6-Hydrazinonicotinamide Derivatives as Bifunctional Coupling Agents for 99mTc-Labeling of Small Biomolecules

Liu, Shuang

doi:10.1007/b101226

Cited by 42 publications

(46 citation statements)

References 79 publications

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“…This conclusion is also supported by the coligand effect observed in this and our previous studies [28]. The HYNIC technology and its utility in the development of targetspecific radiopharmaceuticals have been reviewed extensively [49][50][51][52].…”

Section: Radiochemistrysupporting

confidence: 82%

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Liu

Kim

Hsieh

et al. 2008

Nuclear Medicine and Biology

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In this study, we present the evaluation of two new ternary ligand 99m Tc complexes [ 99m Tc(HYNICtetramer)(tricine)(L)] (L = ISONIC and PDA) as potential radiotracers for tumor imaging. The athymic nude mice bearing the MDA-MB-435 human breast cancer xenografts were used to evaluate their biodistribution and metabolic properties. The solution stability data showed that [ 99m Tc (HYNIC-tetramer)(tricine)(L)] (L = ISONIC and PDA) had a significant (14% and 35%, respectively) at 6 h in the absence of excess ISONIC or PDA coligand. Biodistribution data clearly showed that [ 99m Tc(HYNIC-tetramer)(tricine)(PDA)] has much lower uptake in most organs of interest than [ 99m Tc(HYNIC-tetramer)(tricine)(ISONIC)] during the 2 h study period. Results from metabolism studies revealed that ~50% of [ 99m Tc(HYNIC-tetramer)(tricine)(ISONIC)] remained intact in feces samples at 120 min p.i. Only 10% of [ 99m Tc(HYNIC-tetramer)(tricine)(PDA)] remained intact in feces samples. The extent of metabolism correlates well with the radiotracer solution stability. The results from this and our previous studies clearly demonstrated that coligands (TPPTS, ISONIC and PDA) have a significant impact on tumor uptake, excretion kinetics and metabolism of the 99m Tc-labeled cyclic RGDfK tetramer. Among the three radiotracers evaluated in this tumor-bearing animal model, [ 99m Tc(HYNIC-tetramer)(tricine)(TPPTS)] remains the best with respect to blood clearance, tumor uptake, target/background ratios.

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Section: Radiochemistrysupporting

confidence: 82%

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Liu

Kim

Hsieh

et al. 2008

Nuclear Medicine and Biology

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“…To overcome these problems, we developed a new ASGP-R agent using PVLA as the backbone by incorporating hydrazinonicotinamide-functionalized groups for radiolabeling with 99m Tc. Hydrazinonicotinamide is an attractive bifunctional coupling agent for preparing 99m Tc-labeled antibodies, peptides, and small biomolecules (30). We synthesized P(VLAco-VNI) through polymerization of 2 monomers, VLA and VNI, with good yield and easy purification.…”

Section: Discussionmentioning

confidence: 99%

“…About 0.185 MBq (in 100 mL of solution) of 99m Tc[P(VLA-co-VNI)](tricine) 2 (;1 · 10 29 mol of polymer/kg of body weight) was injected through the tail vein. At selected times (10,30, and 120 min), mice (n 5 5 at each time point) were sacrificed, and the tissues and organs of interest were collected, wet-weighed, and counted in a g-counter. The percentage injected dose per gram (%ID/g) for each sample was calculated by comparing its activity with an appropriate standard of ID.…”

Section: Biodistributionmentioning

confidence: 99%

Copolymer-Based Hepatocyte Asialoglycoprotein Receptor Targeting Agent for SPECT

Yang

Mou²,

Shao³

et al. 2011

J Nucl Med

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Poly(vinylbenzyl-O-b-D-galactopyranosyl-D-gluconamide) (PVLA) can be specifically internalized by hepatocytes via the asialoglycoprotein receptor. In this study, we synthesized and characterized galactose-carrying copolymers with hydrazinonicotinamide chains as bifunctional groups to radiolabel PVLA with 99m Tc for SPECT targeting specific hepatocytes. Methods:The copolymer was labeled with 99m Tc using tricine as a coligand. Then 99m Tc[P(VLA-co-VNI)](tricine) 2 was evaluated by in vivo metabolic stability and biodistribution in normal mice. SPECT was performed in normal New Zealand White rabbits and rabbits with liver cancer. Results: 99m Tc[P(VLA-co-VNI)](tricine) 2 was prepared in high labeling yield (.95%) and radiochemical purity (.99%), with good stability. The results of biodistribution in mice demonstrated that the liver uptake was 125.33 6 10.99 percentage injected dose per gram at 10 min after injection and could be blocked significantly by preinjecting free neogalactosylalbumin or P(VLA-co-VNI). SPECT images with high quality were obtained at 15, 30, 60, and 120 min after injection of the radiotracer. Significant radioactivity defect was observed in the liver cancer model. Conclusion: The bifunctional coupling agent hydrazinonicotinamide was introduced to PVLA via copolymerization and labeled with 99m Tc. The promising biologic properties of 99m Tc[P(VLA-co-VNI)](tricine) 2 afford potential applications for the assessment of hepatocyte function in the future.

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“…Decomposition of the radiopharmaceutical prior to or during administration will decrease the targeting capability. Therefore, it is very important to use the antioxidant after preparation of MS [21].…”

Section: Discussionmentioning

confidence: 99%

Radiolabeling and cell incorporation studies of gemcitabine HCl microspheres on bladder cancer and papilloma cell line

İlem-Özdemir

Karavana

Şenyiğit

et al. 2016

J Radioanal Nucl Chem

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In the present study incorporation differences between the developed formulations for treatment for bladder cancer was investigated by radioactive cell culture studies. Developed bioadhesive microspheres (MS) and gemcitabinehydrochloride loaded MS (GHCl-MS) were radiolabeled. After observing the optimum labeling conditions, 99m Tc-MS and 99m Tc-GHCl-MS were loaded to the chitosan gel (CG) and poloxamer gel. The in vitro cell incorporation affinity of newly developed formulations to bladder papilloma (RT4) and the carcinoma (T24) cell lines was investigated. Cell culture studies results indicate that the use of prolonged release bioadhesive CG formulation was highly improved the targeting of the GHCl to the cancer cells. Graphical Abstract

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6-Hydrazinonicotinamide Derivatives as Bifunctional Coupling Agents for 99mTc-Labeling of Small Biomolecules

Cited by 42 publications

References 79 publications

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Copolymer-Based Hepatocyte Asialoglycoprotein Receptor Targeting Agent for SPECT

Radiolabeling and cell incorporation studies of gemcitabine HCl microspheres on bladder cancer and papilloma cell line

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