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KMID : 0359320040440010015
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Korean Journal of Veterinary Research
2004 Volume.44 No. 1 p.15 ~ p.21
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Preparation and biological evaluation of (99m)Tc tricarbonyl cysteine
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Jang, Beom-su/장범수
Park, Kyung-bae/Yun, Hyo-in/박경배/윤효인
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Abstract
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This paper describes the development of ^(99m)Tc tricarbonyl cysteine as potential renal function diagnostic radiopharmaceutical and evaluation of its biological characteristics using experimental animals. l-Cysteine was labeled efficiently with ^(99m)Tc tricarbonyl precursor ([^(99m)Tc(CO)₃(H₂O)₃)]^(+)) under 30 min heating at 75℃. Labeling yield and stability were analyzed by high performance liquid chromatography (HPLC). The biodistribution property of ^(99m)Tc tricarbonyl cysteine in mice and its dynamic imaging profiles in rabbits were carried out. To investigate the excretion mechanism of ^(99m)Tc tricarbonyl cysteine, tubular transport inhibition test with probenecid was adopted. ^(99m)Tc tricarbonyl cysteine was obtained with a high labeling yield under the moderate condition. The results of biodistribution experiments of ^(99m)Tc tricarbonyl cysteine in ICR mice at 3 and 90 min provided that 99mTc tricarbonyl cysteine was very highly accumulated in the kidney and bladder, thereby almost 99% of ^(99m)Tc tricarbonyl cysteine was excreted within 90 min post injection. The same results were confirmed by the whole body dynamic images for 30 minutes and static images in rabbits at given time intervals after injection. Renogram of ^(99m)Tc tricarbonyl cysteine in rabbits showed that its T_(max) and T_(1/2) of ^(99m)Tc tricarbonyl cysteine were 2.33±0.56 and 4.30±0.79 min, respectively. The T_(max) of ^(99m)Tc tricarbonyl cysteine with probenecid pretreatment was 2.30±0.17 min, whereas T_(1/2) of that with probenecid pretreatment was 17.0±32.47 min. T_(1/2) of ^(99m)Tc tricarbonyl cysteine with probenecid pretreatment was significantly different, as compared to the result without probenecid (p<0.0001). The results showed that the excretion of ^(99m)Tc tricarbonyl cysteine was extremely affected by probenecid. Therefore, ^(99m)Tc tricarbonyl cysteine was rapidly excreted from the kidney principally by the tubular secretion.
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