The pharmacokinetics of [11C]methoxy-norchloroprogabidic acid, a potential PET tracer for GABA receptors in the brain. |
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| Authors: | P Santens F De Vos D Bouden G Slegers I Lemahieu P Boon J De Reuck |
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| Affiliation: | Department of Neurology, PET-Centre, University Hospital and University of Gent, Belgium. santens@petsparc.rug.ac.be |
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| Abstract: | We have described the kinetic properties of [11C]methoxy-norchloroprogabidic acid, a potential radioligand for the gamma-aminobutyric acid (GABA) receptor. Early metabolism in mice was negligible. Protein binding in human plasma was 89 ± 7%. Distribution volumes were 89.6 ± 29.4 l whereas the elimination half-life was 41.6 ± 14.3 min. Animal and human positron emission tomography (PET) data demonstrate limited uptake of the activity in brain tissue. Displacement studies in mice suggest a nonsignificant fraction of specific receptor binding. [11C] Methoxy-norchloroprogabidic acid is therefore unsuitable for brain PET. |
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