Synthesis of L-2,4-diamino[4-11C]butyric acid and its use in some in vitro and in vivo tumour models.
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.
Antoni
G
G
Subfemtomole Biorecognition Project, Research Development Corporation of Japan, Osaka.Gunnar.Antoni@pet.uu.se
Omura
H
H
Bergström
M
M
Furuya
Y
Y
Moulder
R
R
Roberto
A
A
Sundin
A
A
Watanabe
Y
Y
Långström
B
B
D000613:Aminobutyrates / Q000493:pharmacokinetics; D000818:Animals; D001345:Autoradiography; D002250:Carbon Radioisotopes; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging*; D051381:Rats; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D014407:Tumor Cells, Cultured
D000613:Aminobutyrates; D002250:Carbon Radioisotopes; C005959:2,4-diaminobutyric acid