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Vol. 53, Issue 4, 727-733, April 1998
Institut National de la Santé et de la Recherche
Médicale U311 (B.H., C.L., C.G.), Etablissment de Transfusion
Sanguine de Strasbourg, BP 36, 67065 Strasbourg Cédex, France,
Institut de Pharmacologie Moléculaire et Cellulaire (P.V., C.F.),
Centre National de la Recherche Scientifique UPR 411, 06560 Valbonne,
France, and
Institut National de la Santé et de la Recherche
Médicale U343 (J.-P.B.), Hôpital de l'Archet, BP 79, 06202 Nice Cédex 3, France
Pharmacological properties of the human P2Y1 receptor
transfected in Jurkat cells and of the endogenous receptor in rat brain capillary endothelial cells were analyzed under conditions in which the
purity of adenine triphosphate nucleotides was controlled by creatine
phosphate/creatine phosphokinase (CP/CPK). ATP, a partial agonist of
the receptor, was inactive in the presence of CP/CPK. Results further
indicated that ATP was a competitive antagonist of ADP actions.
Ki values were 23.0 ± 1.5 µM in endothelial cells and 14.3 ± 0.3 µM in Jurkat cells. Solutions prepared from
commercially available 2-methylthio-ATP (2-MeSATP) or 2-chloro-ATP
(2-ClATP) contained 
10% of ADP derivatives. ADP derivatives were
removed from the solution by treatment with CP/CPK. Purified 2-MeSATP
and 2-ClATP antagonized platelet aggregation induced by ADP. They did
not activate P2Y1 receptors but prevented ADP actions in a
competitive manner. Ki values for
2-MeSATP were 36.5 µM in endothelial cells and
5.7 ± 0.4 µM in Jurkat cells, and
Ki values for 2-ClATP were 27.5 µM in endothelial cells and 2.3 ± 0.3 µM in Jurkat cells. EDTA potentiated actions of ADP
and ATP on endothelial cells by 2.4- and 3.6-fold, respectively. In
conclusion, the rat and human P2Y1 receptors are
ADP-specific receptors that recognize ADP and 2-methylthio-ADP, whereas
ATP, 2-MeSATP, and 2-ClATP are competitive antagonists. The results further point to the close pharmacological similarity of the
P2Y1 receptor and the platelet ADP receptor.
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