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Characterization of P2x1 purinoreceptors on rat platelets: effect of clopidogrel by Pierre Savi; Josette Bornia; Veronique Salel; Marianne Delfaud; Jean‐Marc Herbert is a Medicine article available to read on EtoBox.

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This study aimed to determine the binding characteristics of [^3^H]α,β‐Me‐ATP, a specific ligand of the P2x1 receptors to rat platelets, and to investigate the effect of clopidogrel, a thienopyridine compound which has been found to selectively inhibit ADP‐induced platelet aggregation and adenylyl cyclase __ex vivo__. Binding of [^3^H]α,β‐Me‐ATP to rat platelets was time‐dependent and saturable. Scatchard analysis of the saturation binding data indicated that [^3^H]α,β‐Me‐ATP bound to one population of specific binding sites with high affinity (__K__~D~ = 23.6 ± 1.6 nm; __B__~max~ = 690 ± 24 fmole/10^8^cells) (__n=__3). Unlabelled α,β‐Me‐ATP as well as 2‐MeS‐ADP and ADP competitively inhibited the specific binding of [^3^H]α,β‐Me‐ATP with IC~50~ values of 19.0 ± 6.6, 103 ± 20 and 1120 ± 80 nm respectively (__n=__3). Other nucleotide analogues such as ATP, ATP‐γS, UTP and GTP also antagonized [^3^H]α,β‐Me‐ATP binding. When administered orally (10 mg/kg, p.o.), clopidogrel inhibited ADP‐ or 2‐MeS‐ADP‐induced platelet aggregation but did not affect the binding of [^3^H]α,β‐Me‐ATP to rat platelets __ex vivo. In vitro__, α,β‐Me‐ATP did not induce the aggregation or shape change of rat

Who reads Characterization of P2x1 purinoreceptors on rat platelets: effect of clopidogrel?

Author

Pierre Savi; Josette Bornia; Veronique Salel; Marianne Delfaud; Jean‐Marc Herbert

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley (ISSN 0007-1048)

Published

1997

Language

EN

Field

Medicine (Health Sciences)