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A novel amidophosphonate analog of Platelet Activating Factor (PAF), trimethyl (3-phosphonopropyl) ammonium hydroxide (R)-mono[2-acetamido-3-(hexadecyloxy)propyl] ester (PAF-AP), was synthesized. A potent inhibitor of aggregation induced by Platelet Activating Factor, arachidonic acid, Ca2+-ionophore, ADP, and thrombin, PAF-AP had no or very little effect on aggregation induced by epinephrine and collagen. Inhibition of phospholipase A2 and C2 activity was suggested from suppression of release of [14C]-arachidonic acid from pre-labeled platelet glycerophospholipids.
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