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No brain uptake? What is the mechanism?

Posted by Gelovani on 30 Nov 2009 at 17:28 GMT

The mechanism of accumulation of this fluorescent IR800 2-DG analogue remains uncertain, despite the authors' comparisons with mechanisms of accumulation of 2DG and 18F-FDG. If this compound sould be transported by the GLUT1 (or other variants) and/or phosphorylated by hexokinase, thenn it should accumulate in the brain cortex much more than the tumor.

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RE: No brain uptake? What is the mechanism?

dawen replied to Gelovani on 02 Dec 2009 at 22:24 GMT

Thanks for the comment. I totally agree with it. The pharmacokinetics of the IRDye 2DG are not very clear, despite a few studies (Kovar et al.) have shown that uptake of the 2DG dye is specifically blocked by GLUT1 inhibitor and also competitively inhibited by free 2DG. More mechanistic studies on uptake and also clearance will be needed. Distinguishing the tumor from surrounding normal brain observed ex vivo and microscopically 24 h postinjection may result from different clearance mechanism.

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