Synthesis of novel bifunctional chelators and their use in preparing

David A. Westerberg, Patrick L. Carney, Patrick E. Rogers, Steven J. Kline, and David K. Johnson. J. Med. Chem. .... Min Li and Paul R. Selvin. Biocon...
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J . Med. Chem. 1989,32, 236-243

Table XIII. Percent Inhibition of ADP-Induced Platelet Aggregation Data for Compounds 1 and 58 % inhibn expt concn of compda PGEl 1 1 32 94 82 10 56 38 26 3.2 29 1.0 2 32 90 10 85 28 1 3.2 62 27 1.0 72 3 32 37 10 14 3.2 1.0 OThe concentration of PGE, is in ng/mL; the concentration and 58 is in fig, mL.

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Ex Vivo Studies. Compounds were dissolved in Emulphor/ethanol/Tyrodes and were administered gastrically to rats and guinea pigs via gavage. A t 2 h after drug or placebo administration, blood samples were drawn from all animals as described previously. P R P was prepared and aggregation experiments were conducted as previously described. Activity was determined by demonstration of a p value of