A-839977

A-839977 is a potent antagonist of the purinergic receptor P2X subtype 7 (P2X7). A-839977 potently blocks BzATP-induced calcium influx at recombinant human, rat and mouse P2X7 receptors with IC₅₀ values of 20 nM, 42 nM and 150 nM respectively. It also potently blocks agonist-induced YO-PRO uptake and IL-1β release from differentiated human THP-1 cells. It shows antihyperalgesic and antinociceptive effects in animal models of inflammatory pain.