Complexation of rhenium-186 and technetium-99m tricarbonyl cores with 1,4,7-triazacyclononane based chelators for radiopharmaceutical applications
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Technetium-99m is widely used as a Single Photon Emission Computed Tomography (SPECT) imaging radionuclide in nuclear medicine due to its favorable decay characteristics (t1/2 = 6 h, [gamma] 140 keV (89 percent)) and the low cost and widespread availability of 99Mo/99mTc generators. Technetium-99m can be combined with beta-emitting rhenium radioisotopes 186Re (t1/2 = 89 h, E[beta]max = 1.07 MeV) or 188Re (t1/2 = 17 h, E[beta]max = 2.12 MeV) as a theranostic matched pair. Metal complexes of the general formula [MI(CO)3(k3-L)]+ (M = natRe, 99mTc, 186Re, 188Re) are of particular interest for radiopharmaceutical development because of the ease of synthesis of the [MI(CO)3(OH2)3]+ precursors in which the labile water ligands can be replaced by a suitable tridentate bifunctional chelator. In particular, cyclic chelators containing a 1,4,7-triazacyclononane (TACN) ring (e.g., NOTA and NODAGA) have proven to form exceptionally stable complexes with the [MI(CO)3]+ cores. In this work, we have investigated the role of the pendant arms on TACN-based chelators in complexation of the [M(CO)3]+ core through the synthesis of novel TACN-based chelators, (radio)labeling with the [MI(CO)3]+ cores, and evaluation of the stability and hydrophilicity of the resulting radiometal complexes.
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Ph. D.