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P2X receptor antagonists and modulators act on ion channels gated by extracellular adenosine triphosphate (ATP). Cloning of the P2X1 and P2X2 subunits in 1994 defined a new structural class of ligand-gated ion channels. Seven subunits, P2X1 to P2X7, assemble as trimers that pass sodium, potassium and calcium ions. P2X3 and P2X2/3 receptors on sensory neurons are studied in pain signaling, and P2X7 receptors in inflammation. In 1996 the cytolytic P2Z receptor of macrophages was identified as P2X7, which opens large pores during sustained ATP exposure. A-317491 sodium salt hydrate and AF-353 block P2X3 and P2X2/3 receptors. A 740003 and A 438079 hydrochloride are P2X7 antagonists, whereas NF 279 acts at P2X1.
