Abstract
The novel RGDF mimetics were synthesized with the use of 4-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-4-oxobutyric or 5-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-5-oxopentanoic acids as a surrogate of Arg-Gly motif. The synthesized compounds have demonstrated a high potency to inhibit platelet aggregation in vitro and to block FITC-Fg binding to alpha(IIb)beta(3) on washed human platelets.
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MeSH terms
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Fibrinogen / chemistry
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Fluorescein-5-isothiocyanate / chemistry
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Humans
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Oligopeptides / chemistry
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Platelet Aggregation / drug effects
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Platelet Aggregation Inhibitors / chemical synthesis*
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Platelet Aggregation Inhibitors / chemistry
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Platelet Aggregation Inhibitors / pharmacology
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Platelet Glycoprotein GPIIb-IIIa Complex / antagonists & inhibitors*
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Platelet Glycoprotein GPIIb-IIIa Complex / metabolism
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Protein Binding
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Tetrahydroisoquinolines / chemical synthesis
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Tetrahydroisoquinolines / chemistry*
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Tetrahydroisoquinolines / pharmacology
Substances
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Oligopeptides
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Platelet Aggregation Inhibitors
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Platelet Glycoprotein GPIIb-IIIa Complex
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Tetrahydroisoquinolines
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arginyl-glycyl-aspartyl-phenylalanine
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1,2,3,4-tetrahydroisoquinoline
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Fibrinogen
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Fluorescein-5-isothiocyanate