Assessment of the best N(3-) donors in preparation of [M(N)(PNP)]-based (M=(99m)Tc-; (188)Re) target-specific radiopharmaceuticals: Comparison among succinic dihydrazide (SDH), N-methyl-S-methyl dithiocarbazate (HDTCZ) and PEGylated N-methyl-S-methyl dithiocarbazate (HO2C-PEG600-DTCZ)
| Autor: | Nicolò Morellato, Stefan Thieme, Davide Carta, Paolo Ruzza, Cristina Bolzati, Christian Jentschel, Hans-Jürgen Pietzsch, Fiorenzo Refosco, Nicola Salvarese, Ralf Bergmann |
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| Rok vydání: | 2014 |
| Předmět: |
Male
Cancer Research Stereochemistry Nitrogen chemistry.chemical_element Peptide High-performance liquid chromatography Medicinal chemistry Mice Drug Stability Succinates Animals Radiology Nuclear Medicine and imaging chemistry.chemical_classification Radioisotopes Tomography Emission-Computed Single-Photon Ligand Technetium Organotechnetium Compounds Rhenium Rats Hydrazines chemistry Yield (chemistry) Molecular Medicine Specific activity Therapy Radiopharmaceuticals Diphosphinoamines Cysteine |
| Zdroj: | Nuclear medicine and biology 41 (2014): 570–581. doi:10.1016/j.nucmedbio.2014.04.126 info:cnr-pdr/source/autori:Carta D.; Jentschel C.; Thieme S.; Salvarese N.; Morellato N.; Refosco F.; Ruzza P.; Bergmann R.; Pietzsch H.-J.; Bolzati C./titolo:Assessment of the best N3-donors in preparation of [M(N)(PNP)]-based (M=Tc-99m-; Re-188) target-specific radiopharmaceuticals: Comparison among succinic dihydrazide (SDH), N-methyl-S-methyl dithiocarbazate (HDTCZ) and PEGylated N-methyl-S-methyl dithiocarbazate (HO2C-PEG(600)-DTCZ)/doi:10.1016%2Fj.nucmedbio.2014.04.126/rivista:Nuclear medicine and biology/anno:2014/pagina_da:570/pagina_a:581/intervallo_pagine:570–581/volume:41 |
| ISSN: | 1872-9614 |
| DOI: | 10.1016/j.nucmedbio.2014.04.126 |
| Popis: | Succinic dihydrazide (SDH), N-methyl-S-methyl dithiocarbazate (HDTCZ) and PEGylated N-methyl-S-methyl dithiocarbazate (HO2C-PEG600-DTCZ) are nitrido nitrogen atom donors employed for the preparation of nitride [M(N)]-complexes (M=(99m)Tc and (188)Re). This study aims to compare the capability and the efficiency of these three N(3-) group donors, in the preparation of [M(N)PNP]-based target-specific compounds (M=(99m)Tc, (188)Re; PNP=aminodiphosphine). For this purpose, three different kit formulations (SDH kit; HO2C-PEG600-DTCZ kit; HDTCZ kit) were assembled and used in the preparation of [M(N)(cys~)(PNP3)](0/+) complexes (cys~=cysteine derivate ligands). For each formulation, the radiochemical yield (RCY) of the [M(N)(~cys)(PNP3)] compounds, was determined by HPLC. The deviation of the percentage of RCY, due to changes in concentration of the N(3-) donors and of the exchanging ligand, was determined. For (99m)Tc, data clearly show that HDTCZ is the most efficient donor of N(3-); however, SDH is the most suitable nitrido nitrogen atom donor for the preparation of [(99m)Tc(N)(PNP)]-based target-specific agents with high specific activity. When HO2C-PEG600-DTCZ or HDTCZ are used in N(3-) donation, high amounts of the exchanging ligand (10(-4)M) were required for the formation of the final complex in acceptable yield. The possibility to use microgram amounts of HDTCZ also in [(188)Re(N)] preparation (0.050mg) reduces its ability to compete in ligand exchange reactions, minimizing the quantity of chelators required to obtain the final complex in high yield. This finding can be exploit for increasing the radiolabeling efficiency in [(188)Re(N)]-radiopharmaceutical preparations compared to the previously reported HDTCZ-based procedure, notwithstanding a purification process could be necessary to improve the specific activity of the complexes. |
| Databáze: | OpenAIRE |
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