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Synthesis, radio-LC–MS analysis and biodistribution in mice of 99mTc–NIM–BAT

✍ Scribed by G. Bormans; B. Cleynhens; T.J. de Groot; L. Mortelmans; J.-L. Moretti; A. Verbruggen


Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
172 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

S,S′‐bis‐trityl‐N‐BOC‐1,2‐ethylenedicysteamine (S,S′‐bis‐trityl‐N‐BOC–BAT) was conjugated to 2‐nitroimidazole (NIM) through a propylene spacer in order to provide a precursor for a potential technetium‐99 m labelled hypoxia tracer. For labelling with technetium‐99 m, a two‐step one‐pot procedure was developed consisting of deprotection of the ligand by heating in mild acidic conditions and subsequent exchange labelling in the presence of SnCl~2~, tartrate and ^99m^TcO.

The labelling reaction mixture was analyzed using electrospray radio‐LC–MS and the observed mass spectrum corresponding to the main radiometric peak was in accordance with the predicted structure of oxo–Tc(V)–NIM–BAT.

^99m^Tc–NIM–BAT was purified using RP–HPLC and its biodistribution was evaluated in normal mice at 10 min and 4 h p.i. ^99m^Tc–NIM–BAT was cleared from plasma mainly by hepatobiliary excretion. Copyright © 2003 John Wiley & Sons, Ltd.


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