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The Effect Of A Novel Glycoprotein Iib/Iiia Antagonist, Sr 121566a, On Platelet Aggregation And Activation In Rhesus Monkeys., Mark Santillan, J. Herring, D. Hoppensteadt, W. Jeske, J. Herbert, J. Fareed
The Effect Of A Novel Glycoprotein Iib/Iiia Antagonist, Sr 121566a, On Platelet Aggregation And Activation In Rhesus Monkeys., Mark Santillan, J. Herring, D. Hoppensteadt, W. Jeske, J. Herbert, J. Fareed
Mark K. Santillan
SR 121566A represents a peptidomimetic glycoprotein IIb/IIIa (GP IIb/IIIa) inhibitor 3-[N- 4-[4-(aminoiminomethyl)phenyl]-1,3-thiazol-2-yl ) -N-(1-carboxymethylpiperid-4-yl) amino] propionic acid, trihydrochloride. To investigate the intravenous and subcutaneous pharmacodynamics of this agent, a primate model ( Macaca mulatta) was used. The IC50 for adenosine diphosphate (ADP) (10 micromol/L)-induced platelet aggregation in this primate platelet system was found to be 45 +/- 6 nmol/L. Comparatively in the human platelet rich plasma system, SR 121566A demonstrated an IC50 of 39 +/- 4 nmol/L. Graded doses of SR 121566A in the range of 25-400 microg/kg were administered intravenously. Blood samples were drawn from individual groups of primates …