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Vol. 58, Issue 1, 82-88, July 2000
Institute of Molecular Physiology, University of Sheffield,
Sheffield, England
There are few antagonists selective for subtypes of the several P2X
receptors, but these are needed to identify the receptors expressed on
native cells and tissues. In particular, P2X4 and P2X7 receptor subunits are colocalized on immune,
epithelial, and exocrine gland cells, but both are relatively
insensitive to suramin and
pyridoxal-5-phosphate-6-azo-2',4'-disulfonic acid derivative. In
this article, we show that Coomassie Brilliant Blue G selectively
inhibits P2X7 receptors with nanomolar affinity. We
measured currents in response to P2X receptor activation in HEK293
cells heterologously expressing human or rat P2X1,
P2X2, P2X3, P2X2/3,
P2X4, P2X1/5, and P2X7 receptors.
Brilliant Blue G produced a noncompetitive inhibition of rat and human
P2X7 receptors with IC50 values of 10 and 200 nM, respectively. IC50 values for inhibition of the other
receptors ranged from 2 to >30 µM; the rat and human
P2X4 receptors showed IC50 values of
>10 and 3.2 µM. Coomassie Blue G also blocked YO-PRO1 uptake and
membrane blebbing, which are uniquely associated with activation of
P2X7 receptors. Thus, Brilliant Blue G is at least
1000-fold more potent at rat P2X7 receptors than at rat
P2X4 receptors.
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