Synthesis of L-2,4-diamino[4-11C]butyric acid and its use in some in vitro and in vivo tumour models

: Antoni G, Omura H, Bergström M, Furuya Y, Moulder R, Roberto A, Sundin A, Watanabe Y, Långström B

: 1997

: Nuclear Medicine and Biology

: Nuclear medicine and biology

: Nucl Med Biol

: 24

: 6

: 595

: 601

: 7

: 0969-8051

DOI: https://doi.org/10.1016/S0969-8051(97)00032-2

L-2,4-Diamino[4-11C]butyric acid (DAB) was synthesized by an enzyme catalysed carrier added (0.1 micromol KCN) reaction of hydrogen [11C]cyanide with O-acetyl-L-serine followed by reduction. L-[11C]DAB was obtained with a radiochemical purity higher than 96% and with a decay corrected radiochemical yield of 30-40% within a 32 min reaction time. The enantiomeric excess was 98%. The uptake of L-[11C]DAB was investigated in multicellular aggregates of six different cell lines and animal tumour models. L-[11C]DAB is potentially useful for the assessment of pharmacokinetics of L-DAB in vivo for part of its evaluation as an antitumoural agent, although its use for diagnostic purposes seems limited.