Uses
AR-C66096 tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism[1].
Biological Activity
the platelet p2t receptor plays a major role in platelet aggregation, and its antagonists are suggested to have significant therapeutic potential as antithrombotic agents. ar-c 66096 is a novel, potent and selective antagonist at human platelet p2t-purinoceptors.
in vitro
in suspensions of human washed platelets, ar-c 66096 (1-100 nm) produced concentrationdependent rightward displacement of concentration-effect (e/[a]) curves obtained for adp-induced platelet aggregation. the anti-aggregatory potency of ar-c 66096 was not influenced by increasing the incubation time from 2 to 15 min nor by inclusion of the p1-purinoceptor antagonist 8-sulphophenyltheophylline at a concentration (300 μm) [1].
in vivo
ar-c 66096 behaved as a weak (pa50 3.68) but full p2x-purinoceptor agonist in preparations of the isolated rabbit ear artery and as a weak, competitive antagonist (apparent pkb 4.71) at p2y-purinoceptors in the isolated guinea-pig aorta, indicating a selectivity of at least 9000 fold for the pzrsubtype. in the latter preparation, non-specific relaxations were observed by concentrations of ar-c 66096 >10 μm [1].
References
[1] humphries, r. g.; tomlinson, w.; ingall, a. h.; cage, p. a.; leff, p. fpl 66096: a novel, highly potent and selective antagonist at human platelet p2t-purinoceptors. br. j. pharmacol. 1994, 113, 1057-1063.
