99mTc-roxifiban: a potential molecular imaging agent for the detection and localization of acute venous thrombosis

99m Tc-roxifiban was obtained in a high radiochemical yield (98.4%) by complexing ~750 MBq 99m Tc with 2.5 mg roxifiban in the presence of 150 µg SnCl 2 ·2H 2 O. Factors affecting the labelling yield were investigated and optimized. The complex was lipophilic and stable in saline and serum for more...

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Bibliographic Details
Published in:Journal of radioanalytical and nuclear chemistry 2017, Vol.311 (3), p.1719-1728
Main Authors: El-Kawy, O. A., García-Horsman, J. A.
Format: Article
Language:English
Subjects:
Chemistry
Chemistry and Materials Science
Diagnostic Radiology
Hadrons
Heavy Ions
Imaging
In vitro methods and tests
In vivo methods and tests
Inorganic Chemistry
Molecular docking
Molecular structure
Nuclear Chemistry
Nuclear Physics
Physical Chemistry
Platelets
Radiochemistry
Rats
Technetium isotopes
Thrombosis
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Summary:99m Tc-roxifiban was obtained in a high radiochemical yield (98.4%) by complexing ~750 MBq 99m Tc with 2.5 mg roxifiban in the presence of 150 µg SnCl 2 ·2H 2 O. Factors affecting the labelling yield were investigated and optimized. The complex was lipophilic and stable in saline and serum for more than 8 h. The complex structure prediction and molecular docking to its target activated GPIIb/IIIa receptor were performed. The tracer in vitro binding to activated platelets was high (27–32%). In vivo evaluation was performed through clearance, biodistribution and imaging studies in rats. All results supported the usefulness of the tracer as thrombus imaging agent.
ISSN:0236-5731
1588-2780
DOI:10.1007/s10967-017-5183-4