Cloned and transfected P2Y4 receptors: characterization of a suramin and PPADS-insensitive response to UTP.
The P2Y family of receptors are G protein-coupled receptors for ATP, ADP, UTP and UDP. Recently several members of this family have been cloned, including the P2Y4, which is activated by UTP but not by ATP. In the present report, using receptors stably transfected into 1321N1 cells, we show that suramin acts as an antagonist at cloned P2Y1 and (less potently) P2Y2 receptors, but not at the cloned P2Y4 receptor. Furthermore, PPADS (pyridoxal-phosphate-6-azophenyl-2',4'-disulphonic acid), a potent antagonist at the P2Y1 receptor, is a relatively inneffective antagonist at the cloned P2Y4 receptor. This work moves us closer to the goal of classifying the native P2Y receptors on the basis of agonist and antagonist profiles.
Charlton
S J
SJ
Department of Cell Physiology and Pharmacology, University of Leicester.
Brown
C A
CA
Weisman
G A
GA
Turner
J T
JT
Erb
L
L
Boarder
M R
MR
D002460:Cell Line; D003001:Cloning, Molecular; D006801:Humans; D058919:Purinergic P2 Receptor Antagonists; D011732:Pyridoxal Phosphate / Q000031:analogs & derivatives* / Q000494:pharmacology; D018048:Receptors, Purinergic P2 / Q000235:genetics*; D013498:Suramin / Q000494:pharmacology*; D014162:Transfection; D014544:Uridine Triphosphate / Q000494:pharmacology*
D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; C104749:purinoceptor P2Y4; C077792:pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid; D011732:Pyridoxal Phosphate; D013498:Suramin; D014544:Uridine Triphosphate