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Overview
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Background
A 438079 hydrochloride is a selective antagonist of P2X7 receptor with IC50 values of 100 and 300 nM in rat and human, respectively [1].
A 438079 is a derivative of the origin compound tetrazole 5 selected out as a novel P2X7 receptor antagonist. In human 1321N1 astrocytoma cells with expressing recombinant human P2X7, A 438079 treatment suppressed the Ca 2+ flux with pIC50 value of 6.9. In the pore formation assay, A 438079 blocked the pore formation of human THP-1 cells and prevented the cells from uptaking the diiodide dye YO-PRO. Moreover, in the spinal nerve ligation model, administration of A 438079 reduced the neuropathic pain induced by the application of a von Frey hair. The ED50 value was 76 μM/kg [2].1. Nelson D W, Gregg R J, Kort M E, et al. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. Journal of medicinal chemistry, 2006, 49(12): 3659-3666.
2. Donnelly-Roberts D L, Jarvis M F. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. British journal of pharmacology, 2007, 151(5): 571-579.
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