Issue 42, 2017

99mTc-3Cboroxime: a novel 99mTc(iii) complex [99mTcCl(CDO)(CDOH)2B-3C] (CDOH2 = cyclohexanedione dioxime; 3C-B(OH)2 = 3-(carbamoylphenyl)boronic acid) with high heart uptake and long myocardial retention

Abstract

In this study, a new 99mTc(III) complex [99mTcCl(CDO)(CDOH)2B-3C] (99mTc-3Cboroxime: CDOH2 = cyclohexanedione dioxime; 3C-B(OH)2 = 3-(carbamoylphenyl)boronic acid) was evaluated as a radiotracer for heart imaging. 99mTc-3Cboroxime was prepared in high radiochemical purity (RCP > 95%). Biodistribution and imaging studies were performed using Sprague–Dawley rats (200–225 g). We found that the heart uptake of 99mTc-3Cboroxime (3.43 ± 0.11%ID g−1) at 2 min postinjection (p.i.) was close to that of 99mTc-Teboroxime (3.00 ± 0.37%ID g−1), and the heart uptake value of 99mTc-3Cboroxime was almost unchanged over the first 15 min (3.05 ± 0.35%ID g−1 at 15 min p.i.). 99mTc-3Cboroxime had lower uptake than 99mTc-Teboroxime in the blood, lungs and muscle over a 60 min period. Its heart/blood, heart/lung and heart/muscle ratios were better than those of 99mTc-Teboroxime. These results suggest that 99mTc-3Cboroxime has a significant advantage over 99mTc-Teboroxime with respect to myocardial retention and heart/background ratios. However, its liver uptake at 2 min p.i. was higher than that of 99mTc-Teboroxime. Because of its faster liver clearance, 99mTc-3Cboroxime had heart/liver ratios close to or better than that of 99mTc-Teboroxime at ≥5 min p.i. As a result, good quality SPECT images could be obtained in any of the 5 min imaging windows over the first 20 min after injection of 99mTc-3Cboroxime. More importantly, the results from this study show that the use of the 3-carbamylphenyl group is an interesting approach to achieve long heart retention for new 99mTc(III) radiotracers. Future research will focus on further minimizing liver radioactivity while maintaining high heart uptake over a wide time window.

Graphical abstract: 99mTc-3Cboroxime: a novel 99mTc(iii) complex [99mTcCl(CDO)(CDOH)2B-3C] (CDOH2 = cyclohexanedione dioxime; 3C-B(OH)2 = 3-(carbamoylphenyl)boronic acid) with high heart uptake and long myocardial retention

Article information

Article type
Frontier
Submitted
10 Apr 2017
Accepted
30 Mai 2017
First published
31 Mai 2017

Dalton Trans., 2017,46, 14509-14518

99mTc-3Cboroxime: a novel 99mTc(III) complex [99mTcCl(CDO)(CDOH)2B-3C] (CDOH2 = cyclohexanedione dioxime; 3C-B(OH)2 = 3-(carbamoylphenyl)boronic acid) with high heart uptake and long myocardial retention

M. Liu and S. Liu, Dalton Trans., 2017, 46, 14509 DOI: 10.1039/C7DT01292F

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