Key result
Novel P2T receptor antagonists, such as compound 10l, potently inhibited ADP-induced platelet aggregation (IC50 0.4 nM) with minimal prolongation of bleeding time compared to GPIIb/IIIa antagonists.
Population
Human platelets (in vitro) and in vivo models
Comparison
Platelet P2T receptor antagonists vs GPIIb/IIIa antagonists
Design
Preclinical
Authors
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Supports P2T antagonists for potent antiplatelet activity with minimal bleeding prolongation; leaves open translation from animal models.
Novel P2T receptor antagonists potently inhibit platelet aggregation with significantly less prolongation of bleeding time compared to GPIIb/IIIa antagonists in preclinical models.
Ingall et al. (1999) studied Platelet aggregation. P2T receptor antagonists (compounds 10e and 10l) vs. GPIIb/IIIa antagonists was evaluated on ADP-induced aggregation of human platelets and bleeding time prolongation. Novel P2T receptor antagonists, such as compound 10l, potently inhibited ADP-induced platelet aggregation (IC50 0.4 nM) with minimal prolongation of bleeding time compared to GPIIb/IIIa antagonists.
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