Recent cloning of the human P2X(1) receptor revealed high levels of it
s messenger RNA in differentiated promyelocytes (HL60 cells), We found
expression of P2X(1) receptor protein in HL60 cells by radioligand bi
nding, by immunohistochemistry, using a receptor specific antibody, an
d by electrophysiology, The currents elicited by adenosine triphosphat
e (ATP) had the expected properties of P2X(1) receptors (rapid desensi
tization, mimicked by alpha,beta-methylene-ATP). However, these curren
ts were only observed in cells that were pretreated with apyrase, whic
h destroys extracellular ATP, or with suramin, a P2X receptor antagoni
st, This implies that HL60 cells release ATP, which chronically desens
itizes the receptor, ATP release was detected by direct measurement, u
sing the luciferin-luciferase assay. It is concluded that functional P
2X(1) receptors are present in the membrane of differentiated HL60 cel
ls. (C) 1996 by The American Society of Hematology.