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Summary: In vivo evaluation of copper-64-labeled
monooxo-tetraazamacrocyclic ligands
Xiankai Suna,1
, Joonyoung Kima
, Arthur E. Martellb,F
, Michael J. Welcha
, Carolyn J. Andersona,*
a
Mallinckrodt Institute of Radiology, School of Medicine, Washington University, St. Louis, MO 63110, USA
b
Department of Chemistry, Texas A & M University, College Station, TX, 77842 USA
Received 27 February 2004; received in revised form 24 July 2004; accepted 3 August 2004
Abstract
Copper-64 (T1/2 =12.7 h; b+
: 0.653 MeV, 17.4%; bÀ
: 0.578 MeV, 39%) has applications in positron emission tomography (PET) imaging
and radiotherapy, and is conveniently produced on a biomedical cyclotron. Tetraazamacrocyclic ligands are the most widely used bifunctional
chelators (BFCs) for attaching copper radionuclides to antibodies and peptides due to their relatively high kinetic stability. In this paper, we
evaluated three monooxo-tetraazamacrocyclic ligands with different ring sizes and oxo group positions. H1 [1,4,7,10-tetraazacyclotridecan
11-one], H2 [1,4,8,11-tetraazacyclotetradecan-5-one] and H3 [1,4,7,10-tetraazacyclotridecan-2-one] were radiolabeled with 64
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