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Enzymatic synthesis and biodistribution in mice of β ‐O‐D‐galactopyranosyl‐(1,4′)‐2′‐[ 18 F]fluoro‐2′‐deoxy‐D‐glucopyranose (2′‐[ 18 F]fluorodeoxylactose]
Author(s) -
Bormans G.,
Verbruggen A.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.471
Subject(s) - biodistribution , chemistry , enzyme , clearance , in vivo , excretion , biochemistry , in vitro , medicine , microbiology and biotechnology , urology , biology
We have synthesized β ‐O‐ D ‐galactopyranosyl‐(1,4′)‐2′‐[ 18 F]fluoro‐2′‐deoxy‐ D ‐glucopyranose (2′‐[ 18 F]fluorodeoxylactose, 18 FDL) using an enzymatic method starting from 18 FDG in order to evaluate this compound with regard to its usefulness for in vivo visualization of the expression of the LacZ gene. Incubation of 18 FDL with β ‐galactosidase results in the formation of 18 FDG. Biodistribution studies in normal mice showed that 18 FDL is cleared by urinary excretion and is not retained in any tissue. Biodistribution in Rosa‐26 mice is identical to the biodistribution in normal mice, suggesting that 18 FDL is not able to cross the cell membrane. Copyright © 2001 John Wiley & Sons, Ltd.