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Cloned and transfected P2Y 4 receptors: characterization of a suramin and PPADS‐insensitive response to UTP
Author(s) -
Charlton Steven J.,
Brown Colin A.,
Weisman Gary A.,
Turner John T.,
Erb Laurie,
Boarder Michael R.
Publication year - 1996
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1996.tb16038.x
Subject(s) - ppads , suramin , p2y receptor , p2 receptor , receptor , agonist , antagonist , g protein coupled receptor , biology , receptor antagonist , transfection , competitive antagonist , microbiology and biotechnology , biochemistry , gene
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 P2Y 4 , 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 P2Y 1 and (less potently) P2Y 2 receptors, but not at the cloned P2Y 4 receptor. Furthermore, PPADS (pyridoxal‐phosphate‐6‐azophenyl‐2′,4′‐disulphonic acid), a potent antagonist at the P2Y 1 receptor, is a relatively inneffective antagonist at the cloned P2Y 4 receptor. This work moves us closer to the goal of classifying the native P2Y receptors on the basis of agonist and antagonist profiles.