A Useful Method for in situ Indirect Radiolabeling of Carbonyl-Containing Biomolecules

Abstract

[125I] 2-(2,3-diiodo-4-hydroxyphenyl)-1,3,4-oxadiazole was synthesized (48% yield) and acid-hydrolyzed in situ with direct derivatization with p-nitro benzaldehyde to obtain the required 125I hydrazone (89% yield). A blood clearance kinetic study was performed on the 125I oxadiazole in a Sprague-Dawley rat and a biphasic behaviour was obtained. This study shows that 125I oxadiazole has potential to be metabolically stable and enough to allow imaging and tracking for a minimum of 2 h, making it a viable option for in situ indirect labeling of carbonyl containing macromolecules and keto steroids.