## Abstract A ^99m^Tc‐labelled compound with the biological characteristics of flumazenil would be useful for determination of neuronal viability after the onset of a stroke. Therefore, we have derivatized Ro‐15‐3890 (a flumazenil metabolite bearing a carboxylic acid group instead of an ethyl ester
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
- DOI
- 10.1002/jlcr.698
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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.
📜 SIMILAR VOLUMES
## Abstract The bis(__N__‐cyclopentyl dithiocarbamato) nitrido technetium‐99m complex ^99m^TcN(CPEDTC)~2~ was synthesized by the reduction of ^99m^TcO into [^99m^Tc≡N]^2+^ with stannous chloride in the presence of succinic dihydrazide and propylenediamine tetraacetic acid, followed by the addition