Leila Hassanzadeh, M. Erfani, S. Ebrahimi
Aug 1, 2012
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0
Influential Citations
5
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
To develop a novel 5HT1A receptor imaging agent, a new methoxyphenyl piperazine derivative was synthesized and radiolabeled with 99mTc-tricarbonyl precursor. We used the Cu (I)-catalyzed cycloaddition of azide and terminal alkynes to synthesize 1, 2, 3 triazole as the metal chelating system. This synthesis provided reliable and reproducible method to attach technetium to the methoxyphenyl piperazine moiety. 99mTc-tricabonyl labeling of ligand was performed at high radiochemical purity (greater than 95%). The radiolabeled compound was stable at least 24 h in room temperature. In vitro stability study in human serum albumin showed more than 90% stability in 37 °C incubation for 6 h. Biodistribution studies in rat have shown brain hippocampus uptake of 0.31 ± 0.02 %ID/g at 5-min post-injection. The favorable in vitro/in vivo stability, lipophilicity, and biodistribution profiles suggest that this radioconjugate is a good candidate for further exploration of its potential clinical application. Copyright © 2012 John Wiley & Sons, Ltd.