AZ10606120 dihydrochloride

AZ-10606120 is a potent purinoceptor P2X7 negative allosteric modulator that antagonizes ATP-dependent P2X7 activation (IC50 against ATP-induced ethidium bromide uptake = 2.3 nM and 24 nM, respectively, using human or rat P2X7 HEK293 transfectants; [ATP] = EC50) in a non-competitive and slowly reversible manner via affinity interaction at an allosteric pocket (human/rat P2X7 KD = 1.4 nM/19 nM) distinct from the KN-62- or ATP-binding site. A useful tool for probing P2X7-mediated physiological and pathological processes both in cultures (0.1-10 µM) and in vivo (e.g. 5 mg/kg i.p., 300 nM i.m., or 3 µg i.c.v.; in mice).