Chemical and biological properties of 2,6-diisopropyl IDA labelled with 99mTc

Zmbova, B.; Djokić, D.; Ninković, D.; Obradović, Vladimir; Kostić, K.

doi:10.1016/0883-2889(87)90233-4

Cited by 5 publications

(1 citation statement)

References 3 publications

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“…Biodistribution studies showed that the radioactive copper complex was cleared quickly from body exclusively through the hepatic pathway in normal Sprague-Dawley rats (Figure 1). Kidney uptake of this Cu(II) complex was lower than that of clinically used hepatobiliary specificity reagents such as disofenin (DISIDA) [35], even though blood pool and liver clearance of Cu- 5 are much slower than those of the 99m Tc-IDA derivatives [36]. This comparatively slow blood clearance and very low renal excretion could be explained by the plasma protein binding.…”

Section: Discussionmentioning

confidence: 99%

A Potential Dubin-Johnson Syndrome Imaging Agent: Synthesis, Biodistribution, and MicroPET Imaging

Yoo¹,

Reichert²,

Kim³

et al. 2005

Mol Imaging

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Dubin-Johnson syndrome (DJS) is caused by a deficiency of the human canalicular multispecific organic anion transporter (cMOAT). A new lipophilic copper-64 complex of 1,4,7-tris(carboxymethyl)-10-(tetradecyl)-1,4,7,10-tetraazadodecane (5) was prepared and evaluated for potential as a diagnostic tool for DJS. The prepared ligand was labeled with (64)Cu citrate in high radiochemical purity. In vivo uptake and clearance of the complex was determined through biodistribution studies using normal Sprague-Dawley rats and mutant cMOAT-deficient (TR(-)) rats. In normal rats, the radioactive copper complex was cleared quickly from the body exclusively through the hepatic pathway. The (64)Cu complex was taken up rapidly by the liver and quickly excreted into the small intestine and then the upper large intestine, whereas <1% ID/organ was found in the kidney at all time points post injection. Whereas activity was accumulated continuously in the liver of TR(-) rats, it was not excreted into the small intestine. MicroPET studies of normal and TR(-) rats were consistent with biodistribution data and showed dramatically different images. This study strongly suggests that cMOAT is involved in excretion of (64)Cu-5. The significant difference between the biodistribution data and microPET images of the normal and TR(-) rats demonstrates that this new (64)Cu complex may allow noninvasive diagnosis of DJS in humans.

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Section: Discussionmentioning

confidence: 99%