Synthesis, Solution‐State and Solid‐State Structural Characterization of Monocationic Nitrido Heterocomplexes [M(N)(DTC)(PNP)]<sup>+</sup> (M = <sup>99</sup>Tc, Re; DTC = Dithiocarbamate; PNP = Heterodiphosphane)

Bolzati, Cristina; Refosco, Fiorenzo; Cagnolini, Aldo; Tisato, Francesco; Boschi, Alessandra; Duatti, Adriano; Uccelli, Licia; Dolmella, Alessandro; Marotta, Ester; Tubaro, Michela

doi:10.1002/ejic.200300666

Cited by 49 publications

(29 citation statements)

References 18 publications

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“…The N10–Re– X angles ( X = equatorial donor atom) fall in the range between 92.6 and 111.5°, the corresponding N10–Tc– X angles are between 93.3 and 112.0°. These values are in complete agreement with the typical bonding situation of square‐pyramidal Re V N and Tc V N complexes 8…”

Section: Resultssupporting

confidence: 87%

Syntheses and Structures of Nitridorhenium(V) and Nitridotechnetium(V) Complexes with N,N‐[(Dialkylamino)(thiocarbonyl)]‐N′‐(2‐hydroxyphenyl)benzamidines

Nguyen¹,

Trieu²,

Abram³

2011

Zeitschrift anorg allge chemie

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Section: Resultssupporting

confidence: 87%

Syntheses and Structures of Nitridorhenium(V) and Nitridotechnetium(V) Complexes with N,N‐[(Dialkylamino)(thiocarbonyl)]‐N′‐(2‐hydroxyphenyl)benzamidines

Nguyen¹,

Trieu²,

Abram³

2011

Zeitschrift anorg allge chemie

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“…The nitrido ligand is a powerful π-electron donor and shows a high capacity to stabilize the Tc(V) oxidation state. The [Tc≡N] 2+ core forms Tc(V)-nitrido complexes with various chelators[120][121][122][123][124][125][126]. The [ 99m Tc≡N] 2+ core has been used for 99m Tc-labeling of small peptides and benzodiazepine receptor ligands[127][128][129].…”

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confidence: 99%

Bifunctional coupling agents for radiolabeling of biomolecules and target-specific delivery of metallic radionuclides

Liu

2008

Advanced Drug Delivery Reviews

365

339

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Receptor-based radiopharmaceuticals are of great current interest in molecular imaging and radiotherapy of cancers, and provide a unique tool for target-specific delivery of radionuclides to the diseased tissues. In general, a target-specific radiopharmaceutical can be divided into four parts: targeting biomolecule (BM), pharmacokinetic modifying (PKM) linker, bifunctional coupling or chelating agent (BFC), and radionuclide. The targeting biomolecule serves as a "carrier" for specific delivery of the radionuclide. PKM linkers are used to modify radiotracer excretion kinetics. BFC is needed for radiolabeling of biomolecules with a metallic radionuclide. Different radiometals have significant difference in their coordination chemistry, and require BFCs with different donor atoms and chelator frameworks. Since the radiometal chelate can have a significant impact on physical and biological properties of the target-specific radiopharmaceutical, its excretion kinetics can be altered by modifying the coordination environment with various chelators or coligand, if needed. This review will focus on the design of BFCs and their coordination chemistry with technetium, copper, gallium, indium, yttrium and lanthanide radiometals.

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“…Previ ously, we reported a new class of nitrido 99m Tc agents of the type [ 99m Tc(N)(DTC)(PNP)] 1 , where DTC is a dithiocarbamate ligand and PNP an aminodiphosphine ligand, as potential myocardial imaging agents (1)(2)(3). Among the tested compounds, [ 99m Tc(N)(DBODC)(PNP5)] 1 and [ 99m Tc(N)(DBODC)(PNP3)] 1 ( Fig.…”

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confidence: 99%

Subcellular Distribution and Metabolism Studies of the Potential Myocardial Imaging Agent [^99mTc(N)(DBODC)(PNP5)]⁺

Bolzati¹,

Cavazza-Ceccato²,

Agostini³

et al. 2008

J Nucl Med

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99m Tc(N)-DBODC(5) is the lead compound of a new series of monocationic 99m Tc(N)-based potential myocardial imaging agents that exhibit original biodistribution properties. This study was addressed to elucidate the mechanisms of distribution, retention, and elimination of this promising 99m Tc(N)-agent. Methods: The sex-related in vitro and in vivo stability and the subcellular distribution of 99m Tc(N)-DBODC(5) were investigated. Studies were performed by considering binding to the serum proteins; stability in rat serum, human serum, and rat liver homogenates; and the chemical integrity of the complex after extraction from rat tissues such as heart, liver, and kidney, as well as from intestinal fluids and urine. The effect of cyclosporin A on the in vivo pharmacokinetic properties of 99m Tc(N)-DBODC(5) was also evaluated. Subcellular distribution of 99m Tc(N)-DBODC(5) in ex vivo rat heart was determined by standard differential centrifugation techniques. Results: No significant in vitro serum protein binding and no notable biotransformation of the native compound into different species by the in vitro action of the serum and liver enzymes was evidenced. In vivo experiments showed that sex affects the pharmacokinetic profile of the 99m Tc(N)-complexes including metabolism and excretion. Chromatographic profiles of 99m Tc(N)-radioactivity extracted from tissues and fluids of female rats were always coincident with the control. Conversely, a small percentage of metabolized species was detected by high-performance liquid chromatography in liver extracts of male rats. Furthermore, administration of cyclosporin A caused a significant reduction of lung, liver, and kidney washout along with a considerable variation in activity distribution in the intestinal tract in both male and female rats, thus indicating a possible implication of Pgp transporters in determining the biologic behavior of 99m Tc(N)-DBODC(5). However, this phenomenon was more pronounced in females. Subcellular distribution studies showed that 86.3% 6 7.4% of 99m Tc(N)-DBODC(5) was localized into mitochondrial fraction as a result of the interaction with the negative membrane potential. Conclusion: Evidence showing that the new 99m Tc(N)-myocardial tracers behave as multidrug resistance-associated protein P-glycoprotein substrates, combined with their selective mitochondrial accumulation, strongly supports the possibility that diagnostic application of 99m Tc(N)-DBODC(5) can be extended to tumor imaging and noninvasive multidrug resistance studies. (Fig. 1) (DBODC 5 bis-(N-ethoxyethyl)dithiocarbamato; PNP5 5 bis-(dimethoxypropylphosphinoethyl)ethoxyethylamine, PNP3 5 bis-(dimethoxypropylphosphinoethyl)methoxyethylamine) exhibited the most interesting biodistribution properties (3). In particular, animal studies of [ 99m Tc(N)(DBODC)(PNP5)] 1 (abbreviated 99m Tc(N)-DBODC(5)) revealed high and persistent myocardial uptake and rapid blood, lung, and liver clearance yielding high-quality images of the heart as early as 20 to 30 min after injection (4,5).S...

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Synthesis, Solution‐State and Solid‐State Structural Characterization of Monocationic Nitrido Heterocomplexes [M(N)(DTC)(PNP)]⁺ (M = ⁹⁹Tc, Re; DTC = Dithiocarbamate; PNP = Heterodiphosphane)

Cited by 49 publications

References 18 publications

Syntheses and Structures of Nitridorhenium(V) and Nitridotechnetium(V) Complexes with N,N‐[(Dialkylamino)(thiocarbonyl)]‐N′‐(2‐hydroxyphenyl)benzamidines

Syntheses and Structures of Nitridorhenium(V) and Nitridotechnetium(V) Complexes with N,N‐[(Dialkylamino)(thiocarbonyl)]‐N′‐(2‐hydroxyphenyl)benzamidines

Bifunctional coupling agents for radiolabeling of biomolecules and target-specific delivery of metallic radionuclides

Subcellular Distribution and Metabolism Studies of the Potential Myocardial Imaging Agent [^99mTc(N)(DBODC)(PNP5)]⁺

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Synthesis, Solution‐State and Solid‐State Structural Characterization of Monocationic Nitrido Heterocomplexes [M(N)(DTC)(PNP)]+ (M = 99Tc, Re; DTC = Dithiocarbamate; PNP = Heterodiphosphane)

Cited by 49 publications

References 18 publications

Syntheses and Structures of Nitridorhenium(V) and Nitridotechnetium(V) Complexes with N,N‐[(Dialkylamino)(thiocarbonyl)]‐N′‐(2‐hydroxyphenyl)benzamidines

Syntheses and Structures of Nitridorhenium(V) and Nitridotechnetium(V) Complexes with N,N‐[(Dialkylamino)(thiocarbonyl)]‐N′‐(2‐hydroxyphenyl)benzamidines

Bifunctional coupling agents for radiolabeling of biomolecules and target-specific delivery of metallic radionuclides

Subcellular Distribution and Metabolism Studies of the Potential Myocardial Imaging Agent [99mTc(N)(DBODC)(PNP5)]+

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Product

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Synthesis, Solution‐State and Solid‐State Structural Characterization of Monocationic Nitrido Heterocomplexes [M(N)(DTC)(PNP)]⁺ (M = ⁹⁹Tc, Re; DTC = Dithiocarbamate; PNP = Heterodiphosphane)

Subcellular Distribution and Metabolism Studies of the Potential Myocardial Imaging Agent [^99mTc(N)(DBODC)(PNP5)]⁺