2005
DOI: 10.1162/15353500200504160
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A Potential Dubin-Johnson Syndrome Imaging Agent: Synthesis, Biodistribution, and MicroPET Imaging

Abstract: 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… Show more

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Cited by 7 publications
(5 citation statements)
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“…Recently, the ATSM analog has been used as a bifunctional chelator to attach Cu radionuclides to peptides. Several other small molecules have been labeled with 64 Cu (Figure ), for instance, a series of tetraaza macrocyclic ligands with methanephosphonate pendant arms showing a therapeutic effect on bone tumors or 1,4,7-tris(carboxymethyl)-10-(tetradecyl)-1,4,7,10-tetraazadodecane, which was shown to be an agent to diagnose Dubin–Johnson Syndrome (DJS).…”
Section: Radionuclides For Imaging and Therapymentioning
confidence: 99%
“…Recently, the ATSM analog has been used as a bifunctional chelator to attach Cu radionuclides to peptides. Several other small molecules have been labeled with 64 Cu (Figure ), for instance, a series of tetraaza macrocyclic ligands with methanephosphonate pendant arms showing a therapeutic effect on bone tumors or 1,4,7-tris(carboxymethyl)-10-(tetradecyl)-1,4,7,10-tetraazadodecane, which was shown to be an agent to diagnose Dubin–Johnson Syndrome (DJS).…”
Section: Radionuclides For Imaging and Therapymentioning
confidence: 99%
“…Copper-64 macrocycles have been evaluated as substrates for the organic anion transporter for potential use as a diagnostic tool for Dubin-Johnson's syndrome. Small animal studies indicated that the cMOAT was involved in the excretion of the Cu-64 complex of compound 5 (47). A gene mutation of this organic anion transporter appears to cause Dubin-Johnson syndrome in humans (48).…”
Section: Membrane Transportmentioning
confidence: 99%
“…Biliary scintigraphy with agents such as 99m Tc-lidofenin or 99m TC-disofenin may be helpful in the evaluation of patients with Dubin-Johnson and Rotor syndromes [204][205][206]. In six patients with Dubin-Johnson syndrome, administration of 99m Tc-lidofenin was followed by rapid, intense, homogeneous accumulation of isotope within the liver without visualization of the intrahepatic biliary tree [204].…”
Section: Imaging Studiesmentioning
confidence: 99%