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Description: RO-3 is potent, selective, orally active and brain penetrant antagonist of homomeric P2X3 and heteromeric P2X2/3 receptor with pIC50 values are 7.0 and 5.9 respectively. It exhibits no activity at P2X1, P2X2, P2X4, P2X5 and P2X7 receptors (IC50 > 10 uM). It attenuates nociceptive sensitivity in animal models of pain. Evidence from a variety of experimental strategies, including genetic disruption studies and the development of selective antagonists, has indicated that the activation of P2X receptor subtypes, including P2X(3), P2X(2/3), P2X(4) and P2X(7), and P2Y (e.g., P2Y(2)) receptors, can modulate pain
References: Br J Pharmacol. 2006 Feb; 147 Suppl 2:S132-43; J Pharmacol Exp Ther. 2008 Feb; 324(2):409-15.
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