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Monovalent and Bivalent Fibrin‐specific MRI Contrast Agents for Detection of Thrombus
Author(s) -
Nair Shrikumar A.,
Kolodziej Andrew F.,
Bhole Gandhali,
Greenfield Matthew T.,
McMurry Thomas J.,
Caravan Peter
Publication year - 2008
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200800563
Subject(s) - bivalent (engine) , gadolinium , thrombus , fibrin , chemistry , in vivo , peptide , combinatorial chemistry , radiology , medicine , biochemistry , organic chemistry , metal , biology , microbiology and biotechnology , immunology
Probing in contrast : Four gadolinium‐DTPA moieties (DTPA=diethylenetriaminepentaacetic acid) and two fibrin‐specific cyclic peptides are linked by a compact triethylenetetraamine core (see scheme) to create a highly sensitive probe for molecular MR imaging of thrombosis. The contrast agent has a high molecular relaxivity, and the dual peptide construct provides five‐fold higher fibrin affinity than the monovalent analogue. This bivalent probe showed significant specific thrombus uptake in an in vivo model of thrombosis.