Synthesis and assessment of [11C]acetylhomotaurine as an imaging agent for the study of the pharmacodynamic properties of acamprosate by positron emission tomography.

Acetylhomotaurine was labeled with (11)C via N-acetylation with [(11)C]acetyl chloride. The synthesis yielded 48.2+/-3.8%, decay corrected to end of bombardment. The specific activity of the (radio)chemically pure product was 20.8+/-2.0 GBq/micromol at EOS. In vivo studies revealed a very fast clearance of the tracer from the blood and a uniform distribution in the different brain regions. Unfortunately, the poor passage through the blood brain barrier makes the tracer not suitable for PET studies.