human p2x4

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.

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

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.

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.

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.

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.

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.

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.