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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