Effects of lysine-naphthalene sulfonamide derivatives on the thrombin induced human platelet aggregation and the release reaction

Abstract

Lysine-naphthalene-sulfonamide derivatives activated TAME (tosyl-L-arginine methyl ester) esterase activity of thrombin. These compounds stimulated also thrombin-induced aggregation, ATP release and serotonin secretion from human platelet. On the other hand, analogues of these compounds which contain arginine residue in stead of lysine residue inhibited not only TAME esterase of thrombin but also thrombin-induced platelet aggregation. Lysine-naphthalene-sulfonamide and arginine-naphthalene-sulfonamide were the opposite actions each other against thrombin. The structure and activity relationship in these naphthalene-sulfonamide suggest that lysine and arginin residues play a very important role in the function of thrombin.