Ester-modified (TcO)-Tc-99m[SN(R)S/S] mixed ligand complexes: synthesis and preliminary evaluation

Authors
Tsoukalas, C Pirmettis, I Patsis, G Papadopoulos, A Raptopoulou, CP Terzis, A Papadopoulos, M Chiotellis, E
Citation
C. Tsoukalas et al., Ester-modified (TcO)-Tc-99m[SN(R)S/S] mixed ligand complexes: synthesis and preliminary evaluation, NUCL MED BI, 28(8), 2001, pp. 975-982
Citations number
29
Categorie Soggetti
Medical Research Diagnosis & Treatment
Journal title
NUCLEAR MEDICINE AND BIOLOGY
ISSN journal
09698051 → ACNP
Volume
28
Issue
8
Year of publication
2001
Pages
975 - 982
Database
ISI
SICI code
0969-8051(200111)28:8<975:E(MLCS>2.0.ZU;2-3
Abstract
Two novel Tc-99m-(SNS/S) complexes: a mono-ester compound carrying an ethyl ester group on the tridentate ligand, (TcO)-Tc-99m[C2H5OOCCH2N(CH2CH2S)(2) ][SC6H4CH3], 3, and a diester compound, carrying a second ethyl ester group on the monodentate ligand, (TcO)-Tc-99m[C2H5OOCCH2N(CH2CH2S)(2)][SC6H4COOC 2H5], 4, were synthesized. The corresponding oxorhenium(V) complexes, 1 and 2 were also synthesized. Enzymatic hydrolysis demonstrated that 3 remains intact after 10 min incubation while 4 is totally converted to an unidentif ied hydrophilic complex. Tissue distribution data in mice revealed that bot h complexes, 3 and 4, exhibit significant initial brain uptake (1.42 and 1. 01% of injected dose at 5 minutes post injection respectively) and fast blo od clearance. (C) 2001 Elsevier Science Inc. All rights reserved.