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  • Title: Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.
    Author: Askew BC, Bednar RA, Bednar B, Claremon DA, Cook JJ, McIntyre CJ, Hunt CA, Gould RJ, Lynch RJ, Lynch JJ, Gaul SL, Stranieri MT, Sitko GR, Holahan MA, Glass JD, Hamill T, Gorham LM, Prueksaritanont T, Baldwin JJ, Hartman GD.
    Journal: J Med Chem; 1997 Jun 06; 40(12):1779-88. PubMed ID: 9191954.
    Abstract:
    The synthesis and pharmacological evaluation of 5 (L-738, 167), a potent, selective non-peptide fibrinogen receptor antagonist is reported. Compound 5 inhibited the aggregation of human gel-filtered platelets with an IC50 value of 8 nM and was found to be > 33000-fold less effective at inhibiting the attachment of human endothelial cells to fibrinogen, fibronectin, and vitronectin than it was at inhibiting platelet aggregation. Ex vivo platelet aggregation was inhibited by > 85% 24 h after the oral administration of 5 to dogs at 100 micrograms/kg. The extended pharmacodynamic profile exhibited by 5 appears to be a consequence of its high-affinity binding to GPIIb/IIIa on circulating platelets and suggests that 5 is suitable for once-a-day dosing.
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