GW791343 hydrochloride

GW791343 hydrochloride is a non-competitive human P2X (7) receptor inhibitor with pIC50 of about 7.1. GW791343 hydrochloride exhibits negative allosteric effects at the human P2X (7) receptor but is a positive allosteric modulator of the rat P2X (7) receptor. GW791343 hydrochloride competitively interacted at the ATP binding site and so were probably negative allosteric modulators of the P2X (7) receptor. GW791343 hydrochloride increased responses to BzATP at the F95L mutant receptor, although the magnitude of this effect was not as marked as at the rat ECD, rat–human or domain 1 receptor.