Semin Thromb Hemost 2005; 31(2): 162-167
DOI: 10.1055/s-2005-869521
Copyright © 2005 by Thieme Medical Publishers, Inc., 333 Seventh Avenue, New York, NY 10001, USA. Tel: +1(212) 584-4662.

The Platelet P2 Receptors in Thrombosis

Christian Gachet1 , 2 , Béatrice Hechler2
  • 1Researcher, Etablissement Français du Sang-Alsace, Strasbourg Cedex, France
  • 2INSERM U.311, Etablissement Français du Sang-Alsace, Strasbourg Cedex, France
Further Information

Publication History

Publication Date:
26 April 2005 (online)

ABSTRACT

Adenosine diphosphate (ADP) and adenosine triphosphate (ATP) play a crucial role in hemostasis and thrombosis, and their receptors are potential targets for antithrombotic drugs. The ATP-gated channel P2X1 and the two G protein-coupled P2Y1 and P2Y12 ADP receptors selectively contribute to platelet aggregation. Because of its central role in the formation and stabilization of a thrombus, the P2Y12 receptor is a well-established target of antithrombotic drugs such as clopidogrel, which has proven efficacy in many clinical trials and experimental models of thrombosis. Competitive P2Y12 antagonists have also been shown to be effective in experimental thrombosis as well as in several clinical trials. Studies in P2Y1 and P2X1 knockout mice and experimental thrombosis models using selective P2Y1 and P2X1 antagonists have shown that, depending on the conditions, these receptors could also be potential targets for new antithrombotic drugs. Because both P2X1 and P2Y1 receptor inhibition result in milder prolongation of the bleeding time as compared with P2Y12 inhibition, the idea is put forward that combinations of P2 receptor antagonists could improve efficacy with diminished hemorrhagic risk. However, further studies with stronger and more selective P2 receptor antagonists are required to validate such a point of view.

REFERENCES

 Dr.
Christian Gachet

INSERM U.311, Etablissement Francais du Sang-Alsace

10, Rue Spielmann, BP N° 36, 67065 Strasbourg Cedex, France

Email: christian.gachet@efs-alsace.fr

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