Biological evaluation of two anomeric glucose analogues iodinated in position

• Published in: Nuclear medicine and biology 1997-08, Vol.24 (6), p.519-525
• Main Authors: Koumanov, Françoise, Henry, Christelle, Ghezzi, Catherine, Mathieu, Jean-Paul, Morin, Christophe, Vidal, Michel, de Leiris, Joël, Comet, Michel, Fagret, Daniel
• Format: Article
• Language: English
• Subjects: Glucose transport; Iodinated analogues of glucose; Radiopharmaceuticals
• ISSN: 0969-8051; 1872-9614
• DOI: 10.1016/S0969-8051(97)00022-X

Two anomeric analogues of glucose labelled with 123 iodine in position 6, proposed as tracers of glucose transport in vivo, have been synthesized: α- and β-methyl-6-deoxy-6-iodo- d-glucopyranoside (αMDIG and βMDIG). The aim of this study was to determine whether these molecules interact with the glucose transporter and whether they could be used as tracers of glucose transport in vivo. The biodistribution of αMDIG and βMDIG was studied in the mouse in vivo. To determine if these two anomers enter the cell via the glucose transporter, their uptake was measured in isolated perfused rat hearts, in human erythrocytes in suspension, and in cardiomyocytes of neonatal rat in culture. Both αMDIG and βMDIG had similar repartitions in the mouse: myocardial uptake averaged 7% of the injected dose/g of organ at 2 min postinjection and αMDIG competed with d-glucose to enter the cells. Insulin produced a 123% increase of its uptake in isolated perfused rat hearts and a 100% increase in cardiomyocytes of neonatal rat in culture. αMDIG uptake was lowered in the presence of glucose transport inhibitors in each experimental model. An interaction between βMDIG and glucose transporters was observed only in human erythrocytes in suspension. Only αMDIG interacts with the glucose transporter, and thus could be used to estimate glucose transport in vivo.