Preparation and characterization of technetium complexes with Schiff base and phosphine coordination. 1. complexes of technetium-99g and -99m with substituted acac2en and trialkyl phosphines (where acac2en = N,N′-ethylenebis[acetylacetone iminato])

Marmion, Mary E.; Woulfe, Steven R.; Neumann, William L.; Nosco, Dennis L.; Deutsch, Edward

doi:10.1016/s0969-8051(99)00040-2

Cited by 37 publications

(37 citation statements)

References 16 publications

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“…The difference in the heart uptake of cationic 99m Tc radiotracers is most likely caused by their lipophilicity and capability to across the plasma and mitochondrial membranes. Cationic 99m Tc radiotracers with the log P>1.5 often have a low heart uptake and a slow liver clearance while more hydrophilic cationic radiotracers with log P<0 tend to show fast washout from the myocardium (1)(2)(3)(22)(23)(24)(25). In both cases, the heart/liver ratio is low because of either high liver uptake or fast myocardial washout.…”

Section: Discussionmentioning

confidence: 99%

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Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic ^99mTc-Nitrido Complexes

Kim

Hsieh

et al. 2007

Bioconjugate Chem.

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This report describes synthesis and evaluation of novel cationic 99m Tc-nitrido complexes, [ 99m TcN (L)(PNP)] + (L = ma, ema, tma, etma and mpo; PNP = PNP5, PNP6 and L6), as potential radiotracers for heart imaging. is of particular interest due to its high initial heart uptake (1.81±0.35 %ID/g at 5 min postinjection), and long myocardial retention (1.99±0.47 %ID/g at 120 min postinjection). The heart/liver ratio of [ 99m TcN(etma)(PNP5)] + (6.06±1.48) at 30 min postinjection is almost identical that of 99m TcN-DBODC5 (6.01±1.45), and is >2 times better than that of 99m Tcsestamibi (2.90±0.22). Results from metabolism studies show that [ 99m TcN(etma)(PNP5)] + has no significant metabolism in the urine; but it does show significant metabolism in feces samples at 120 min postinjection. Planar imaging studies suggest that [ 99m TcN(etma)(PNP5)] + might be able to give clinically useful images of the heart as early as 30 min postinjection. [ 99m TcN(etma)(PNP5)] + is a very promising candidate for more pre-clinical evaluations in various animal models.

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Section: Discussionmentioning

confidence: 99%

“…Lipophilicity plays a significant role in the heart uptake and excretion kinetics of cationic 99m Tc radiotracers (1,(22)(23)(24)(25). Thus, it is important to explore the impact of bidentate chelators and bisphosphines on lipophilicity of their cationic 99m Tc-nitrido complexes.…”

Section: Radiochemistrymentioning

confidence: 99%

Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic ^99mTc-Nitrido Complexes

Kim

Hsieh

et al. 2007

Bioconjugate Chem.

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“…However, several mechanistic studies suggest that molecular size, lipophilicity and charge play a major role in the uptake and retention in myocytes (21,34,35). In particular, ether containing chelators has been used to prepare complexes with improved heart-background ratios (36). The lipophilicity modulates the entry into the sarcolemmal and mitochondrial membranes, while the negative mitochondrial potential provides the electrochemical driving force for the radiotracers to enter the myocyté s mitochondria (37)(38)(39)(40)(41).…”

Section: Discussionmentioning

confidence: 99%

Rapid hepatic clearance of ^99mTc‐TMEOP: a new candidate for myocardial perfusion imaging

Goethals

Santos

Caveliers

et al. 2010

Contrast Media & Molecular

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“…In theory, the lower the lipophilicity of a compound the faster the clearance from the liver, whereas more hydrophilic radiotracers tend to show a low heart uptake with a fast washout from the myocardium [12, 13]. The special chemical feature of [ 99m Tc(PNP5)(DBODC)] + lies in the fact that its molecular structure is a compound of two different bidentate ligands, PNP5 and DBODC, bound to the same Tc≡N group [9, 10].…”

Section: Discussionmentioning

confidence: 99%

Experimental Study of [<sup>99m</sup>Tc(PNP5) (DBODC)]<sup>+</sup> as a New Myocardial Perfusion Imaging Agent

Zhang

Fang

et al. 2008

Cardiology

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Objectives: This study was aimed to compare the properties of [^99mTc(PNP5)(DBODC)]⁺ with ^99mTc-MIBI in normal swine and in canine models of myocardial ischemia. Methods: Seven anesthetized swine were injected intravenously with [^99mTc(PNP5)(DBODC)]⁺. Serial planar images were acquired meanwhile. Twelve adult dogs were studied. A critical stenosis of left anterior descending artery was produced. [^99mTc(PNP5)(DBODC)]⁺ or ^99mTc-MIBI (randomly) was injected intravenously at the end of 3 min of adenosine infusion. The occluder was released after adenosine infusion. Myocardial SPECT imaging was obtained at 30, 60, 90 and 180 min, respectively, after tracer injection. Rest myocardial SPECT imaging was acquired on the next day. Results: Blood disappearance of [^99mTc(PNP5)(DBODC)]⁺ was biexponential with an initial half-time of 2.97 ± 0.48 min and a late half-time of 52.49 ± 19.49 min. Myocardial [^99mTc(PNP5)(DBODC)]⁺ uptake was similar to ^99mTc-MIBI. Heart-to-liver ratio of [^99mTc(PNP5)(DBODC)]⁺ was significantly higher than that of ^99mTc-MIBI (0.99 ± 0.03 vs. 0.46 ± 0.10, p < 0.05) 30 min after injection. In canine models of myocardial ischemia, image quality of [^99mTc(PNP5)(DBODC)]⁺ was better than ^99mTc-MIBI. Segments with perfusion defects by [^99mTc(PNP5)(DBODC)]⁺ was 3.60 ± 1.52 and 4.25 ± 0.96 by ^99mTc-MIBI (p = n.s.). Conclusions: [^99mTc(PNP5)(DBODC)]⁺ seems to be a promising new myocardial perfusion imaging agent.

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Preparation and characterization of technetium complexes with Schiff base and phosphine coordination. 1. complexes of technetium-99g and -99m with substituted acac2en and trialkyl phosphines (where acac2en = N,N′-ethylenebis[acetylacetone iminato])

Cited by 37 publications

References 16 publications

Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic ^99mTc-Nitrido Complexes

Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic ^99mTc-Nitrido Complexes

Rapid hepatic clearance of ^99mTc‐TMEOP: a new candidate for myocardial perfusion imaging

Experimental Study of [<sup>99m</sup>Tc(PNP5) (DBODC)]<sup>+</sup> as a New Myocardial Perfusion Imaging Agent

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Preparation and characterization of technetium complexes with Schiff base and phosphine coordination. 1. complexes of technetium-99g and -99m with substituted acac2en and trialkyl phosphines (where acac2en = N,N′-ethylenebis[acetylacetone iminato])

Cited by 37 publications

References 16 publications

Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic 99mTc-Nitrido Complexes

Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic 99mTc-Nitrido Complexes

Rapid hepatic clearance of 99mTc‐TMEOP: a new candidate for myocardial perfusion imaging

Experimental Study of [<sup>99m</sup>Tc(PNP5) (DBODC)]<sup>+</sup> as a New Myocardial Perfusion Imaging Agent

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Product

Resources

About

Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic ^99mTc-Nitrido Complexes

Impact of Bidentate Chelators on Lipophilicity, Stability, and Biodistribution Characteristics of Cationic ^99mTc-Nitrido Complexes

Rapid hepatic clearance of ^99mTc‐TMEOP: a new candidate for myocardial perfusion imaging