Chloro → hydroxy substitution on technetium BATO [TcCl(dioxime)3BR] complexes

Jurisson, Silvia S.; Hirth, Walter; Linder, Karen E.; Rocco, Richard J. Di; Narra, Ramakrishna; Nowotnik, David P.; Nunn, Adrian D.

doi:10.1016/0883-2897(91)90012-a

Cited by 11 publications

(37 citation statements)

References 13 publications

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“…99m Tc-Teboroxime was prepared according to the literature method [20,22]. Its RCP is 95 – 98% without purification.…”

Section: Resultsmentioning

confidence: 99%

“…Once it was prepared, 99m Tc-Teboroxime was stable for more than 6 h in kit matrix (Figure SI1). In the literature [20,22], excess NaCl (~100 mg per vial) was used to maintain the solution stability of 99m Tc-Teboroxime. We found that NaCl was not needed since the product showed identical HPLC profiles without NaCl (Figure SI2).…”

Section: Resultsmentioning

confidence: 99%

“…The short myocardial retention of 99m Tc-Teboroxime has been attributed to rapid dissociation of the Cl ligand and its hydrolysis in vivo [19,20]. It was reported that the half-life of Cl − anion was ~13 min under physiological conditions (pH = 7.4) [20].…”

Section: Introductionmentioning

confidence: 99%

“…It was reported that the half-life of Cl − anion was ~13 min under physiological conditions (pH = 7.4) [20]. If this is true, then the myocardial retention of a radiotracer might be improved by increasing its solution stability.…”

Section: Introductionmentioning

confidence: 99%

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Effect of co-ligands on chemical and biological properties of 99mTc(III) complexes [99mTc(L)(CDO)(CDOH)2BMe] (L=Cl, F, SCN and N3; CDOH2=cyclohexanedione dioxime)

Zheng

Tomaselli

et al. 2014

Nuclear Medicine and Biology

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Introduction 99mTc-Teboroxime ([99mTcCl(CDO)(CDOH)2BMe]) is a member of the BATO (boronic acid adducts of technetium dioximes) class of 99mTc(III) complexes. This study sought to explore the impact of co-ligands on solution stability, heart uptake and myocardial retention of [99mTc(L)(CDO)(CDOH)2BMe] (99mTc-Teboroxime: L = Cl; 99mTc-Teboroxime(F): L = F; 99mTc-Teboroxime(SCN): L = SCN; and 99mTc-Teboroxime(N3): L = N3). Methods Radiotracers 99mTc-Teboroxime(L) (L = F, SCN and N3) were prepared by reacting 99mTc-Teboroxime with NaF, NaSCN and NaN3, respectively. Biodistribution and imaging studies were carried out in Sprague-Dawley rats. Image quantification was performed to compare their heart retention and liver clearance kinetics. Results Complexes 99mTc-Teboroxime(L) (L = F, SCN and N3) were prepared in high yield with high radiochemical purity. All new radiotracers were stable for >6 h in the kit matrix. In its HPLC chromatogram, 99mTc-Teboroxime showed one peak at ~15.5 min, which was shorter than that of 99mTc-Teboroxime(F) (~16.4 min). There were two peaks for 99mTc-Teboroxime(SCN) at 16.5 and 18.3 min. 99mTc-Teboroxime(N3) appeared as a single peak at 18.4 min. Their heart retention and liver clearance curves were best fitted to the bi-exponential decay function. The half-times of fast/slow components were 1.6 ± 0.4/60.7±8.9 min for 99mTc-Teboroxime, 0.8±0.2/101.7±20.7 min for 99mTc-Teboroxime(F), 1.2±0.3/84.8±16.6 min for 99mTc-Teboroxime(SCN), and 2.9±0.9/51.6±5.0 min for 99mTc-Teboroxime(N3). The 2-min heart uptake followed the order of 99mTc-Teboroxime (3.00±0.37%ID/g) > 99mTc-Teboroxime(N3) (2.66±0.01 %ID/g) ≈ 99mTc-Sestamibi (2.55±0.46 %ID/g) > 99mTcN-MPO (2.38±0.15 %ID/g). 99mTc-Teboroxime remains the best in first-pass extraction. The best image acquisition window is 0 – 5 min for 99mTc-Teboroximine and 0 – 15 min for 99mTc-Teboroximine(N3). Conclusion Co-ligands had significant impact on the heart uptake and myocardial retention of complexes [99mTc(L)(CDO)(CDOH)2BMe] (L = Cl, F, SCN and N3). Future studies should be directed towards minimizing the liver uptake and radioactivity accumulation in the blood vessels while maintaining their high heart uptake.

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“…99m Tc-Teboroxime was prepared according to the literature method [20,22]. Its RCP is 95 – 98% without purification.…”

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Effect of co-ligands on chemical and biological properties of 99mTc(III) complexes [99mTc(L)(CDO)(CDOH)2BMe] (L=Cl, F, SCN and N3; CDOH2=cyclohexanedione dioxime)

Zheng

Tomaselli

et al. 2014

Nuclear Medicine and Biology

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“…Initial brain imaging studies appear to show similar regional distribution patterns as the other agents, however, the mechanism of uptake and retention is not clear. It is important to note that Tc-BATO complexes contain a labile chloride ion in the coordination sphere which may contribute to its retention properties [21].…”

Section: Introductionmentioning

confidence: 99%