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A-740003 is a selective and competitive antagonist of P2X7 receptor with IC50 values of 40 nM and 18 nM in human and rat, respectively [1].

P2X7 receptors are members of ATP-sensitive ionotropic P2X receptor family (P2X1–P2X7). P2X7 receptors can trigger various responses such as activation of caspases, cytokine release, membrane permeabilization, apoptosis and cell proliferation, in immunologically genetic cells [1].

Activated P2X7 receptors rapidly change intracellular calcium concentrations, the release of interleukin-1β (IL-1β), and cytolytic plasma membrane pore formation. In human THP-1 cells with a macrophage phenotype that P2X7 receptors were expressed, IL-1β release and pore formation were resulted from the activation of P2X7 receptors. A-740003 potently inhibited pore formation (measured by Yo-Pro uptake) with an IC50 value of 92 nM and blocked the release of IL-1β with an IC50 value of 156 nM [1].

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