Kit formulation and preliminary toxicity of [^99mTc(CO)₃]⁺ intermediate: A novel technetium radiopharmaceutical platform

Abstract

The radiochemistry of 99"'Tc carbonyl complexes has been expanding over the last few years following the basic chemistry advances of preparing the [Tc(CO)3]' core in aqueous solution directly from perte~hnetatel-~. The field is participating in research of novel organometallic molecules for specific brain imaging receptors, in addition to finding wide applications in protein and peptide labeling4.'.

Comparative evaluation of [99mTc(H2O)3(CO)3]+ precursor synthesized by conventional method and by using carbonyl kit

“…Preliminary investigations using HPLC have confirmed the formation of Tc carbonyl core while using the freeze dried kit. 24 It has shown that the formulation is reproducible, robust and simple for the preparation of 99m Tc(OH 2 ) 3 (CO) 3 precursor. Complexation studies of histidine with kit precursor have been carried out earlier to confirm its utility for synthesis of tricarbonyl complexes.…”

Diagnostic Nuclear Medicine

“…Moreover, these complexes can be formed with very small amounts of the ligand, resulting in preparations with extremely high specific activity. Recently, the preparation of the intermediary tri-aqua tricarbonyl Tc(I) core has been further optimized by using potassium boranocarbonate (K 2 BH 3 CO 2 ) as both a solid source of CO and the reductant for labeling with 99m Tc (Dyszlewski et al 2001). This has allowed the production of a kit formulation for the preparation of the tricarbonyl Tc(I) intermediate, which can then be further used for convenient production of a wide diversity of Tc(I) tricarbonyl compounds by ligand for water exchange.…”

2‐Amino‐3‐(1‐(4‐(4‐(2‐methoxyphenyl) piperazine‐1‐yl)butyl)‐1H‐1,2,3‐triazol‐4‐yl) propanoic acid: synthesized, 99mTc‐tricarbonyl labeled, and bioevaluated as a potential 5HT1A receptor ligand

“…Over the last years, the radiochemistry of 99m Tc‐tricarbonyl complexes has been extended to find useful applications in radiochemistry and nuclear medicine. The basis for this kind of radiochemistry is the convenient preparation of the Tc‐tricarbonyl precursor [ 99m Tc(CO) 3 (H 2 O) 3 ] + either in the classic way with CO gas and borohydride reduction or with an IsoLink kit . In the resulting precursor, the three water molecules can easily be replaced by ligands that contain suitable donor atoms to form stable complexes.…”