µmol/kg). Moreover, TNP-ATP exhibits a notable fluorescence characteristic, with an emission peak at 547 nm after excitation at 403 nm, which enhances four-fold and shifts to 538 nm when bound to the insulin-degrading enzyme (IDE).

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.