Imaging of deep venous thrombosis using radioactive-labeled tirofiban

Darkovska-Serafimovska, Marija and Janevik-Ivanovska, Emilija and Ugresic, Nenad and Djorgoski, Icko (2015) Imaging of deep venous thrombosis using radioactive-labeled tirofiban. Bratislava Medical Journal / Bratisl Lek Listy 2012, 116 (10). pp. 621-626. ISSN 1336- 0345

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The development of radiolabeled small peptide or peptidomimetic ligands can bind platelets and their specific expressed receptor have been suggested as a new approach to detect the clot location and, more essentially, to determine the age and morphology of the evolving thrombus. This new approach is focused on the use of a series of radiolabeled platelet GPIIb/IIIa receptor antagonists.
Tirofi ban N-(butylsulfonyl)- 4-O-(4-(4-piperidyl)-L-tyrosine is a non-peptide tyrosine derivate. The aim of the study was to introduce radioactive-labeled tirofi ban as a specifi c imaging agent for acute DVT.
The labeling was performed with technetium-99 in the presence of a stannous reducing agent. The labeled
preparation showed fast blood clearance in a normal rat model (without induced thrombosis). More than 80 %
of the injected dose was eliminated from the circulation in the fi rst hour after injection. Biodistribution and visualization of the labeled molecule was carried out using an experimental model of thrombosis in a male Wistar
rat. Planar images were obtained 30 and 60 min after application of 2 × 106 imp/min 99m-technetium-tirofi ban
in the rat’s tail vein. Sensitivity and specifi city were determined using the ratio of ‘left leg positive for DVT’ to ‘right leg negative for DVT’. The obtained ratio was 1.54 after 30 min and 5.04 after 60 min. These values were
considered positive in the detection of acute DVT. The high DVT uptake shows that radiolabeled tirofi ban in
the introduced rat model can be a promising agent for imaging the deep venous thrombosis.

Item Type: Article
Subjects: Medical and Health Sciences > Basic medicine
Divisions: Faculty of Medical Science
Depositing User: Emilija Janevik
Date Deposited: 11 Feb 2016 09:55
Last Modified: 11 Feb 2016 09:55

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