A subtype-selective, competitive and reversible P2X 1 receptor antagonist. Displays IC 50 values of 0.21, 28.9, > 50 and > 100 μ M for human P2X 1 , P2X 3 , P2X 2 , and P2X 4 -mediated responses respectively. Selective over adrenoceptors, histamine and P2Y receptors. Also selectively inhibits the α -subunit of G o/i (EC 50 ~? 300 nM).
NF 023 contains six benzene rings and is a suramin analog. It is a potent, competitive, and selective P2X purinoceptor antagonist that aids in discriminating between P2X receptor subtypes.
