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Vol. 56, Issue 4, 720-727, October 1999
Department of Pharmacological and Physiological Sciences, St. Louis
University School of Medicine, St. Louis, Missouri
We recently reported that a novel hetero-oligomeric P2X receptor is
formed from the P2X1 and P2X5 isoforms when
coexpressed in human embryonic kidney 293 cells (Torres et al., 1998).
A more complete description of the pharmacology of this novel receptor is presented here. A brief application of ATP to a voltage-clamped cell
transiently expressing P2X1/5 receptors resulted in a
biphasic current that rapidly reached a peak and then decayed to a
sustained plateau. Washout of ATP was accompanied by generation and
fade of a pronounced tail of inward current. EC50 values
were determined from concentration-response curves for a range of
agonists. The rank order of agonist potency was ATP 
2 methylthio ATP > adenosine 5'-O-(3-thiotriphosphate) > 
,
-methylene ATP > ADP > CTP.
,-methylene ADP, UTP, GTP, and AMP were
ineffective. Only ATP and 2 methylthio ATP were full agonists.
IC50 values were determined from concentration-response curves for three commonly used purinergic antagonists. Suramin and
pyridoxal phosphate-6-azophenyl-2', 4'-disulfonic acid
were equipotent at P2X1 and P2X1/5 receptors;
however, the P2X1/5 receptor was much less sensitive to
TNP-ATP than was the P2X1 receptor. The amplitude of peak
ATP-gated current was relatively insensitive to changes in
[Ca2+]O (1-30 mM). Finally, plateau currents
were potentiated by low concentrations of pyridoxal
phosphate-6-azophenyl-2', 4'-disulfonic acid and by
raising [Ca2+]O. These results provide
additional information on the pharmacological profile of the
recombinant P2X1/5 receptor channel and provide a basis to
further evaluate ATP-induced currents in native tissues.
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