Synthesis and biodistribution of two novel 99mTc “3+1”mixed ligand complexes as potential brain perfusion agents |
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Authors: | Duan Xin-hong L? Gong-xu Wang Xue-bin |
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Institution: | (1) College of Basic Science and Technology, Beijing Forestry University, Beijing, 100083, P.R. China;(2) Department of Chemistry, Beijing Normal University, Beijing, 100875, P.R. China |
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Abstract: | The research in the last decade has been mainly aimed at the development of technetium-99m radiopharmaceuticals, among which
are the “3+1”mixed ligand complexes. Two novel 99mTc]“3+1”mixed ligand complexes each carrying the tridentate ligand, the N-(o-Methylthiophenyl)ethylenediamine or the N-(o-Methylthiophenyl)-b-mercaptoacetamide
in combination with monothiolate coligand were produced using stannous chloride as reductant and glucoheptonate as transfer
ligand. The identification of 99mTc]-6 and 99mTc]-7 was established by thin layer chromatography. The radiochemical purity of two complexes was over 90%. Biodistribution
data in mice showed that both 99mTc]-6 and 99mTc]-7 can penetrate the intact blood-brain barrier and exhibited retention in mice brain. The brain uptakes (%ID/g) were 1.76,
1.17, 0.90 and 0.68, 0.38 ,0.37 at 2, 30, and 60 minutes i.v. postinjection for 99mTc]-6 and 99mTc]-7, respectively. Examples in this report comfirm us that it is promising to develop 99mTc complexes as potential brain perfusion agents based on modifying either the tridentate or the monodentate ligands.
This revised version was published online in August 2006 with corrections to the Cover Date. |
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