Enzymatic synthesis and biodistribution in mice of β-O-D-galactopyranosyl-(1,4′)-2′-[1 18F]fluoro-2′-deoxy-D-glucopyranose (2′-[18F]fluorodeoxylactose)

We have synthesized beta -O-D-galactopyranosyl-(1,4')-2'-[F-18]fluoro-2'-deoxy-D-glucopyranose (2'-[F-18]fluorodeoxylactose, (FDL)-F-18) 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 (FDL)-F-18 with beta -galactosidase results in the formation of (18)FDG. Biodistribution studies in normal mice showed that (FDL)-F-18 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 (FDL)-F-18 is not able to cross the cell membrane. Copyright (C) 2001 John Wiley & Sons, Ltd.