A438079

A438079 is a potent and selective **competitive antagonist of the P2X7 receptor**, a subtype of purinergic (P2X) ligand-gated ion channels[2][4][5][17][22]. It displays high selectivity for P2X7 over other P2 receptor subtypes (IC50 > 10 μM for others)[2][5][21][22]. In preclinical studies, A438079 exhibits activity in several models: it has demonstrated **antagonism of ATP-induced inflammation**, antinociceptive (pain-reducing) effects in neuropathic pain models, neuroprotective activity in models of seizures and neuronal injury, and modulation of inflammasome activation[1][3][9][15][19]. The mechanism of action is blockade of the P2X7 receptor, which inhibits downstream events such as calcium influx, inflammasome assembly, cytokine release (e.g., IL-1β), and cell death[1][3][9][15]. In various in vivo and in vitro studies, it has been shown to attenuate liver and neuronal injury, reduce inflammatory responses, and protect against tissue damage induced by drugs (e.g., acetaminophen) or lipopolysaccharide (LPS)[1][3][12][15]. A438079 was initially developed by Abbott Laboratories[16].

Other names

A438079 hydrochlorideA-438079 hydrochlorideA 438079 hydrochloride3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride