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.
Courtyn
Jan
J
Laboratory for Analytical Chemistry, Institute for Nuclear Sciences, Ghent University, Proeftuinstraat 86, B-9000 Gent, Belgium. Jan.Courtyn@UGent.be
Cornelissen
Bart
B
Oltenfreiter
Ruth
R
Vandecapelle
Marleen
M
Slegers
Guido
G
Strijckmans
Karel
K
D000077443:Acamprosate; D000427:Alcohol Deterrents / Q000494:pharmacology; D000437:Alcoholism / Q000188:drug therapy; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000187:drug effects / Q000378:metabolism*; D002250:Carbon Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D008657:Metabolic Clearance Rate; D051379:Mice; D049268:Positron-Emission Tomography / Q000379:methods*; D011817:Rabbits; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D013654:Taurine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology*; D014018:Tissue Distribution; D016896:Treatment Outcome
D000427:Alcohol Deterrents; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D013654:Taurine; D000077443:Acamprosate