Decavanadate, a P2X receptor antagonist, and its use to study ligand interactions with P2X7 receptors.

2006 
Abstract In this study we have studied decavanadate effects at P2X receptors. Decavanadate competitively blocked 2′- and 3′- O -(4benzoylbenzoyl) ATP (BzATP) stimulated ethidium accumulation in HEK293 cells expressing human recombinant P2X 7 receptors (p K B 7.5). The effects of decavanadate were rapid (minutes) in both onset and offset and contrasted with the much slower kinetics of pyridoxal 5-phosphate (P5P), Coomassie brilliant blue (CBB) and 1-[ N , O -bis(5-isoquinolinesulfonyl)- N -methyl- l -tyrosyl]-4-phenylpiperazine (KN62). Decavanadate competitively blocked the slowly reversible, or irreversible, blockade of the P2X 7 receptor produced by P5P and oxidised ATP suggesting competition for a common binding site. However, the interaction between decavanadate and KN62 was non-competitive. Decavanadate also blocked P2X 2 and P2X 4 receptors but with slightly lower potency. These data demonstrate that decavanadate is the first reversible and competitive antagonist of the P2X 7 receptor and is a useful tool for studying the mechanism of interaction of ligands with the P2X 7 receptor.
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