allosteric antagonist (IC50
= 0.54 μ
M). Exhibits >10-fold selectivity for human P2X4
receptors over P2X1
receptors. Binds noncompetitively at extracellular allosteric site. Effective at human and zebrafish, but not mouse and rat P2X4
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Identification and characterization of a selective allosteric antagonist of human P2X4 receptor channels
Ase et al.