Abstract
3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid, RGDS, RGDV, RGDF and their linkers were synthesized. The anti-aggregation and adhesion of platelet indicated that the in vitro activities of the linkers remained at the same level as RGDS, RGDV, and RGDF (p>0.05). The antithrombotic activities in vivo suggested, however, that the potencies of RGDS, RGDV and RGDF were enhanced by the introduction of 3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxyl group into their alpha amino group (p<0.05, 0.01 or 0.001).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Carbolines / administration & dosage
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Carbolines / chemical synthesis*
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Carbolines / pharmacology
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Cell Adhesion / drug effects
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Disease Models, Animal
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Fibrinolytic Agents / administration & dosage
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Fibrinolytic Agents / chemical synthesis*
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Fibrinolytic Agents / pharmacology
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Humans
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Male
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Oligopeptides / administration & dosage
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Oligopeptides / chemical synthesis*
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Oligopeptides / pharmacology
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Platelet Aggregation / drug effects
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Rabbits
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Rats
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Rats, Wistar
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Structure-Activity Relationship
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Thrombosis / drug therapy
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Tumor Cells, Cultured / drug effects
Substances
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Carbolines
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Fibrinolytic Agents
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Oligopeptides
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arginyl-glycyl-aspartic acid