Synthesis and assessment of [11C]acetylhomotaurine as an imaging agent for the study of the pharmacodynamic properties of acamprosate by positron emission tomography.
Courtyn J., Cornelissen B., Oltenfreiter R., Vandecapelle M., Slegers G., Strijckmans K.
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.