A-804598

A-804598 is a potent, selective, and competitive antagonist of the P2X7 receptor, a purinergic receptor activated by high concentrations of extracellular ATP. A-804598 exhibits high affinity across species (IC50: 9 nM mouse, 10 nM rat, 11 nM human), effectively inhibiting P2X7-mediated responses, including agonist-stimulated release of the pro-inflammatory cytokine IL-1β and cellular pore formation[3][5][7]. It readily crosses the blood-brain barrier and has been extensively studied in preclinical models of neuroinflammation, depression, neuropathic pain, rheumatoid arthritis, and liver inflammation under settings of chronic ethanol and high-fat diet exposure[1][2][4]. Mechanistically, A-804598 blocks P2X7R activation on immune and glial cells, thereby reducing downstream pro-inflammatory signaling such as IL-1β, IL-6, TNFα, induction of NF-κB, and related neuroimmune responses[1][2][5]. It has demonstrated efficacy in decreasing neuroinflammatory markers, oxidative stress, and behavioral readouts in animal models, although it is not approved for human use. The compound is structurally novel among P2X7R antagonists and has been used experimentally as a high-affinity radioligand and tool compound in neuroscience and immunology research[5][7].

Other names

A-804598A804598A 804598