GSK1482160

GSK1482160 is an orally available small molecule that acts as a potent, selective negative allosteric modulator (antagonist) of the purinergic P2X7 receptor. The P2X7 receptor is an ATP-gated cation channel highly expressed on immune cells such as microglia, macrophages, and monocytes. Activation of this receptor leads to the production and release of pro-inflammatory cytokines like IL-1β and plays a key role in neuroinflammation and inflammatory pain. GSK1482160 was developed by GSK (formerly GlaxoSmithKline) for potential use in treating inflammatory pain and neuroinflammatory conditions. It has demonstrated efficacy in preclinical models of chronic joint pain and neuropathic pain, with desirable pharmacokinetic properties including high blood–brain barrier penetration. Additionally, radiolabeled forms ([^11C]GSK1482160 or [^18F]GSK1482160) have been used as PET tracers for imaging neuroinflammation via targeting P2X7R in animal models of Alzheimer’s disease and tauopathies[1][2][3][5][6][7].