Functionalized linear tetra-aza ligands for complexing technetium: potential species for antibody labelling

Syntheses of charge-compensated dicarbollide ligand precursors and their use in the preparation of novel metallacarboranes

“…The 160-MHz nB FTNMR spectra of each of the three products shows a similar pattern, which includes eight terminal proton-coupled resonances (J = 128-158 Hz) in the region between -2 and -37 ppm and one bridging proton-coupled peak (J = 43 Hz in the diisopropylamine derivative) near -10 ppm due to the nitrogen-substituted boron. Such a pattern is characteristic of a substituted-boron atom located at the open pentagonal face of the nido cage and occupying either of the equivalent B (10) or B (11) positions. In the 200-MHz FTNMR spectra of CD2C12 solutions of each product at 298 K, two different carboranyl CH resonances with equal intensity around 2 ppm were observed.…”

“…The dicarbollide dianions1 [m'</o-7,8-C2B9Hu]2" (1) and carborane complex by a Lewis base,5•9 addition of dialkyl sulfide to a protonated metallocene-type sandwich complex,41" and metalation of a pyridine-substituted carborane ligand. 10 In order to develop a more general methodology for the synthesis of novel metallacarborane complexes of this type, we have investigated the synthesis of neutral charge-compensated carborane cage derivatives for use as precursors to monoanionic substituted dicarbollide ligands and the use of the latter in the preparation of metallacarborane complexes.6…”

A nuclear chocolate box: the periodic table of nuclear medicine

“…has yet to be introduced. The TcO 3+ core can be linked to biomolecules by a variety of nitrogen- and sulfur-donor polydentate ligands such as mercaptoacetyl triglycine (MAG3, 19 ),44 1,4,8,11-tetraaminododecane ( 25 ),45, 46 dimercaptosuccinic acid ( 15 )47 etc. (Fig.…”

Experience with the iodine-123 and technetium-99m labelled anti-granulocyte antibody MAb47: a comparison of labelling methods

“…The ligand 2,12-dimethyl-5,9,-bis(n-propionic acid)-2,5,9,12-tetraazatridecane (mtp) was synthesized and activated with N-hydroxy-succinimide, yielding mtp-nhs (Fig. 1) according to the method de- [12]. For coupling, a solution of about 5-8 mg MAb47 in slightly alkaline phosphate buffer (0.1 M, pH 7.5-8) was mixed with a solution of 5-70 mg dry mtp-nhs .…”

“…It is known that this amount of antibody generally induces a HAMA response [9][10][11]. We tried to circumvent this problem by increasing the specific activity, so minimizing the protein content, and our strategy to achieve this goal involved the use of a 99mTc-selective ligand coupled to the protein [12]. Experimentally it was difficult to govern the coupling conditions of the particular ligand used and subsequently a simpler kit preparation was evaluated.…”