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

摘要

Tc-99m-roxifiban was obtained in a high radiochemical yield (98.4%) by complexing similar to 750 MBq Tc-99m with 2.5 mg roxifiban in the presence of 150 mu g SnCl2 center dot 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.